Faculty Appointments
Research Professor of Pharmacology
Education
Ph.D., Organic Chemistry, Emory University, Atlanta, GeorgiaB.S., Chemistry, Mississippi State University, Starkville, Mississippi
Office Address
12415D MRB4
Nashville, TN 37232-6600
Nashville, TN 37232-6600
Research Description
My interests lie in the application of synthetic organic chemistry to questions of biological importance. Since 2001, I been engaged in medicinal chemistry toward primarily oncology related drug discovery efforts. Previous experience with the pharmaceutical industry included a key role in the discovery of dabrafenib, currently approved for the treatment of B-Raf positive metastatic melanoma.
Currently, I lead medicinal chemistry and project teams in the Fesik cancer drug discovery group. We employ fragment based drug discovery techniques to discover inhibitors of "undruggable" protein-protein interactions that are important for the future discovery of cancer therapeutics. Outside of the Fesik lab, I have also been involved in several collaborations, including active projects in the cancer, antibacterial, and antimalarial fields, and function as the Associate Director for Medicinal Chemistry in the Vanderbilt Institute of Chemical Biology.
I am also the Director and Scientific Coordinator of the Vanderbilt Center for Cancer Drug Discovery, a center in the NCI’s NExT Chemical Biology Consortium. The center, which is co-directed by Professor Stephen Fesik and Professor Gary Sulikowski, was originally created in 2009, and engages in collaborative efforts with other centers across the country to discovery drug candidates for novel and challenging targets for cancer treatment.
Currently, I lead medicinal chemistry and project teams in the Fesik cancer drug discovery group. We employ fragment based drug discovery techniques to discover inhibitors of "undruggable" protein-protein interactions that are important for the future discovery of cancer therapeutics. Outside of the Fesik lab, I have also been involved in several collaborations, including active projects in the cancer, antibacterial, and antimalarial fields, and function as the Associate Director for Medicinal Chemistry in the Vanderbilt Institute of Chemical Biology.
I am also the Director and Scientific Coordinator of the Vanderbilt Center for Cancer Drug Discovery, a center in the NCI’s NExT Chemical Biology Consortium. The center, which is co-directed by Professor Stephen Fesik and Professor Gary Sulikowski, was originally created in 2009, and engages in collaborative efforts with other centers across the country to discovery drug candidates for novel and challenging targets for cancer treatment.
Research Keywords
Oncology medicinal chemistry and drug discovery
Publications
Bröker J, Waterson AG, Smethurst C, Kessler D, Böttcher J, Mayer M, Gmaschitz G, Phan J, Little A, Abbott JR, Sun Q, Gmachl M, Rudolph D, Arnhof H, Rumpel K, Savarese F, Gerstberger T, Mischerikow N, Treu M, Herdeis L, Wunberg T, Gollner A, Weinstabl H, Mantoulidis A, Krämer O, McConnell DB, W Fesik S. Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor. J Med Chem [print-electronic]. 2022 Oct 10/27/2022; PMID: 36300829, DOI: 10.1021/acs.jmedchem.2c01120, ISSN: 1520-4804.
Fricke N, Raghunathan K, Tiwari A, Stefanski KM, Balakrishnan M, Waterson AG, Capone R, Huang H, Sanders CR, Bauer JA, Kenworthy AK. High-Content Imaging Platform to Discover Chemical Modulators of Plasma Membrane Rafts. ACS Cent Sci [print-electronic]. 2022 Mar 3/23/2022; 8(3): 370-8. PMID: 35355811, PMCID: PMC8961798, DOI: 10.1021/acscentsci.1c01058, ISSN: 2374-7943.
Drury SL, Miller AR, Laut CL, Walter AB, Bennett MR, Su M, Bai M, Jing B, Joseph SB, Metzger EJ, Bane CE, Black CC, Macdonald MT, Dutter BF, Romaine IM, Waterson AG, Sulikowski GA, Jansen ED, Crowe JE, Sciotti RJ, Skaar EP. Simultaneous Exposure to Intracellular and Extracellular Photosensitizers for the Treatment of Staphylococcus aureus Infections. Antimicrob Agents Chemother [print-electronic]. 2021 Nov 11/17/2021; 65(12): e0091921. PMID: 34516248, PMCID: PMC8597735, DOI: 10.1128/AAC.00919-21, ISSN: 1098-6596.
Kozlyuk N, Gilston BA, Salay LE, Gogliotti RD, Christov PP, Kim K, Ovee M, Waterson AG, Chazin WJ. A fragment-based approach to discovery of Receptor for Advanced Glycation End products inhibitors. Proteins [print-electronic]. 2021 Nov; 89(11): 1399-412. PMID: 34156100, PMCID: PMC8492516, DOI: 10.1002/prot.26162, ISSN: 1097-0134.
Christov PP, Kim K, Jana S, Romaine IM, Rai G, Mott BT, Allweil AA, Lamers A, Brimacombe KR, Urban DJ, Lee TD, Hu X, Lukacs CM, Davies DR, Jadhav A, Hall MD, Green N, Moore WJ, Stott GM, Flint AJ, Maloney DJ, Sulikowski GA, Waterson AG. Optimization of ether and aniline based inhibitors of lactate dehydrogenase. Bioorg Med Chem Lett [print-electronic]. 2021 Jun 6/1/2021; 41: 127974. PMID: 33771585, PMCID: PMC8113097, PII: S0960-894X(21)00200-6, DOI: 10.1016/j.bmcl.2021.127974, ISSN: 1464-3405.
Kim K, Christov PP, Romaine I, Tian J, Jana S, Lamers AP, Dutter BF, Scaggs T, Jeon K, Guttentag B, Weaver CD, Lindsley CW, Waterson AG, Sulikowski GA. Ten-Year Retrospective of the Vanderbilt Institute of Chemical Biology Chemical Synthesis Core. ACS Chem Biol [print-electronic]. 2021 May 5/21/2021; 16(5): 787-93. PMID: 33877812, DOI: 10.1021/acschembio.0c00818, ISSN: 1554-8937.
Rai G, Urban DJ, Mott BT, Hu X, Yang SM, Benavides GA, Johnson MS, Squadrito GL, Brimacombe KR, Lee TD, Cheff DM, Zhu H, Henderson MJ, Pohida K, Sulikowski GA, Dranow DM, Kabir M, Shah P, Padilha E, Tao D, Fang Y, Christov PP, Kim K, Jana S, Muttil P, Anderson T, Kunda NK, Hathaway HJ, Kusewitt DF, Oshima N, Cherukuri M, Davies DR, Norenberg JP, Sklar LA, Moore WJ, Dang CV, Stott GM, Neckers L, Flint AJ, Darley-Usmar VM, Simeonov A, Waterson AG, Jadhav A, Hall MD, Maloney DJ. Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties. J Med Chem [print-electronic]. 2020 Oct 10/8/2020; 63(19): 10984-1011. PMID: 32902275, PMCID: PMC7830743, DOI: 10.1021/acs.jmedchem.0c00916, ISSN: 1520-4804.
Sarkar D, Olejniczak ET, Phan J, Coker JA, Sai J, Arnold A, Beesetty Y, Waterson AG, Fesik SW. Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods. J Med Chem [print-electronic]. 2020 Aug 8/13/2020; 63(15): 8325-37. PMID: 32673492, DOI: 10.1021/acs.jmedchem.0c00511, ISSN: 1520-4804.
Chacón Simon S, Wang F, Thomas LR, Phan J, Zhao B, Olejniczak ET, Macdonald JD, Shaw JG, Schlund C, Payne W, Creighton J, Stauffer SR, Waterson AG, Tansey WP, Fesik SW. Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design. J Med Chem [print-electronic]. 2020 Apr 4/23/2020; 63(8): 4315-33. PMID: 32223236, PMCID: PMC7187413, DOI: 10.1021/acs.jmedchem.0c00224, ISSN: 1520-4804.
Oshima N, Ishida R, Kishimoto S, Beebe K, Brender JR, Yamamoto K, Urban D, Rai G, Johnson MS, Benavides G, Squadrito GL, Crooks D, Jackson J, Joshi A, Mott BT, Shrimp JH, Moses MA, Lee MJ, Yuno A, Lee TD, Hu X, Anderson T, Kusewitt D, Hathaway HH, Jadhav A, Picard D, Trepel JB, Mitchell JB, Stott GM, Moore W, Simeonov A, Sklar LA, Norenberg JP, Linehan WM, Maloney DJ, Dang CV, Waterson AG, Hall M, Darley-Usmar VM, Krishna MC, Neckers LM. Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy. Cell Rep. 2020 Feb 2/11/2020; 30(6): 1798-1810.e4. PMID: 32049011, PMCID: PMC7039685, PII: S2211-1247(20)30054-1, DOI: 10.1016/j.celrep.2020.01.039, ISSN: 2211-1247.
Macdonald JD, Chacón Simon S, Han C, Wang F, Shaw JG, Howes JE, Sai J, Yuh JP, Camper D, Alicie BM, Alvarado J, Nikhar S, Payne W, Aho ER, Bauer JA, Zhao B, Phan J, Thomas LR, Rossanese OW, Tansey WP, Waterson AG, Stauffer SR, Fesik SW. Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J Med Chem [print-electronic]. 2019 Dec 12/26/2019; 62(24): 11232-59. PMID: 31724864, PMCID: PMC6933084, DOI: 10.1021/acs.jmedchem.9b01411, ISSN: 1520-4804.
Akan DT, Howes JE, Sai J, Arnold AL, Beesetty Y, Phan J, Olejniczak ET, Waterson AG, Fesik SW. Small Molecule SOS1 Agonists Modulate MAPK and PI3K Signaling via Independent Cellular Responses. ACS Chem Biol [print-electronic]. 2019 Mar 3/15/2019; 14(3): 325-31. PMID: 30735352, DOI: 10.1021/acschembio.8b00869, ISSN: 1554-8937.
Dumas ME, Chen GY, Kendrick ND, Xu G, Larsen SD, Jana S, Waterson AG, Bauer JA, Hancock W, Sulikowski GA, Ohi R. Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes. Bioorg Med Chem Lett [print-electronic]. 2019 Jan 1/15/2019; 29(2): 148-54. PMID: 30528696, PMCID: PMC6681659, PII: S0960-894X(18)30942-9, DOI: 10.1016/j.bmcl.2018.12.008, ISSN: 1464-3405.
Waterson AG, Scott SA, Kett NR, Blobaum AL, Alex Brown H, Lindsley CW. Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives. Bioorg Med Chem Lett [print-electronic]. 2018 Dec 12/15/2018; 28(23-24): 3670-3. PMID: 30528979, PII: S0960-894X(18)30835-7, DOI: 10.1016/j.bmcl.2018.10.033, ISSN: 1464-3405.
Hodges TR, Abbott JR, Little AJ, Sarkar D, Salovich JM, Howes JE, Akan DT, Sai J, Arnold AL, Browning C, Burns MC, Sobolik T, Sun Q, Beesetty Y, Coker JA, Scharn D, Stadtmueller H, Rossanese OW, Phan J, Waterson AG, McConnell DB, Fesik SW. Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS. J Med Chem [print-electronic]. 2018 Oct 10/11/2018; 61(19): 8875-94. PMID: 30205005, PMCID: PMC8314423, DOI: 10.1021/acs.jmedchem.8b01108, ISSN: 1520-4804.
Abbott JR, Patel PA, Howes JE, Akan DT, Kennedy JP, Burns MC, Browning CF, Sun Q, Rossanese OW, Phan J, Waterson AG, Fesik SW. Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS. ACS Med Chem Lett. 2018 Sep 9/13/2018; 9(9): 941-6. PMID: 30258545, PMCID: PMC6142059, DOI: 10.1021/acsmedchemlett.8b00296, ISSN: 1948-5875.
Abbott JR, Hodges TR, Daniels RN, Patel PA, Kennedy JP, Howes JE, Akan DT, Burns MC, Sai J, Sobolik T, Beesetty Y, Lee T, Rossanese OW, Phan J, Waterson AG, Fesik SW. Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling. J Med Chem [print-electronic]. 2018 Jul 7/26/2018; 61(14): 6002-17. PMID: 29856609, DOI: 10.1021/acs.jmedchem.8b00360, ISSN: 1520-4804.
Burns MC, Howes JE, Sun Q, Little AJ, Camper DV, Abbott JR, Phan J, Lee T, Waterson AG, Rossanese OW, Fesik SW. High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling. Anal Biochem [print-electronic]. 2018 May 5/1/2018; 548: 44-52. PMID: 29444450, PMCID: PMC5935105, PII: S0003-2697(18)30058-7, DOI: 10.1016/j.ab.2018.01.025, ISSN: 1096-0309.
Howes JE, Akan DT, Burns MC, Rossanese OW, Waterson AG, Fesik SW. Small Molecule-Mediated Activation of RAS Elicits Biphasic Modulation of Phospho-ERK Levels that Are Regulated through Negative Feedback on SOS1. Mol Cancer Ther [print-electronic]. 2018 May; 17(5): 1051-60. PMID: 29440291, PII: 1535-7163.MCT-17-0666, DOI: 10.1158/1535-7163.MCT-17-0666, ISSN: 1538-8514.
Padmanabhan C, Rellinger EJ, Zhu J, An H, Woodbury LG, Chung DH, Waterson AG, Lindsley CW, Means AL, Beauchamp RD. CFLIP critically modulates apoptotic resistance in epithelial-to-mesenchymal transition. Oncotarget. 2017 Nov 11/24/2017; 8(60): 101072-86. PMID: 29254146, PMCID: PMC5731856, PII: 19557, DOI: 10.18632/oncotarget.19557, ISSN: 1949-2553.
Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ. Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH). J Med Chem [print-electronic]. 2017 Nov 11/22/2017; 60(22): 9184-204. PMID: 29120638, PMCID: PMC5894102, DOI: 10.1021/acs.jmedchem.7b00941, ISSN: 1520-4804.
Rellinger EJ, Padmanabhan C, Qiao J, Craig BT, An H, Zhu J, Correa H, Waterson AG, Lindsley CW, Beauchamp RD, Chung DH. Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma. Oncotarget. 2017 Oct 10/31/2017; 8(53): 91040-51. PMID: 29207623, PMCID: PMC5710904, PII: 19406, DOI: 10.18632/oncotarget.19406, ISSN: 1949-2553.
Rellinger EJ, Padmanabhan C, Qiao J, Appert A, Waterson AG, Lindsley CW, Beauchamp RD, Chung DH. ML327 induces apoptosis and sensitizes Ewing sarcoma cells to TNF-related apoptosis-inducing ligand. Biochem Biophys Res Commun [print-electronic]. 2017 Sep 9/16/2017; 491(2): 463-8. PMID: 28716733, PMCID: PMC5564678, PII: S0006-291X(17)31392-X, DOI: 10.1016/j.bbrc.2017.07.050, ISSN: 1090-2104.
Patrone JD, Waterson AG, Fesik SW. Recent advancements in the discovery of protein-protein interaction inhibitors of replication protein A. Medchemcomm. 2017 Feb 2/1/2017; 8(2): 259-67. PMID: 30108742, PMCID: PMC6071986, PII: c6md00460a, DOI: 10.1039/c6md00460a, ISSN: 2040-2503.
Patrone JD, Pelz NF, Bates BS, Souza-Fagundes EM, Vangamudi B, Camper DV, Kuznetsov AG, Browning CF, Feldkamp MD, Frank AO, Gilston BA, Olejniczak ET, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW. Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A. ChemMedChem [print-electronic]. 2016 Apr 4/19/2016; 11(8): 893-9. PMID: 26748787, PMCID: PMC4838552, DOI: 10.1002/cmdc.201500479, ISSN: 1860-7187.
Brogan JT, Stoops SL, Brady S, An H, Weaver C, Daniels JS, Beauchamp RD, Lindsley CW, Waterson AG. Optimization of a small molecule probe that restores e-cadherin expression. Bioorg. Med. Chem. Lett [print-electronic]. 2015 Oct 10/1/2015; 25(19): 4260-4. PMID: 26299347, PMCID: PMC4567403, PII: S0960-894X(15)00823-9, DOI: 10.1016/j.bmcl.2015.07.104, ISSN: 1464-3405.
An H, Stoops SL, Deane NG, Zhu J, Zi J, Weaver C, Waterson AG, Zijlstra A, Lindsley CW, Beauchamp RD. Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition. Oncotarget. 2015 Sep 9/8/2015; 6(26): 22934-48. PMID: 26082441, PMCID: PMC4673210, PII: 4473, DOI: 10.18632/oncotarget.4473, ISSN: 1949-2553.
Waterson AG, Kennedy JP, Patrone JD, Pelz NF, Feldkamp MD, Frank AO, Vangamudi B, Souza-Fagundes EM, Rossanese OW, Chazin WJ, Fesik SW. Diphenylpyrazoles as replication protein a inhibitors. ACS Med Chem Lett. 2015 Feb 2/12/2015; 6(2): 140-5. PMID: 25699140, PMCID: PMC4329576, DOI: 10.1021/ml5003629, ISSN: 1948-5875.
Romaine IM, Taylor RW, Saidu SP, Kim K, Sulikowski GA, Zwiebel LJ, Waterson AG. Narrow SAR in odorant sensing Orco receptor agonists. Bioorg. Med. Chem. Lett [print-electronic]. 2014 Jun 6/15/2014; 24(12): 2613-6. PMID: 24813736, PMCID: PMC4111141, PII: S0960-894X(14)00438-7, DOI: 10.1016/j.bmcl.2014.04.081, ISSN: 1464-3405.
Frank AO, Vangamudi B, Feldkamp MD, Souza-Fagundes EM, Luzwick JW, Cortez D, Olejniczak ET, Waterson AG, Rossanese OW, Chazin WJ, Fesik SW. Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A. J. Med. Chem [print-electronic]. 2014 Mar 3/27/2014; 57(6): 2455-61. PMID: 24491171, PMCID: PMC3969094, DOI: 10.1021/jm401730y, ISSN: 1520-4804.
Burns MC, Sun Q, Daniels RN, Camper D, Kennedy JP, Phan J, Olejniczak ET, Lee T, Waterson AG, Rossanese OW, Fesik SW. Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2014 Mar 3/4/2014; 111(9): 3401-6. PMID: 24550516, PMCID: PMC3948241, PII: 1315798111, DOI: 10.1073/pnas.1315798111, ISSN: 1091-6490.
Frank AO, Feldkamp MD, Kennedy JP, Waterson AG, Pelz NF, Patrone JD, Vangamudi B, Camper DV, Rossanese OW, Chazin WJ, Fesik SW. Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragment-linking approach. J. Med. Chem [print-electronic]. 2013 Nov 11/27/2013; 56(22): 9242-50. PMID: 24147804, PMCID: PMC3932990, DOI: 10.1021/jm401333u, ISSN: 1520-4804.
Feldkamp MD, Frank AO, Kennedy JP, Patrone JD, Vangamudi B, Waterson AG, Fesik SW, Chazin WJ. Surface reengineering of RPA70N enables cocrystallization with an inhibitor of the replication protein A interaction motif of ATR interacting protein. Biochemistry [print-electronic]. 2013 Sep 9/17/2013; 52(37): 6515-24. PMID: 23962067, PMCID: PMC3804075, DOI: 10.1021/bi400542z, ISSN: 1520-4995.
Patrone JD, Kennedy JP, Frank AO, Feldkamp MD, Vangamudi B, Pelz NF, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW. Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A. ACS Med Chem Lett. 2013 Jul 7/11/2013; 4(7): 601-5. PMID: 23914285, PMCID: PMC3728914, DOI: 10.1021/ml400032y, ISSN: 1948-5875.
Taylor RW, Romaine IM, Liu C, Murthi P, Jones PL, Waterson AG, Sulikowski GA, Zwiebel LJ. Structure-activity relationship of a broad-spectrum insect odorant receptor agonist. ACS Chem. Biol [print-electronic]. 2012 Oct 10/19/2012; 7(10): 1647-52. PMID: 22924767, DOI: 10.1021/cb300331z, ISSN: 1554-8937.
Delpire E, Baranczak A, Waterson AG, Kim K, Kett N, Morrison RD, Daniels JS, Weaver CD, Lindsley CW. Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorg. Med. Chem. Lett [print-electronic]. 2012 Jul 7/15/2012; 22(14): 4532-5. PMID: 22727639, PMCID: PMC3389279, PII: S0960-894X(12)00738-X, DOI: 10.1016/j.bmcl.2012.05.126, ISSN: 1464-3405.
Sun Q, Burke JP, Phan J, Burns MC, Olejniczak ET, Waterson AG, Lee T, Rossanese OW, Fesik SW. Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation. Angew. Chem. Int. Ed. Engl [print-electronic]. 2012 Jun 6/18/2012; 51(25): 6140-3. PMID: 22566140, PMCID: PMC3620661, DOI: 10.1002/anie.201201358, ISSN: 1521-3773.
Vangamudi, B.; Ayres, A. E.; Burke, J. P.; Waterson, A. G.; Rossanese, O. W.; Fesik, S. W., editor.. Evaluation of TBK1 as a novel cancer target in the K-Ras pathway.
Jones PL, Pask GM, Romaine IM, Taylor RW, Reid PR, Waterson AG, Sulikowski GA, Zwiebel LJ. Allosteric antagonism of insect odorant receptor ion channels. PLoS ONE [print-electronic]. 2012; 7(1): e30304. PMID: 22272331, PMCID: PMC3260273, PII: PONE-D-11-19400, DOI: 10.1371/journal.pone.0030304, ISSN: 1932-6203.
Stellwagen JC, Adjabeng GM, Arnone MR, Dickerson SH, Han C, Hornberger KR, King AJ, Mook RA, Petrov KG, Rheault TR, Rominger CM, Rossanese OW, Smitheman KN, Waterson AG, Uehling DE. Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup. Bioorg. Med. Chem. Lett [print-electronic]. 2011 Aug 8/1/2011; 21(15): 4436-40. PMID: 21733693, PII: S0960-894X(11)00804-3, DOI: 10.1016/j.bmcl.2011.06.021, ISSN: 1464-3405.
Stoops SL, Pearson AS, Weaver C, Waterson AG, Days E, Farmer C, Brady S, Weaver CD, Beauchamp RD, Lindsley CW. Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells. ACS Chem. Biol [print-electronic]. 2011 May 5/20/2011; 6(5): 452-65. PMID: 21241068, PMCID: PMC3401128, DOI: 10.1021/cb100305h, ISSN: 1554-8937.
Thorne CA, Hanson AJ, Schneider J, Tahinci E, Orton D, Cselenyi CS, Jernigan KK, Meyers KC, Hang BI, Waterson AG, Kim K, Melancon B, Ghidu VP, Sulikowski GA, LaFleur B, Salic A, Lee LA, Miller DM, Lee E. Small-molecule inhibition of Wnt signaling through activation of casein kinase 1a. Nat. Chem. Biol [print-electronic]. 2010 Nov; 6(11): 829-36. PMID: 20890287, PMCID: PMC3681608, PII: nchembio.453, DOI: 10.1038/nchembio.453, ISSN: 1552-4469.
Bhagwanth S, Waterson AG, Adjabeng GM, Hornberger KR. Room-temperature Pd-catalyzed amidation of aryl bromides using tert-butyl carbamate. J. Org. Chem. 2009 Jun 6/19/2009; 74(12): 4634-7. PMID: 19518153, DOI: 10.1021/jo9004537, ISSN: 1520-6904.
Waterson AG, Petrov KG, Hornberger KR, Hubbard RD, Sammond DM, Smith SC, Dickson HD, Caferro TR, Hinkle KW, Stevens KL, Dickerson SH, Rusnak DW, Spehar GM, Wood ER, Griffin RJ, Uehling DE. Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors. Bioorg. Med. Chem. Lett [print-electronic]. 2009 Mar 3/1/2009; 19(5): 1332-6. PMID: 19208477, PII: S0960-894X(09)00081-X, DOI: 10.1016/j.bmcl.2009.01.080, ISSN: 1464-3405.
Laquere, S.; Arnone, M.; Moss, K.; Yang, J.; Fisher, K.; Kane-Carson, L.; Smitheman, K.; Ward, J.; Heidrich, B.; Rheault, T.; Adjebeng, G.; Hornberger, K.; Stellwagen, J.; Waterson, A.; Han, C.; Mook, Jr. R. A.; Uehling, D.; King, A. J., editor.. A selective Raf kinase inhibitor induces cell death and tumor regression of human cancer cell lines encoding R-Raf V600E mutation.
Waterson, A. G. Delpire, E.; Days, E.; Lewis, M.; Kim, K.; Lindsley, C. W.; Weaver, C. D., editor.. Small molecule inhibitors of the KCC2 neuronal co-transporter.
Stevens KL, Alligood KJ, Alberti JG, Caferro TR, Chamberlain SD, Dickerson SH, Dickson HD, Emerson HK, Griffin RJ, Hubbard RD, Keith BR, Mullin RJ, Petrov KG, Gerding RM, Reno MJ, Rheault TR, Rusnak DW, Sammond DM, Smith SC, Uehling DE, Waterson AG, Wood ER. Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. Bioorg. Med. Chem. Lett [print-electronic]. 2009 Jan 1/1/2009; 19(1): 21-6. PMID: 19028424, PII: S0960-894X(08)01392-9, DOI: 10.1016/j.bmcl.2008.11.023, ISSN: 1464-3405.
Schaaf, G. M.; Mukherjee, S.; Waterson, A. G.. Conjugate addition of sodium methanesulfinate to vinyl pyridines and diazines for the synthesis of aliphatic sulfones. Tetrahedron Lett. 2009; 50: 1928-33.
Hubbard RD, Dickerson SH, Emerson HK, Griffin RJ, Reno MJ, Hornberger KR, Rusnak DW, Wood ER, Uehling DE, Waterson AG. Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Nov 11/1/2008; 18(21): 5738-40. PMID: 18842405, PII: S0960-894X(08)01162-1, DOI: 10.1016/j.bmcl.2008.09.090, ISSN: 1464-3405.
Wood ER, Shewchuk LM, Ellis B, Brignola P, Brashear RL, Caferro TR, Dickerson SH, Dickson HD, Donaldson KH, Gaul M, Griffin RJ, Hassell AM, Keith B, Mullin R, Petrov KG, Reno MJ, Rusnak DW, Tadepalli SM, Ulrich JC, Wagner CD, Vanderwall DE, Waterson AG, Williams JD, White WL, Uehling DE. 6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2008 Feb 2/26/2008; 105(8): 2773-8. PMID: 18287036, PMCID: PMC2268535, PII: 0708281105, DOI: 10.1073/pnas.0708281105, ISSN: 1091-6490.
Waterson AG, Stevens KL, Reno MJ, Zhang YM, Boros EE, Bouvier F, Rastagar A, Uehling DE, Dickerson SH, Reep B, McDonald OB, Wood ER, Rusnak DW, Alligood KJ, Rudolph SK. Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors. Bioorg. Med. Chem. Lett [print-electronic]. 2006 May 5/1/2006; 16(9): 2419-22. PMID: 16483772, PII: S0960-894X(06)00153-3, DOI: 10.1016/j.bmcl.2006.01.111, ISSN: 0960-894X.
Padwa, A.; Waterson, A. G.. A novel synthesis of polysubstituted phenols using the SnAr reaction of 2,5-dinitrofuran.â€. ARKIVOC. 2001; 4: 29-42.
Waterson, A. G.; Meyers, A. I.. Studies directed toward the synthesis of Viridenomycin. Route 2: a second-generation approach. Tetrahedron Lett. 2001; 42: 4305-8.
Waterson AG, Meyers AI. Bicyclic lactams as chiral homoenolate equivalents: synthesis of (-)-penienone. J. Org. Chem. 2000 Oct 10/20/2000; 65(21): 7240-3. PMID: 11031061, ISSN: 0022-3263.
Padwa A, Waterson AG. Studies dealing with thionium ion promoted mannich cyclization reactions. J. Org. Chem. 2000 Jan 1/14/2000; 65(1): 235-44. PMID: 10813921, PII: jo991414h, ISSN: 0022-3263.
Padwa, A.; Waterson, A. G.. The thionium/N-acyliminium ion cyclization cascade as a strategy for the synthesis of azapolycyclic ring systems. Tetrahedron. 2000; ((56)): 10159-73.
Padwa, A.; Waterson, A. G.. Synthesis of nitrogen heterocycles using the intramolecular Pummerer reaction [editorial]. Curr. Org. Chem. 2000; 4: 175-203.
Padwa, A.; Waterson, A.G.. Synthesis of the perhydroindolizine nucleus by a Pummerer/Mannich induced cyclization cascade. Tetrahedron Lett. 1998; 39: 3986-97.
Padwa, A.; Dimitroff, M.; Waterson, A. G.; Wu, T.. IMDAF cycloaddition as a method for the preparation of pyrrolophenanthridine alkaloids. J. Org. Chem. 1998; 63: 8585-8.
Padwa, A.; Dimitroff, M.; Waterson, A. G.; Wu, T.. Diels-Alder reaction of 2-amino-substituted furans as a method for preparing substituted anilines. J. Org. Chem. 1997; 62: 4088-96.
Fricke N, Raghunathan K, Tiwari A, Stefanski KM, Balakrishnan M, Waterson AG, Capone R, Huang H, Sanders CR, Bauer JA, Kenworthy AK. High-Content Imaging Platform to Discover Chemical Modulators of Plasma Membrane Rafts. ACS Cent Sci [print-electronic]. 2022 Mar 3/23/2022; 8(3): 370-8. PMID: 35355811, PMCID: PMC8961798, DOI: 10.1021/acscentsci.1c01058, ISSN: 2374-7943.
Drury SL, Miller AR, Laut CL, Walter AB, Bennett MR, Su M, Bai M, Jing B, Joseph SB, Metzger EJ, Bane CE, Black CC, Macdonald MT, Dutter BF, Romaine IM, Waterson AG, Sulikowski GA, Jansen ED, Crowe JE, Sciotti RJ, Skaar EP. Simultaneous Exposure to Intracellular and Extracellular Photosensitizers for the Treatment of Staphylococcus aureus Infections. Antimicrob Agents Chemother [print-electronic]. 2021 Nov 11/17/2021; 65(12): e0091921. PMID: 34516248, PMCID: PMC8597735, DOI: 10.1128/AAC.00919-21, ISSN: 1098-6596.
Kozlyuk N, Gilston BA, Salay LE, Gogliotti RD, Christov PP, Kim K, Ovee M, Waterson AG, Chazin WJ. A fragment-based approach to discovery of Receptor for Advanced Glycation End products inhibitors. Proteins [print-electronic]. 2021 Nov; 89(11): 1399-412. PMID: 34156100, PMCID: PMC8492516, DOI: 10.1002/prot.26162, ISSN: 1097-0134.
Christov PP, Kim K, Jana S, Romaine IM, Rai G, Mott BT, Allweil AA, Lamers A, Brimacombe KR, Urban DJ, Lee TD, Hu X, Lukacs CM, Davies DR, Jadhav A, Hall MD, Green N, Moore WJ, Stott GM, Flint AJ, Maloney DJ, Sulikowski GA, Waterson AG. Optimization of ether and aniline based inhibitors of lactate dehydrogenase. Bioorg Med Chem Lett [print-electronic]. 2021 Jun 6/1/2021; 41: 127974. PMID: 33771585, PMCID: PMC8113097, PII: S0960-894X(21)00200-6, DOI: 10.1016/j.bmcl.2021.127974, ISSN: 1464-3405.
Kim K, Christov PP, Romaine I, Tian J, Jana S, Lamers AP, Dutter BF, Scaggs T, Jeon K, Guttentag B, Weaver CD, Lindsley CW, Waterson AG, Sulikowski GA. Ten-Year Retrospective of the Vanderbilt Institute of Chemical Biology Chemical Synthesis Core. ACS Chem Biol [print-electronic]. 2021 May 5/21/2021; 16(5): 787-93. PMID: 33877812, DOI: 10.1021/acschembio.0c00818, ISSN: 1554-8937.
Rai G, Urban DJ, Mott BT, Hu X, Yang SM, Benavides GA, Johnson MS, Squadrito GL, Brimacombe KR, Lee TD, Cheff DM, Zhu H, Henderson MJ, Pohida K, Sulikowski GA, Dranow DM, Kabir M, Shah P, Padilha E, Tao D, Fang Y, Christov PP, Kim K, Jana S, Muttil P, Anderson T, Kunda NK, Hathaway HJ, Kusewitt DF, Oshima N, Cherukuri M, Davies DR, Norenberg JP, Sklar LA, Moore WJ, Dang CV, Stott GM, Neckers L, Flint AJ, Darley-Usmar VM, Simeonov A, Waterson AG, Jadhav A, Hall MD, Maloney DJ. Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties. J Med Chem [print-electronic]. 2020 Oct 10/8/2020; 63(19): 10984-1011. PMID: 32902275, PMCID: PMC7830743, DOI: 10.1021/acs.jmedchem.0c00916, ISSN: 1520-4804.
Sarkar D, Olejniczak ET, Phan J, Coker JA, Sai J, Arnold A, Beesetty Y, Waterson AG, Fesik SW. Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods. J Med Chem [print-electronic]. 2020 Aug 8/13/2020; 63(15): 8325-37. PMID: 32673492, DOI: 10.1021/acs.jmedchem.0c00511, ISSN: 1520-4804.
Chacón Simon S, Wang F, Thomas LR, Phan J, Zhao B, Olejniczak ET, Macdonald JD, Shaw JG, Schlund C, Payne W, Creighton J, Stauffer SR, Waterson AG, Tansey WP, Fesik SW. Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design. J Med Chem [print-electronic]. 2020 Apr 4/23/2020; 63(8): 4315-33. PMID: 32223236, PMCID: PMC7187413, DOI: 10.1021/acs.jmedchem.0c00224, ISSN: 1520-4804.
Oshima N, Ishida R, Kishimoto S, Beebe K, Brender JR, Yamamoto K, Urban D, Rai G, Johnson MS, Benavides G, Squadrito GL, Crooks D, Jackson J, Joshi A, Mott BT, Shrimp JH, Moses MA, Lee MJ, Yuno A, Lee TD, Hu X, Anderson T, Kusewitt D, Hathaway HH, Jadhav A, Picard D, Trepel JB, Mitchell JB, Stott GM, Moore W, Simeonov A, Sklar LA, Norenberg JP, Linehan WM, Maloney DJ, Dang CV, Waterson AG, Hall M, Darley-Usmar VM, Krishna MC, Neckers LM. Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy. Cell Rep. 2020 Feb 2/11/2020; 30(6): 1798-1810.e4. PMID: 32049011, PMCID: PMC7039685, PII: S2211-1247(20)30054-1, DOI: 10.1016/j.celrep.2020.01.039, ISSN: 2211-1247.
Macdonald JD, Chacón Simon S, Han C, Wang F, Shaw JG, Howes JE, Sai J, Yuh JP, Camper D, Alicie BM, Alvarado J, Nikhar S, Payne W, Aho ER, Bauer JA, Zhao B, Phan J, Thomas LR, Rossanese OW, Tansey WP, Waterson AG, Stauffer SR, Fesik SW. Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J Med Chem [print-electronic]. 2019 Dec 12/26/2019; 62(24): 11232-59. PMID: 31724864, PMCID: PMC6933084, DOI: 10.1021/acs.jmedchem.9b01411, ISSN: 1520-4804.
Akan DT, Howes JE, Sai J, Arnold AL, Beesetty Y, Phan J, Olejniczak ET, Waterson AG, Fesik SW. Small Molecule SOS1 Agonists Modulate MAPK and PI3K Signaling via Independent Cellular Responses. ACS Chem Biol [print-electronic]. 2019 Mar 3/15/2019; 14(3): 325-31. PMID: 30735352, DOI: 10.1021/acschembio.8b00869, ISSN: 1554-8937.
Dumas ME, Chen GY, Kendrick ND, Xu G, Larsen SD, Jana S, Waterson AG, Bauer JA, Hancock W, Sulikowski GA, Ohi R. Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes. Bioorg Med Chem Lett [print-electronic]. 2019 Jan 1/15/2019; 29(2): 148-54. PMID: 30528696, PMCID: PMC6681659, PII: S0960-894X(18)30942-9, DOI: 10.1016/j.bmcl.2018.12.008, ISSN: 1464-3405.
Waterson AG, Scott SA, Kett NR, Blobaum AL, Alex Brown H, Lindsley CW. Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives. Bioorg Med Chem Lett [print-electronic]. 2018 Dec 12/15/2018; 28(23-24): 3670-3. PMID: 30528979, PII: S0960-894X(18)30835-7, DOI: 10.1016/j.bmcl.2018.10.033, ISSN: 1464-3405.
Hodges TR, Abbott JR, Little AJ, Sarkar D, Salovich JM, Howes JE, Akan DT, Sai J, Arnold AL, Browning C, Burns MC, Sobolik T, Sun Q, Beesetty Y, Coker JA, Scharn D, Stadtmueller H, Rossanese OW, Phan J, Waterson AG, McConnell DB, Fesik SW. Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS. J Med Chem [print-electronic]. 2018 Oct 10/11/2018; 61(19): 8875-94. PMID: 30205005, PMCID: PMC8314423, DOI: 10.1021/acs.jmedchem.8b01108, ISSN: 1520-4804.
Abbott JR, Patel PA, Howes JE, Akan DT, Kennedy JP, Burns MC, Browning CF, Sun Q, Rossanese OW, Phan J, Waterson AG, Fesik SW. Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS. ACS Med Chem Lett. 2018 Sep 9/13/2018; 9(9): 941-6. PMID: 30258545, PMCID: PMC6142059, DOI: 10.1021/acsmedchemlett.8b00296, ISSN: 1948-5875.
Abbott JR, Hodges TR, Daniels RN, Patel PA, Kennedy JP, Howes JE, Akan DT, Burns MC, Sai J, Sobolik T, Beesetty Y, Lee T, Rossanese OW, Phan J, Waterson AG, Fesik SW. Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling. J Med Chem [print-electronic]. 2018 Jul 7/26/2018; 61(14): 6002-17. PMID: 29856609, DOI: 10.1021/acs.jmedchem.8b00360, ISSN: 1520-4804.
Burns MC, Howes JE, Sun Q, Little AJ, Camper DV, Abbott JR, Phan J, Lee T, Waterson AG, Rossanese OW, Fesik SW. High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling. Anal Biochem [print-electronic]. 2018 May 5/1/2018; 548: 44-52. PMID: 29444450, PMCID: PMC5935105, PII: S0003-2697(18)30058-7, DOI: 10.1016/j.ab.2018.01.025, ISSN: 1096-0309.
Howes JE, Akan DT, Burns MC, Rossanese OW, Waterson AG, Fesik SW. Small Molecule-Mediated Activation of RAS Elicits Biphasic Modulation of Phospho-ERK Levels that Are Regulated through Negative Feedback on SOS1. Mol Cancer Ther [print-electronic]. 2018 May; 17(5): 1051-60. PMID: 29440291, PII: 1535-7163.MCT-17-0666, DOI: 10.1158/1535-7163.MCT-17-0666, ISSN: 1538-8514.
Padmanabhan C, Rellinger EJ, Zhu J, An H, Woodbury LG, Chung DH, Waterson AG, Lindsley CW, Means AL, Beauchamp RD. CFLIP critically modulates apoptotic resistance in epithelial-to-mesenchymal transition. Oncotarget. 2017 Nov 11/24/2017; 8(60): 101072-86. PMID: 29254146, PMCID: PMC5731856, PII: 19557, DOI: 10.18632/oncotarget.19557, ISSN: 1949-2553.
Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ. Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH). J Med Chem [print-electronic]. 2017 Nov 11/22/2017; 60(22): 9184-204. PMID: 29120638, PMCID: PMC5894102, DOI: 10.1021/acs.jmedchem.7b00941, ISSN: 1520-4804.
Rellinger EJ, Padmanabhan C, Qiao J, Craig BT, An H, Zhu J, Correa H, Waterson AG, Lindsley CW, Beauchamp RD, Chung DH. Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma. Oncotarget. 2017 Oct 10/31/2017; 8(53): 91040-51. PMID: 29207623, PMCID: PMC5710904, PII: 19406, DOI: 10.18632/oncotarget.19406, ISSN: 1949-2553.
Rellinger EJ, Padmanabhan C, Qiao J, Appert A, Waterson AG, Lindsley CW, Beauchamp RD, Chung DH. ML327 induces apoptosis and sensitizes Ewing sarcoma cells to TNF-related apoptosis-inducing ligand. Biochem Biophys Res Commun [print-electronic]. 2017 Sep 9/16/2017; 491(2): 463-8. PMID: 28716733, PMCID: PMC5564678, PII: S0006-291X(17)31392-X, DOI: 10.1016/j.bbrc.2017.07.050, ISSN: 1090-2104.
Patrone JD, Waterson AG, Fesik SW. Recent advancements in the discovery of protein-protein interaction inhibitors of replication protein A. Medchemcomm. 2017 Feb 2/1/2017; 8(2): 259-67. PMID: 30108742, PMCID: PMC6071986, PII: c6md00460a, DOI: 10.1039/c6md00460a, ISSN: 2040-2503.
Patrone JD, Pelz NF, Bates BS, Souza-Fagundes EM, Vangamudi B, Camper DV, Kuznetsov AG, Browning CF, Feldkamp MD, Frank AO, Gilston BA, Olejniczak ET, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW. Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A. ChemMedChem [print-electronic]. 2016 Apr 4/19/2016; 11(8): 893-9. PMID: 26748787, PMCID: PMC4838552, DOI: 10.1002/cmdc.201500479, ISSN: 1860-7187.
Brogan JT, Stoops SL, Brady S, An H, Weaver C, Daniels JS, Beauchamp RD, Lindsley CW, Waterson AG. Optimization of a small molecule probe that restores e-cadherin expression. Bioorg. Med. Chem. Lett [print-electronic]. 2015 Oct 10/1/2015; 25(19): 4260-4. PMID: 26299347, PMCID: PMC4567403, PII: S0960-894X(15)00823-9, DOI: 10.1016/j.bmcl.2015.07.104, ISSN: 1464-3405.
An H, Stoops SL, Deane NG, Zhu J, Zi J, Weaver C, Waterson AG, Zijlstra A, Lindsley CW, Beauchamp RD. Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition. Oncotarget. 2015 Sep 9/8/2015; 6(26): 22934-48. PMID: 26082441, PMCID: PMC4673210, PII: 4473, DOI: 10.18632/oncotarget.4473, ISSN: 1949-2553.
Waterson AG, Kennedy JP, Patrone JD, Pelz NF, Feldkamp MD, Frank AO, Vangamudi B, Souza-Fagundes EM, Rossanese OW, Chazin WJ, Fesik SW. Diphenylpyrazoles as replication protein a inhibitors. ACS Med Chem Lett. 2015 Feb 2/12/2015; 6(2): 140-5. PMID: 25699140, PMCID: PMC4329576, DOI: 10.1021/ml5003629, ISSN: 1948-5875.
Romaine IM, Taylor RW, Saidu SP, Kim K, Sulikowski GA, Zwiebel LJ, Waterson AG. Narrow SAR in odorant sensing Orco receptor agonists. Bioorg. Med. Chem. Lett [print-electronic]. 2014 Jun 6/15/2014; 24(12): 2613-6. PMID: 24813736, PMCID: PMC4111141, PII: S0960-894X(14)00438-7, DOI: 10.1016/j.bmcl.2014.04.081, ISSN: 1464-3405.
Frank AO, Vangamudi B, Feldkamp MD, Souza-Fagundes EM, Luzwick JW, Cortez D, Olejniczak ET, Waterson AG, Rossanese OW, Chazin WJ, Fesik SW. Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A. J. Med. Chem [print-electronic]. 2014 Mar 3/27/2014; 57(6): 2455-61. PMID: 24491171, PMCID: PMC3969094, DOI: 10.1021/jm401730y, ISSN: 1520-4804.
Burns MC, Sun Q, Daniels RN, Camper D, Kennedy JP, Phan J, Olejniczak ET, Lee T, Waterson AG, Rossanese OW, Fesik SW. Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2014 Mar 3/4/2014; 111(9): 3401-6. PMID: 24550516, PMCID: PMC3948241, PII: 1315798111, DOI: 10.1073/pnas.1315798111, ISSN: 1091-6490.
Frank AO, Feldkamp MD, Kennedy JP, Waterson AG, Pelz NF, Patrone JD, Vangamudi B, Camper DV, Rossanese OW, Chazin WJ, Fesik SW. Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragment-linking approach. J. Med. Chem [print-electronic]. 2013 Nov 11/27/2013; 56(22): 9242-50. PMID: 24147804, PMCID: PMC3932990, DOI: 10.1021/jm401333u, ISSN: 1520-4804.
Feldkamp MD, Frank AO, Kennedy JP, Patrone JD, Vangamudi B, Waterson AG, Fesik SW, Chazin WJ. Surface reengineering of RPA70N enables cocrystallization with an inhibitor of the replication protein A interaction motif of ATR interacting protein. Biochemistry [print-electronic]. 2013 Sep 9/17/2013; 52(37): 6515-24. PMID: 23962067, PMCID: PMC3804075, DOI: 10.1021/bi400542z, ISSN: 1520-4995.
Patrone JD, Kennedy JP, Frank AO, Feldkamp MD, Vangamudi B, Pelz NF, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW. Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A. ACS Med Chem Lett. 2013 Jul 7/11/2013; 4(7): 601-5. PMID: 23914285, PMCID: PMC3728914, DOI: 10.1021/ml400032y, ISSN: 1948-5875.
Taylor RW, Romaine IM, Liu C, Murthi P, Jones PL, Waterson AG, Sulikowski GA, Zwiebel LJ. Structure-activity relationship of a broad-spectrum insect odorant receptor agonist. ACS Chem. Biol [print-electronic]. 2012 Oct 10/19/2012; 7(10): 1647-52. PMID: 22924767, DOI: 10.1021/cb300331z, ISSN: 1554-8937.
Delpire E, Baranczak A, Waterson AG, Kim K, Kett N, Morrison RD, Daniels JS, Weaver CD, Lindsley CW. Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorg. Med. Chem. Lett [print-electronic]. 2012 Jul 7/15/2012; 22(14): 4532-5. PMID: 22727639, PMCID: PMC3389279, PII: S0960-894X(12)00738-X, DOI: 10.1016/j.bmcl.2012.05.126, ISSN: 1464-3405.
Sun Q, Burke JP, Phan J, Burns MC, Olejniczak ET, Waterson AG, Lee T, Rossanese OW, Fesik SW. Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation. Angew. Chem. Int. Ed. Engl [print-electronic]. 2012 Jun 6/18/2012; 51(25): 6140-3. PMID: 22566140, PMCID: PMC3620661, DOI: 10.1002/anie.201201358, ISSN: 1521-3773.
Vangamudi, B.; Ayres, A. E.; Burke, J. P.; Waterson, A. G.; Rossanese, O. W.; Fesik, S. W., editor.. Evaluation of TBK1 as a novel cancer target in the K-Ras pathway.
Jones PL, Pask GM, Romaine IM, Taylor RW, Reid PR, Waterson AG, Sulikowski GA, Zwiebel LJ. Allosteric antagonism of insect odorant receptor ion channels. PLoS ONE [print-electronic]. 2012; 7(1): e30304. PMID: 22272331, PMCID: PMC3260273, PII: PONE-D-11-19400, DOI: 10.1371/journal.pone.0030304, ISSN: 1932-6203.
Stellwagen JC, Adjabeng GM, Arnone MR, Dickerson SH, Han C, Hornberger KR, King AJ, Mook RA, Petrov KG, Rheault TR, Rominger CM, Rossanese OW, Smitheman KN, Waterson AG, Uehling DE. Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup. Bioorg. Med. Chem. Lett [print-electronic]. 2011 Aug 8/1/2011; 21(15): 4436-40. PMID: 21733693, PII: S0960-894X(11)00804-3, DOI: 10.1016/j.bmcl.2011.06.021, ISSN: 1464-3405.
Stoops SL, Pearson AS, Weaver C, Waterson AG, Days E, Farmer C, Brady S, Weaver CD, Beauchamp RD, Lindsley CW. Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells. ACS Chem. Biol [print-electronic]. 2011 May 5/20/2011; 6(5): 452-65. PMID: 21241068, PMCID: PMC3401128, DOI: 10.1021/cb100305h, ISSN: 1554-8937.
Thorne CA, Hanson AJ, Schneider J, Tahinci E, Orton D, Cselenyi CS, Jernigan KK, Meyers KC, Hang BI, Waterson AG, Kim K, Melancon B, Ghidu VP, Sulikowski GA, LaFleur B, Salic A, Lee LA, Miller DM, Lee E. Small-molecule inhibition of Wnt signaling through activation of casein kinase 1a. Nat. Chem. Biol [print-electronic]. 2010 Nov; 6(11): 829-36. PMID: 20890287, PMCID: PMC3681608, PII: nchembio.453, DOI: 10.1038/nchembio.453, ISSN: 1552-4469.
Bhagwanth S, Waterson AG, Adjabeng GM, Hornberger KR. Room-temperature Pd-catalyzed amidation of aryl bromides using tert-butyl carbamate. J. Org. Chem. 2009 Jun 6/19/2009; 74(12): 4634-7. PMID: 19518153, DOI: 10.1021/jo9004537, ISSN: 1520-6904.
Waterson AG, Petrov KG, Hornberger KR, Hubbard RD, Sammond DM, Smith SC, Dickson HD, Caferro TR, Hinkle KW, Stevens KL, Dickerson SH, Rusnak DW, Spehar GM, Wood ER, Griffin RJ, Uehling DE. Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors. Bioorg. Med. Chem. Lett [print-electronic]. 2009 Mar 3/1/2009; 19(5): 1332-6. PMID: 19208477, PII: S0960-894X(09)00081-X, DOI: 10.1016/j.bmcl.2009.01.080, ISSN: 1464-3405.
Laquere, S.; Arnone, M.; Moss, K.; Yang, J.; Fisher, K.; Kane-Carson, L.; Smitheman, K.; Ward, J.; Heidrich, B.; Rheault, T.; Adjebeng, G.; Hornberger, K.; Stellwagen, J.; Waterson, A.; Han, C.; Mook, Jr. R. A.; Uehling, D.; King, A. J., editor.. A selective Raf kinase inhibitor induces cell death and tumor regression of human cancer cell lines encoding R-Raf V600E mutation.
Waterson, A. G. Delpire, E.; Days, E.; Lewis, M.; Kim, K.; Lindsley, C. W.; Weaver, C. D., editor.. Small molecule inhibitors of the KCC2 neuronal co-transporter.
Stevens KL, Alligood KJ, Alberti JG, Caferro TR, Chamberlain SD, Dickerson SH, Dickson HD, Emerson HK, Griffin RJ, Hubbard RD, Keith BR, Mullin RJ, Petrov KG, Gerding RM, Reno MJ, Rheault TR, Rusnak DW, Sammond DM, Smith SC, Uehling DE, Waterson AG, Wood ER. Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. Bioorg. Med. Chem. Lett [print-electronic]. 2009 Jan 1/1/2009; 19(1): 21-6. PMID: 19028424, PII: S0960-894X(08)01392-9, DOI: 10.1016/j.bmcl.2008.11.023, ISSN: 1464-3405.
Schaaf, G. M.; Mukherjee, S.; Waterson, A. G.. Conjugate addition of sodium methanesulfinate to vinyl pyridines and diazines for the synthesis of aliphatic sulfones. Tetrahedron Lett. 2009; 50: 1928-33.
Hubbard RD, Dickerson SH, Emerson HK, Griffin RJ, Reno MJ, Hornberger KR, Rusnak DW, Wood ER, Uehling DE, Waterson AG. Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Nov 11/1/2008; 18(21): 5738-40. PMID: 18842405, PII: S0960-894X(08)01162-1, DOI: 10.1016/j.bmcl.2008.09.090, ISSN: 1464-3405.
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