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Fesik Lab

Alex Waterson, Ph.D.

Research Professor of Pharmacology and Chemistry

Medicinal Chemistry

Alex G. Waterson, Ph.D. is currently a Research Professor of Pharmacology and Chemistry at Vanderbilt University in Nashville, Tennessee, USA. Trained as a synthetic organic chemist, he completed his Ph.D. studies with Professor Al Padwa at Emory University, and conducted postdoctoral research at Colorado State University in the group of the late Professor Albert I. Meyers. Alex joined a medicinal chemistry team at GlaxoSmithKline in the Research Triangle Park area of North Carolina in 2001, contributing to the discovery of covalently modifying ErbB inhibitors and the B-RAF drug Dabrafenib, among other projects.

Upon transitioning to Vanderbilt in 2008, he helped establish Vanderbilt’s entry into the National Cancer Institute’s Chemical Biology Consortium – the Vanderbilt Center for Cancer Drug Discovery, which he now directs – and joined Professor Fesik’s fragment-based discovery team. He also serves as Associate Director of Medicinal Chemistry for the Vanderbilt Institute of Chemical Biology. He has led and participated in primarily oncology drug discovery projects, including those aimed at direct and indirect inhibition of K-RAS, as well protease, epigenetic, and cancer metabolism targets. Many of his recent efforts have been resourced by the Chemical Biology Consortium, including projects aimed at the discovery of inhibitors of Taspase-1 and LDHA, as well as multiple projects in the Targeted Protein Degradation space.

Faculty Profile

Publications and Patents:

  1. Cox, J.; Boily, M.-O.; Caron, A.; Sheng, T.; Wu, J.; Ding, J.; Gaudreault, S.; Chong, O.; Surendradoss, J.; Gomez, R.; Lester, J.; Dumais, V.; Li. X.; Gumpena, R.; Hall, M.; Waterson, A. G.; Stott, G.; Flint, A.; Moore, W.; Lowther, W.; Knight, J.; Percival, M. D.; Tong, V.; Oballa, R.; Powell, D.; King, A. “Discovery of CHK-336: A First-in-Class, Liver-Targeted, Small Molecule Lactate Dehydrogenase Inhibitor for Hyperoxaluria Treatment” Nat. Chem. Biol. (submitted).

 

  1. Scott, T.; Smethurst, C. A. P.; Westermaier, Y.; Mayer, M.; Greb, P.; Kousek, R.; Biberger, T.; Bader, G.; Jandova, Z.; Schmalhorst, P. S.; Fuchs, J.E.; Magarkar, A.; Hoenke, C.; Gerstberger, T.; Combs, S. A.; Pape, R.; Phul, S.; Kothiwale, S.; Bergner, A.; Waterson, A. G.; Players, Foldit; Weinstabl, H.; McConnell, D. B.; Bottcher, J.; Meiler, J.; Moretti, R. “Drugit: crowd-sourcing molecular design of non-peptidic VHL binders” under revision at Nature Comm. Preprint available: ChemRxiv (2023): DOI: 10.26434/chemrxiv-2023-lczzd.

 

  1. Siricilla, S.; Hansen, C. J.; Rogers, J. H.; De, D.; Simpson, C. L.; Waterson, A. G.; Sulikowski, G. A.; Crockett, S. L.; Boatwright, N.; Reese, J.; Paria, B. C.; Newton, J.; Herington, J. L. “Arrest of mouse preterm labor until term delivery by combination therapy with atosiban and mundulone, a natural product with tocolytic efficacy.” Pharmacological Res. 2023, 195, 106876. DOI: 10.1016/j.phrs.2023.106876.

 

  1. Zarrow, J. E.; Alli-Oluwafuyi, A.-M.; Youwakim, C. M.; Kim, K.; Jenkins, A. N.; Suero, I. C.; Jones, M. R.; Mashhadi, Z.; Mackie, K. P.; Waterson, A. G.; Doran, A. C.; Sulikowski, G. A.; Davies, S. S. “Small Molecule Activation of NAPE-PLD Enhances Efferocytosis by Macrophages ACS Chem. Biol. 2023, 18(8), 1891-1904. DOI: https://doi.org/10.1021/acschembio.3c00401.

 

  1. Bröker, J.; Waterson, A.; Smethurst, C.; Kessler, D.; Boettcher, J.; Mayer, M.; Gmaschitz, G.; Phan, J.; Sun, Q.; Little, A.; Abbot, J.; Gmachl, M.; Rudolph, D.; Arnhof, H.; Rumpel, K.; Savarese, F.; Gerstberger, T.; Mischerikow, N.; Treu, M.; Herdeis, L.; Wunberg, T.; Gollner, A.; Mantoulidis, A.; Krämer, O.; McConnell, D.; 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. 2022, 65(21), 14614-14629. PMID: 31332011. PMCID: PMC6689897.

 

  1. Fricke, N.; Raghunathan, K.; Tiwari, A.; Stefanski, K.M.; Balakrishnan, M.; Waterson, A. G.; Capone, R.; Huang, H.; Sanders, C.R.; Bauer, J.A.; Kenworthy, Anne K. “High-Content Imaging Platform to Discover Chemical Modulators of Plasma Membrane Rafts” ACSChem.Sci. 2022, 8(3), 370-378. PMID: 35355811. PMCID: PMC8961798.

 

  1. Drury, S.L.; Miller, A.R.; Laut, C.; Walter, A.B.; Bennett, M.R.; Su, M.; Bai, M.; Jing, B.; Joseph, S.B.; Metzger, E.J.; Bane, C.E.; Black, C.; Macdonald, M.T.; Dutter, B.F.; Romaine, I.R.; Waterson, A. G.; Sulikowski, G. A.; Jansen, E.D.; Crowe Jr. J.E.; Sciotti, R.J. Skaar, E.P. “Simultaneous exposure to intracellular and extracellular photosensitizers for the treatment of Staphylococcus aureus infections” Antimicrob. Agents Chemother, 2021, 65(12), e00919-21. PMID: 34516248. PMCID: PMC8597735.

 

  1. Kozlyuk, N.; Gilston, B.A.; Salay, L.E.; Gogliotti, R.D.; Christov, P.P.; Kim, K.; Ovee, M.; Waterson, A.G.; Chazin, W.J. “A fragment-based approach to discovery of Receptor for Advanced Glycation End products inhibitors.” Proteins 2021, 89(11), 1399-1412. PMID:34156100. PMCID: PMC8492516.

 

  1. Kim, K.; Christov, P.P.; Romain, I.; Tian, J.; Jana, S.; Lamers, A.P.; Dutter, B.F.; Scaggs, T.; Jeon, K.; Guttentag, B.; Weaver, C.D.; Lindsley, C.W.; Waterson, A.G.; Sulikowsik, G.A. “Ten-Year Retrospective of the Vanderbilt Institute of Chemical Biology Chemical Synthesis Core” ACS Chem. Biol. 2021, 16, 787-793. PMID: 33877812.

 

  1. Christov, P.P.; Kim, K.; Jana, S.; Romaine, I. R.; Rai, G.; Mott, B. T. Allweil, A. A.; Lamers, A.P.; Brimacombe, K.R.; Urban,D. J.; Lee, T. D.; Hu, X.; Lukacs, C.M.; Davies, D. R.; Jadhav, A.; Hall, M. A.; Green, N.; Moore, W. J.; Stott, G.M.; Flint, A.J.; Maloney, D.J.; Sulikowski, G.A.; Waterson, A.G. “Optimization of ether and aniline based inhibitors of lactate dehydrogenase” Bioorg. Med. Chem. Lett. 2021, 41, 127974. PMID: 33771585. PMCID: PMC8113097.

 

  1. Rai, G.; Urban, D.; Mott, B.; Hu, X.; Yang, S.-M.; Benavides, G.; Johnson, M.; Squadrito, G.; Brimacombe, K.; Lee, T.; Cheff, D.; Zhu, H.; Henderson, M. J.; Pohida, Ka.; Sulikowski, G.; Dranow, D.; Kabir, M.; Shah, P.; Padilha, E. ; Tao, D.; Fang, Y.; Christov, P.; Kim, K.; Jana, S.; Muttil, P.; Anderson, T.; Kunda, N.; Hathaway, H.; Kusewitt, D.; Oshima, N.; Cherukuri, M.; Davies, D.; Norenberg, J.; Sklar, L.; Moore, Wi.; Dang, C.; Stott, G.; Neckers, L.; Flint, A.; Usmar, V. D.; Simeonov, A.; Waterson, A. G.; Jadhav, A.; Hall, M.; Maloney, D. “Pyrazole-Based Lactate Dehydrogenase (LDH) Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties” J. Med. Chem. 2020, 63(19), 10984-11011. PMID: 32902275. PMCID: PMC7830743.

 

  1. Sarkar, D.; Olejniczak, E. T.; Phan, J.; Coker, J. A.; Sai, J.; Arnold, A.; Beesetty, Y.; Waterson, A. G.; Fesik, S. W. “Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods” J. Med. Chem. 2020, 63(15): 8325-8337. PMID: 32673492.

 

  1. Simon, S. C.; Wang, F.; Thomas, L. R.; Phan, J.; Zhao, B. Olejniczak, E. T.; Macdonald, J. D.; Shaw, J. G.; Schlund, C.; Payne, W. G.; Creighton, J.; Stauffer, S. R.; Waterson, A. G.; Tansey, W. P.; Fesik, S. W. “Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC inhibitors using fragment-based methods and structure-based design: J. Med. Chem. 2020, 63: 4315-4333. PMID: 32223236. PMCID: PMC7187413.

 

  1. Kessler, D.; Gmachl, M.; Mantoulidis, A.; Martin, L.; Zoephel, A.; Mayer, M.; Golner, A.; Covini, D.; Fischer, S.; Gerstberger, T.; Gmaschitz, T.; Goodwin, C.; Greb, P.; Haering, D.; Hela, W.; Hofmann, J.; Karolyi-Oezguer, J.; Knesl, P; Kornigg, S.; Koegel, M.; Kousek, R.; Lamarre, L.; Moser, F.; Munico-Martinez, S.; Peinsipp, C.; Phan, J.; Rinnenthal, J.; Sai, J.; Salamon, C.; Scherbantin, Y.; Schipany, K.; Schnitzer, R.; Schrenk, A.; Sharps, B.; Siszler, G.; Sun, Q.; Waterson, A.; Wolkerstorfer, B.; Zeeb, M.; Pearson, M.; Fesik, S.; McConnell, D. “Reply to Tran et al.: Dimeric KRAS protein-protein interaction stabilizers.” Proc. Natl. Acad. Sci. 2020, 117(7):3365-3367. PMID: 32047042. PMCID: PMC7035485.

 

  1. Oshima, N; Ishida, R. Kishimoto, S.; beebe, K.; Brender, J. R.; Yamamoto, K.; Urban, D.; Rai, G.; Johnson, M.S.; Benavides, G.; Squadrito, G. L; Crooks, D.; Jackson, J.; Joshi, A.; Mott, B. T.; Shrimp, J. H.; Moses, M. A.; Lee, M. -J.; Yuno, A.; Lee, T. D.; Hu, Z.; Anderson, T. Kusewitt, D.; Hathaway, H. H.; Jadhav, A.; Picard, D.; Trepel, J. B.; Mitchell, J. B.; Stott, G. M.; Moore, W. J.; Simeonov, A.; Skalar, L. A.; Norenberg, J. P,; Linehan, W. M.; Maloney, D. J.; Dang, C. V.; Waterson, A. G.; Hall, M.; Darley-Usmar, V. M.; Krishna, M. C.; Neckers, L. M. “Dynamic Imaging of LDH inhibition in tumors reveals rapid in vivo metabolic rewiring and vulnerability to combination therapy.” Cell Reports 2020, 30:1798-1810. PMID: 32049011. PMCID: PMC7039685.

 

  1. Macdonald, J. D.; Chacón, S. S.; Han, C.; Wang, F. Shaw, J. G.; Howes, J. E.; Sai. J.; Yuh, J. P.; Camper. D. V.; Alicie, B. M.; Alvarado, J. R.; Nikhar, S.; Payne, W. G.; Aho, E. R.; Bauer, J. A.; Zhao, B.; Phan, J.; Thomas, L. R.; Rossanese, O. W.; Tansey, W. P.; Waterson, A. G.; Stauffer, S. R.; Fesik, S. W. “Discovery and optimization of salicylic acid-derived sulfonamide inhibitors of the WDR5:MYC protein–protein interaction” J. Med. Chem. 2019, 62(24): 11232-11259. PMID: 26748787. PMCID: PMC6933084.

 

  1. Kessler, D.; Gmachl, M.; Mantoulidis, A.; Martin, L.; Zoephel, A.; Mayer, M.; Golner, A.; Covini, D.; Fischer, S.; Gerstberger, T.; Gmaschitz, T.; Goodwin, C.; Greb, P.; Haering, D.; Hela, W.; Hofmann, J.; Karolyi-Oezguer, J.; Knesl, P; Kornigg, S.; Koegel, M.; Kousek, R.; Lamarre, L.; Moser, F.; Munico-Martinez, S.; Peinsipp, C.; Phan, J.; Rinnenthal, J.; Sai, J.; Salamon, C.; Scherbantin, Y.; Schipany, K.; Schnitzer, R.; Schrenk, A.; Sharps, B.; Siszler, G.; Sun, Q.; Waterson, A.; Wolkerstorfer, B.; Zeeb, M.; Pearson, M.; Fesik, S.; McConnell, D. “Drugging an ‘undruggable’ pocket on KRAS” Proc. Natl. Acad. Sci. 2019, 116:15823-15829. PMID: 31332011. PMCID: PMC6689897.

 

  1. Akan, D.; Howes, J. E.; Sai, J.; Arnold, A.; Beesetty, Y.; Phan, J.; Olejniczak, E. T.; Waterson, A. G.; Fesik, S. W. “Small molecule SOS1 agonists modulate MAPK and PI3K signaling via independent mechanisms” ACS Chem. Biol. 2019; 14:325-331. PMID: 30735352.

 

  1. Dumas, M.; Chen, G.-Y.; Kendrick, N.; Xu, G.; Larsen, S.; Jana, S.; Waterson, A. G.; Bauer, J.; Hancock, W.; Sulikowski, G. A.; Ohi, R. “Dual inhibition of Kif15 by oxindole and quinazolidindione chemical probes” BioOrg. Med. Chem. 2019; 29(2): 148-154. PMID: 30528696. PMCID: PMC6681659

 

  1. Waterson, A. G., Scott, S. A.; Kett, N. R.; Blobaum, A. L.; Brown, H. A.; Lindsley, C. W. “Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives” BioOrg. Med. Chem. Lett. 2018; 28 (23): 3670-3673. PMID: 30528979.

 

  1. Hodges, T., R.; Abbott, J. R.; Little, A.; Sarkar, D.; Salovich, J. M.; Howes, J. E.; Akan, D.; Sai, J.; Arnold, A.; Browning, C. F.; Burns, M. C.l; Sobolik, T.; Sun, Q.; Beesetty, Y.; Coker, J., A.; Scharn, D.; Stadtmueller, H.; Rossanese, O. W.; Phan, J.; Waterson, A. G.; McConnell, D.; Fesik, S. W. “Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS” J. Med. Chem 2018; 61(19): 8875-8894. PMID: 30528979. PMCID: PMC8314423.

 

  1. Abbott, J. R.; Patel, P. A.; Howes, J. E.; Akan, D. T.; Kennedy, J. P.; Burns, M. C.; Browning, C. F.; Sun, Q.; Rossanese, O. W.; Phan, J.; Waterson, A. G.; Fesik, S. W. “Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS” ACS Med. Chem. Lett. 2018; 9(9): 941-946. PMID: 30258545. PMCID: PMC6142059.

 

  1. Abbott, J. R.; Hodges, T. R.; Daniels, R. N.; Patel, P. A.; Kennedy, J. P.; Howes, J. E.; Akan, D. T.; Burns, M. C.; Sai, J.; Sobolik, T.; Beesetty, Y.; Lee, T.; Rossanese, O. W.; Phan, J.; Waterson, A. G.; Fesik, S. W. “Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling” J. Med. Chem. 2018; 61(14):6002-6017. PMID: 29856609.

 

  1. Burns, M. C.; Howes, J. E.; Sun, Q.; Little, A. J.; Camper, D.V.; Abbott, J. R.; Phan, J.; Waterson, A. G.; Lee, T.; Rossanese, O. W.; Fesik, S. W “High-throughput screening identifies small molecules that bind to the Ras:SOS:Ras complex and perturb Ras signaling” Anal. Biochem. 2018; 548:44-52. PMID: 29444450. PMCID: PMC5935105.

 

  1. Howes, J. E.; Akan, D. T.; Burns, M. C.; Rossanese, O. W.; Waterson, A. G.; Fesik, S. W. “Small molecule-mediated activation of Ras elicits biphasic modulation of phospho ERK levels that are regulated through negative feedback on SOS1” Mol. Canc. Ther. 2018; 17(5): 1051-1060. PMID: 29440291.

 

  1. Padmanabha, C.; Rellinger, E. J.; Zhu, J; An. H.; Woodbury. L. G.; Chung, D. H.; Waterson, A. G.; Lindsley. C. W.; Means, A. L.; Beauchamp, R. D. “cFLIP critically modulates apoptotic resistance in epithelial-to-mesenchymal transition” Oncotarget 2017; 8:101072-101086. PMID: 29254146. PMCID: PMC5731856.

 

  1. Rai, G.; Brimacombe, K. R.; Mott, B. R.; Urban, D. J.; Hu, X; Yang, S, -M.; Lee, T. D.; Cheff, D. M.; Pohida, K.; Benavides, G. A.; Darley-Usmar, V. M.; Moore, W. J.;Stott, G.; Flint, A.; Hall, M. D.; Neckers, L.; Van Dang, C.; Waterson, A. G.; Simeonov, A.; Jadhav, A.; Maloney, D. J. “Discovery and Optimization of potent, cell-active pyrazole-based inhibitors of Lactate Dehydrogenase (LDH)” J. Med. Chem. 2017; 60(22): 9184-9204. PMID: 29120638. PMCID: PMC5731856.

 

  1. Rellinger, E. J.; Padmanabhan, C.; Qiao, J.; Craig, B. T.; An, H.; Zhu, J.; Waterson, A. G.; Lindsley, C. W.; Beauchamp, R. D.; Chung, D. H.; Beauchamp, R. D.  “Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma” Oncotarget 2017; 8(53): 91040-91051. PMID: 29207623. PMCID: PMC5710904.

 

  1. Rellinger, E. J.; Padmanabhan, C.; Qiao, J.; Appert, A.; Waterson, A. G.; Lindsley, C. W.; Beauchamp, R. D.; Chung, D. H. “ML327 induces apoptosis and sensitizes Ewing sarcoma cells to TNF-related apoptosis-inducing ligand” Biochem. Biophys. Res. Commun. 2017; 491(2): 463-468. PMID: 28716733. PMCID: PMC5564678.

 

  1. Patrone, J.D.; Waterson, A.G.; Fesik, S.W. “Recent advancements in the discovery of protein-protein interaction inhibitors of Replication Protein A” MedChemComm 2017; 8(2): 259-267. PMID: 30108742. PMCID: PMC6071986.

 

  1. Patrone, J.D.; Pelz, N.F.; Bates, B.S.; Souza-Fagundes, E.M.; Vangamudi, B.; Camper, D.V.; Kuznetsov, A.G.; Browning, C.F.; Feldkamp, M.D.; Gilston, B.A.; Olejniczak, E.T.; Rossasese, O.W.; Waterson, A.G., Chazin, W.J.; Fesik, S.W. “Identification and optimization of anthranilic acid-based inhibitors of Replication Protein A” ChemMedChem 2016; 11(8): 893-899. PMID: 26748787 PMCID: PMC4838552.

 

  1. Brogan, J.T.; Stoops, S.L.; Brady, S.; An, H.; Weaver, C.; Daniels, S.J.; Beauchamp, R.D.; Lindsley, C.W.; Waterson, A.G. “Optimization of a small molecule probe that restores e-cadherin expression” Bioorg. Med. Chem. Lett. 2015; 25(19): 4260-4264. PMID: 26299347. PMCID: PMC4567403.

 

  1. An, H.; Deane, N. G.; Stoops, S. L.; Zi, J.; Weaver, C.; Waterson, A. G.; Zijlstra, A.; Lindsley, C. W.; Beauchamp, R. D. “Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition” Oncotarget 2015; 6(26): 22934-22948. PMID: 26082441. PMCID: PMC4673210.

 

  1. Waterson, A. G.; Kennedy, J. P.; Patrone, J. D.; Pelz, N. F.; Feldkamp, M. D.; Frank, A. O.; Vangamudi, B.; Souza-Fagundes, E/ M.; Rossanese, O. W.; Chazin, W. J.; Fesik, S. W. “Diphenylpyrazoles as Replication Protein A inhibitors” ACS Med. Chem. Lett. 2015; 6(2): 140-145. PMID: 25699140. PMCID: PMC4329576.

 

  1. Romaine, I. M.; Taylor, R. W.; Saidu, S. P.; Kim, K.; Sulikowski, G. A.; Zwiebel, L. J.; Waterson, A. G. “Narrow SAR in odorant sensing Orco receptor antagonists” Bioorg. Med. Chem. Lett. 2014; 24(12): 2613-2616. PMID: 24813736. PMCID: PMC4111141.

 

  1. Burns, M. C.; Sun, Q.; Daniels, R. N.; Camper, D. V.; Kennedy, J. P.; Phan, J.; Olejniczak, E. O.; Lee, T.; Waterson, A. G.; Rossanese, O. W.; Fesik, S. W. “Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange” Proc. Natl. Acad. Sci. 2014; 11(9): 3401-3406. PMID:24550516. PMCID: PMC3948241.

 

  1. Frank, A. O.; Vangamudi, B.; Feldkamp, M. D.; Souza-Fagundes, E.; Luzwick, J.; Cortez, D.; Olejniczak, E. T.; Waterson, A. G.; Rossanese, O. W.; Chazin, W. J.; Fesik, S. W. “Discovery of a potent stapled helix peptide that binds to the 70N domain of Replication Protein A” J. Med. Chem. 2014; 57(6): 2455-2461. PMID: 24491171. PMCID: PMC3969094.

 

  1. Frank, A. O.; Feldkamp, M. D.; Kennedy, J. P.; Waterson, A. G.; Pelz, N. F.; Patrone, J. D.; Vangamudi, B.; Camper, D. V.; Rossanese, O. W.; Chazin, Walter J., Fesik, S. W. “Discovery of a Potent Inhibitor of Replication Protein A Protein-Protein Interactions Using a Fragment-Linking Approach” J. Med. Chem. 2013; 56(22): 9242-9250. PMID: 24147804. PMCID: PMC3932990.

 

  1. Feldkamp, M. D.; Frank, A. O., Kennedy, J. P.; Patron, J. D.; Vangamudi, B.; Waterson, A. G., Fesik, S. W.; Chazin, W. J. “Surface reengineering of RPA70N enables co-crystallization with an inhibitor of the RPA interaction motif of ATRIP” Biochemistry 2013; 52(37): 6515-6524. PMID: 23962067. PMCID: PMC3804075.

 

  1. Patrone, J. D.; Kennedy, J.P .; Frank, A. O.; Feldkamp, M. D., Vangamudi, B.; Pelz, N. F.; Rossanese, O. W.; Waterson, A. G.; Chazin, W. J.; Fesik, S. W. “Discovery of protein-protein interaction inhibitors of Replication Protein A” ACS Med. Chem. Lett. 2013; 4(7): 601-605. PMID: 23914285. PMCID: PMC3728914.

 

  1. Rheault, T. R.; Stellwagen, J. C.; Adjabeng, G. M.; Hornberger, K. R.; Petrov, K. G.; Waterson, A. G.; Dickerson, S. H.; Mook, R. A.; Laquerre, S. G.; King, A. J.; Rossanese, O. W.; Arnone, M. R.; Smitheman, K. N.; Kane-Carson, L. S.; Han, C.; Moorthy, G. S.; Moss, K. G.; Uehling, D. E. “The discovery of dabrafenib: a selective inhibitor of Raf kinases with anti-tumor activity against B-Raf driven tumors” ACS Med. Chem. Lett. 2013; 4(3): 358-362. PMID: 24900673. PMCID: PMC4027516.

 

  1. Taylor, R. C.; Romaine, I. M.; Liu, C.; Murthi, P.; Jones, P. L.; Waterson, A. G.; Sulikowski, G. A.; Zwiebel, L. J. “Structure activity relationship of a broad-spectrum insect odorant receptor antagonist” ACS Chem. Biol. 2012; 7(10): 1647-1652. PMID: 22924767.

 

  1. Delpire, E.; Baranczak, A.; Waterson, A. G. ;Kim, K.; Kett, N.; Morrison, R. D.; Daniels, J. S.; Weaver, C. D.; Lindsley, C. W. “Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: Development of a highly selective and more potent in vitro probe.” Biorg. Med. Chem. Lett. 2012; 22(14): 4532-4353. PMID: 22727639. PMCID: PMC3389279.

 

  1. Sun, Q.; Burke, J. P.; Phan, J.; Burns, M. C.; Olejniczak, E. T.; Waterson, A. G.; Lee, T.; Rossanese, O. W.; Fesik, S. W. “Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation” Angew. Chemie, Int. Ed. 2012; 51(25): 6140-6143. PMID: 22566140. PMCID: PMC3620661.

 

  1. Jones, P. L.; Pask, G. M.; Romaine, I. M.; Taylor, R. C.; Reid, P. R.; Waterson, A. G.; Sulikowski, G. A.; Zwiebel, L. J. “Allosteric antagonism of insect odorant receptor ion channels” PLoS One 2012; 7(1): e30304. PMID: 22272331. PMCID: PMC3260273.

 

  1. Stellwagen, J. C.; Adjabeng, G. M.; Arnone, M. R.; Dickerson, S. H.; Han, C.; Hornberger, K. R.; King, A. J.; Mook, Jr., R. A.; Petrov, K. G.; Rheault, T. R.; Rominger, C. M.; Rossanese, O. W.; Smitheman, K. N.; Waterson, A. G.; Uehling, D. E. “Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup” Bioorg. Med. Chem. Lett. 2011; 21(15): 4436-4440. PMID: 22272331.

 

  1. Stoops, S. L.; Pearson, A. S.; Weaver, C.; Waterson, A. G.; Days, E.; Farmer, C.; Brady, S.; Weaver, C. D.; Beauchamp, R. D.; Lindsley, C. W. “Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells” ACS Chem. Biol. 2011; 6(5): 452-465. PMID: 21241068. PMCID: PMC3401128.

 

  1. Thorne, C. A.; Schneider, J.; Tahinci, E.; Orton, D.; Cselenyi, C. S.; Jernigan, K. K.; Hanson, A., J.; Meyers, K. C.; Hang, B. I.; Waterson; A. G.; LaFleur, B.; Salic, A.; Lee, L. A.; Miller, III, D. M.; Lee, E. “Small molecule inhibition of Wnt signaling through activation of Casein Kinase 1 alpha” Nature Chemical Biology 2010; 6(11): 829-836. PMID: 20890287. PMCID: PMC3681608.

 

  1. Bhagwanth, S.; Waterson, A. G.; Adjabeng, G. M.; Hornberger, K. R. “Room-temperature Pd-catalyzed amidation of aryl bromides using tert-butyl carbamate” J. Org. Chem. 2009; 74(12): 4634-4637. PMID: 19518153.

 

  1. 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(17): 1928-1933.

 

  1. Waterson, A. G.; Petrov, L. P.; Hornberger, K. R.; Hubbard, R. D.; Sammond, D. M.; Smith, S. C.; Hinkle, K. W.; Uehling, D. E.; Dickerson, S. H.; Rusnak, D. W.; Spehar, G. M.; Wood, E. R.; Griffin, R. J.; Kitrinos, N. P. “Synthesis and evaluation of novel aniline headgroups for thienopyrimidine-based covalent dual EGFR/ErbB2 kinase inhibitors” Biorg. Med. Chem. Lett. 2009; 19(5); 1332-1336. PMID: 19208477.

 

  1. Stevens, K. L; Alligood, K. J.; Alberti, J. G. B.; Caferro, T. R.; Chamberlain, S. D.; Dickerson, S. H.; Disckson, H. D.; Emerson, H. K.; Griffin, R. J.; Hubbard, R. D.; Keith, B. R.; Mullin, R. J.; Petrov, K. G.; Gerding, R. M.; Reno, M. J.; Rheault, T. R.; Rusnak, D. W.; Sammond, D. M.; Smith, S. C.; Uehling, D. E.; Waterson, A. G.; Wood, E. R. “Synthesis and stereochemical effects of pyrrolidyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors” Biorg. Med. Chem. Lett. 2009; 19(1): 21-26. PMID: 19028424.

 

  1. Hubbard, R. D.; Dickerson, S. D.; Emerson, H. K.; Griffin, R. J.; Reno, M. J.; Hornberger, K. R.; Rusnak, D. W.; Wood, E. R.; Uehling, D. E.; Waterson, A. G. “Dual EGFR/ ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines” Biorg. Med. Chem. Lett. 2008; 18(21): 5738-5740. PMID: 18842405.

 

  1. Wood, E. R.; Shewchuck, L. M.; Ellis, B.; Brignola, P.; Brashear, R. L.; Caferro, T. R.; Dickerson, S. H.; Donaldson, K. H.; Gaul, M.; Griffen, R. J.; Hassell, A. M.; Keith, B.; Mullin, R.; Petrov, K., G.; Rusnak, D. W.; Tadepalli, S. M.; Ulrich, J. C.; Wagner, C. D.; Vanderwall, D. E.; Waterson, A. G.; White, W. L.; Uehling, D. E. “6-Ethynylthieno[3,2-d]- and 6-Ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB family receptor tyrosine kinases” Proc. Natl. Acad. Sci. 2008; 105(8): 2773-2778. PMID: 18287036. PMCID: PMC2268535.

 

  1. Waterson, A. G.; Stevens, K. L.; Reno, M. J.; Zhang. Y. –M.; Boros, E. E.; Bouvier, F.; Rastagar, A.; Uehling, D. U.; Dickerson, S. H.; Reep, B.; McDonald, O. B.; Wood, E. R.; Rusnak, D. W.; Alligood, K.; Rudolph, S. “Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors” Biorg. Med. Chem. Lett. 2006; 16(9): 2419-2422. PMID: 16483772.

 

  1. Padwa, A.; Waterson, A. G. “A novel synthesis of polysubstituted phenols using the SnAr reaction of 2,5-dinitrofuran.” ARKIVOC 2001; 4: 29-42.

 

  1. Waterson, A. G.; Meyers, A. I. “Studies directed toward the synthesis of Viridenomycin. Route 2: a second-generation approach.” Tetrahedron Lett. 2001; 42(26): 4305-4308.

 

  1. 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(52): 10159-10173.

 

  1. Waterson, A. G.; Meyers, A. I. “Bicyclic lactams as chiral homoenolate equivalents: Synthesis of (-)-Penienone.” J. Org. Chem. 2000; 65(21): 7240-7243.

 

  1. Padwa, A.; Waterson, A. G. “Synthesis of nitrogen heterocycles using the intramolecular Pummerer reaction.” Curr. Org. Chem. 2000; 4(2): 175-203.

 

  1. Padwa, A.; Waterson, A. G. “Studies dealing with thionium ion promoted Mannich cyclization reactions.” J. Org. Chem. 2000; 65(1): 235-244.

 

  1. Padwa, A.; Waterson, A.G. “Synthesis of the perhydroindolizine nucleus by a Pummerer/Mannich induced cyclization cascade.” Tetrahedron Lett. 1998; 39(47): 8585-8588.

 

  1. 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(12): 3986-3997.

 

  1. Padwa, A.; Dimitroff, M.; Waterson, A. G.; Wu, T. “Diels-Alder reaction of 2-amino-substituted furans as a method for preparing substituted anilines.” Org. Chem. 1997; 62(11): 4088-4096.