Keyword Connections

•  Alex Waterson
•  Charles Hong
•  Corey Hopkins
•  Craig Lindsley

•  C. Weaver
•  Jerod Denton
•  Kyle Emmitte
•  Michelle Armstrong

•  Stephen Fesik
•  Wenbiao Chen

Resources

• No matching connections

Communities

• Hong Lab

Publications

• Cancer-drug discovery and cardiovascular surveillance.
  Groarke JD, Cheng S, Moslehi J
  (2013) N Engl J Med 369: 1779-81
• Genetics of rheumatoid arthritis contributes to biology and drug discovery.
  Okada Y, Wu D, Trynka G, Raj T, Terao C, Ikari K, Kochi Y, Ohmura K, Suzuki A, Yoshida S, Graham RR, Manoharan A, Ortmann W, Bhangale T, Denny JC, Carroll RJ, Eyler AE, Greenberg JD, Kremer JM, Pappas DA, Jiang L, Yin J, Ye L, Su DF, Yang J, Xie G, Keystone E, Westra HJ, Esko T, Metspalu A, Zhou X, Gupta N, Mirel D, Stahl EA, Diogo D, Cui J, Liao K, Guo MH, Myouzen K, Kawaguchi T, Coenen MJ, van Riel PL, van de Laar MA, Guchelaar HJ, Huizinga TW, Dieudé P, Mariette X, Bridges SL, Zhernakova A, Toes RE, Tak PP, Miceli-Richard C, Bang SY, Lee HS, Martin J, Gonzalez-Gay MA, Rodriguez-Rodriguez L, Rantapää-Dahlqvist S, Arlestig L, Choi HK, Kamatani Y, Galan P, Lathrop M, RACI consortium, GARNET consortium, Eyre S, Bowes J, Barton A, de Vries N, Moreland LW, Criswell LA, Karlson EW, Taniguchi A, Yamada R, Kubo M, Liu JS, Bae SC, Worthington J, Padyukov L, Klareskog L, Gregersen PK, Raychaudhuri S, Stranger BE, De Jager PL, Franke L, Visscher PM, Brown MA, Yamanaka H, Mimori T, Takahashi A, Xu H, Behrens TW, Siminovitch KA, Momohara S, Matsuda F, Yamamoto K, Plenge RM
  (2014) Nature 506: 376-81
• Molecular imaging by mass spectrometry--looking beyond classical histology.
  Schwamborn K, Caprioli RM
  (2010) Nat Rev Cancer 10: 639-46
• Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.
  Conn PJ, Lindsley CW, Meiler J, Niswender CM
  (2014) Nat Rev Drug Discov 13: 692-708
• Bringing together the academic drug discovery community.
  Slusher BS, Conn PJ, Frye S, Glicksman M, Arkin M
  (2013) Nat Rev Drug Discov 12: 811-2
• Tackling reproducibility in academic preclinical drug discovery.
  Frye SV, Arkin MR, Arrowsmith CH, Conn PJ, Glicksman MA, Hull-Ryde EA, Slusher BS
  (2015) Nat Rev Drug Discov 14: 733-4
• An interactive resource to identify cancer genetic and lineage dependencies targeted by small molecules.
  Basu A, Bodycombe NE, Cheah JH, Price EV, Liu K, Schaefer GI, Ebright RY, Stewart ML, Ito D, Wang S, Bracha AL, Liefeld T, Wawer M, Gilbert JC, Wilson AJ, Stransky N, Kryukov GV, Dancik V, Barretina J, Garraway LA, Hon CS, Munoz B, Bittker JA, Stockwell BR, Khabele D, Stern AM, Clemons PA, Shamji AF, Schreiber SL
  (2013) Cell 154: 1151-1161
• Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.
  Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA, NIH Molecular Libraries Project Team
  (2015) Cell 161: 1252-65
• An unbiased metric of antiproliferative drug effect in vitro.
  Harris LA, Frick PL, Garbett SP, Hardeman KN, Paudel BB, Lopez CF, Quaranta V, Tyson DR
  (2016) Nat Methods 13: 497-500
• Computational methods in drug discovery.
  Sliwoski G, Kothiwale S, Meiler J, Lowe EW
  (2014) Pharmacol Rev 66: 334-95
• The COXIB experience: a look in the rearview mirror.
  Marnett LJ
  (2009) Annu Rev Pharmacol Toxicol 49: 265-90
• The Future of Cardiovascular Therapeutics.
  MacRae CA, Roden DM, Loscalzo J
  (2016) Circulation 133: 2610-7
• Cardio-Oncology: How New Targeted Cancer Therapies and Precision Medicine Can Inform Cardiovascular Discovery.
  Bellinger AM, Arteaga CL, Force T, Humphreys BD, Demetri GD, Druker BJ, Moslehi JJ
  (2015) Circulation 132: 2248-58
• "Inverse Drug Discovery" Strategy To Identify Proteins That Are Targeted by Latent Electrophiles As Exemplified by Aryl Fluorosulfates.
  Mortenson DE, Brighty GJ, Plate L, Bare G, Chen W, Li S, Wang H, Cravatt BF, Forli S, Powers ET, Sharpless KB, Wilson IA, Kelly JW
  (2018) J Am Chem Soc 140: 200-210
• A fluorescence displacement assay for antidepressant drug discovery based on ligand-conjugated quantum dots.
  Chang JC, Tomlinson ID, Warnement MR, Iwamoto H, DeFelice LJ, Blakely RD, Rosenthal SJ
  (2011) J Am Chem Soc 133: 17528-31
• Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2.
  Delpire E, Days E, Lewis LM, Mi D, Kim K, Lindsley CW, Weaver CD
  (2009) Proc Natl Acad Sci U S A 106: 5383-8
• Computational design of protein-ligand interfaces: potential in therapeutic development.
  Morin A, Meiler J, Mizoue LS
  (2011) Trends Biotechnol 29: 159-66
• Improving the discovery of secondary metabolite natural products using ion mobility-mass spectrometry.
  Schrimpe-Rutledge AC, Sherrod SD, McLean JA
  (2018) Curr Opin Chem Biol 42: 160-166
• Assay strategies for identification of therapeutic leads that target protein trafficking.
  Conn PM, Spicer TP, Scampavia L, Janovick JA
  (2015) Trends Pharmacol Sci 36: 498-505
• Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia.
  Conn PJ, Lindsley CW, Jones CK
  (2009) Trends Pharmacol Sci 30: 25-31
• A Coordinated Attack: Rett Syndrome Therapeutic Development.
  Gogliotti RG, Niswender CM
  (2019) Trends Pharmacol Sci 40: 233-236
• The microculture-kinetic (MiCK) assay: the role of a drug-induced apoptosis assay in drug development and clinical care.
  Bosserman L, Prendergast F, Herbst R, Fleisher M, Salom E, Strickland S, Raptis A, Hallquist A, Perree M, Rajurkar S, Karimi M, Rogers K, Davidson D, Willis C, Penalver M, Homesley H, Burrell M, Garrett A, Rutledge J, Chernick M, Presant CA
  (2012) Cancer Res 72: 3901-5
• The MYC-WDR5 Nexus and Cancer.
  Thomas LR, Foshage AM, Weissmiller AM, Tansey WP
  (2015) Cancer Res 75: 4012-5
• Targeting the untargeted in molecular phenomics with structurally-selective ion mobility-mass spectrometry.
  May JC, Gant-Branum RL, McLean JA
  (2016) Curr Opin Biotechnol 39: 192-197
• Identification and use of biomarkers in treatment strategies for triple-negative breast cancer subtypes.
  Lehmann BD, Pietenpol JA
  (2014) J Pathol 232: 142-50
• Clinical translation of cell-based pharmacogenomic discovery.
  Cox NJ, Gamazon ER, Wheeler HE, Dolan ME
  (2012) Clin Pharmacol Ther 92: 425-7
• Quantitative network mapping of the human kinome interactome reveals new clues for rational kinase inhibitor discovery and individualized cancer therapy.
  Cheng F, Jia P, Wang Q, Zhao Z
  (2014) Oncotarget 5: 3697-710
• Discoidin domain receptor 1 (DDR1) kinase as target for structure-based drug discovery.
  Kothiwale S, Borza CM, Lowe EW, Pozzi A, Meiler J
  (2015) Drug Discov Today 20: 255-61
• Challenges and opportunities in developing respiratory syncytial virus therapeutics.
  Simões EA, DeVincenzo JP, Boeckh M, Bont L, Crowe JE, Griffiths P, Hayden FG, Hodinka RL, Smyth RL, Spencer K, Thirstrup S, Walsh EE, Whitley RJ
  (2015) J Infect Dis 211 Suppl 1: S1-S20
• Melanoma from bench to bedside: meeting report from the 6th international melanoma congress.
  Fisher DE, Barnhill R, Hodi FS, Herlyn M, Merlino G, Medrano E, Bastian B, Landi MT, Landi TM, Sosman J
  (2010) Pigment Cell Melanoma Res 23: 14-26
• Neurobiological Insights from mGlu Receptor Allosteric Modulation.
  O'Brien DE, Conn PJ
  (2016) Int J Neuropsychopharmacol 19:
• Development of allosteric modulators of GPCRs for treatment of CNS disorders.
  Nickols HH, Conn PJ
  (2014) Neurobiol Dis 61: 55-71
• Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A.
  Frank AO, Vangamudi B, Feldkamp MD, Souza-Fagundes EM, Luzwick JW, Cortez D, Olejniczak ET, Waterson AG, Rossanese OW, Chazin WJ, Fesik SW
  (2014) J Med Chem 57: 2455-61
• Discovery, synthesis, and structure-based optimization of a series of N-(tert-butyl)-2-(N-arylamido)-2-(pyridin-3-yl) acetamides (ML188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus (SARS-CoV) 3CL protease.
  Jacobs J, Grum-Tokars V, Zhou Y, Turlington M, Saldanha SA, Chase P, Eggler A, Dawson ES, Baez-Santos YM, Tomar S, Mielech AM, Baker SC, Lindsley CW, Hodder P, Mesecar A, Stauffer SR
  (2013) J Med Chem 56: 534-46
• Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragment-linking approach.
  Frank AO, Feldkamp MD, Kennedy JP, Waterson AG, Pelz NF, Patrone JD, Vangamudi B, Camper DV, Rossanese OW, Chazin WJ, Fesik SW
  (2013) J Med Chem 56: 9242-50
• Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.
  O'Reilly MC, Scott SA, Brown KA, Oguin TH, Thomas PG, Daniels JS, Morrison R, Brown HA, Lindsley CW
  (2013) J Med Chem 56: 2695-9
• Discovery of (R)-2-(6-Methoxynaphthalen-2-yl)butanoic Acid as a Potent and Selective Aldo-keto Reductase 1C3 Inhibitor.
  Adeniji A, Uddin MJ, Zang T, Tamae D, Wangtrakuldee P, Marnett LJ, Penning TM
  (2016) J Med Chem 59: 7431-44
• Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.
  Felts AS, Rodriguez AL, Smith KA, Engers JL, Morrison RD, Byers FW, Blobaum AL, Locuson CW, Chang S, Venable DF, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Emmitte KA
  (2015) J Med Chem 58: 9027-40
• Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).
  Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR
  (2014) J Med Chem 57: 7804-10
• Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM).
  Wenthur CJ, Morrison R, Felts AS, Smith KA, Engers JL, Byers FW, Daniels JS, Emmitte KA, Conn PJ, Lindsley CW
  (2013) J Med Chem 56: 5208-12