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•  Galina Lepesheva

•  Stephen Fesik

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Publications

• Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.
  Lindsley CW, Emmitte KA, Hopkins CR, Bridges TM, Gregory KJ, Niswender CM, Conn PJ
  (2016) Chem Rev 116: 6707-41
• Proof of principle for epitope-focused vaccine design.
  Correia BE, Bates JT, Loomis RJ, Baneyx G, Carrico C, Jardine JG, Rupert P, Correnti C, Kalyuzhniy O, Vittal V, Connell MJ, Stevens E, Schroeter A, Chen M, Macpherson S, Serra AM, Adachi Y, Holmes MA, Li Y, Klevit RE, Graham BS, Wyatt RT, Baker D, Strong RK, Crowe JE, Johnson PR, Schief WR
  (2014) Nature 507: 201-6
• Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders.
  Conn PJ, Christopoulos A, Lindsley CW
  (2009) Nat Rev Drug Discov 8: 41-54
• Aspirin-like molecules that covalently inactivate cyclooxygenase-2.
  Kalgutkar AS, Crews BC, Rowlinson SW, Garner C, Seibert K, Marnett LJ
  (1998) Science 280: 1268-70
• Discovering high-affinity ligands for proteins.
  Hajduk PJ, Meadows RP, Fesik SW
  (1997) Science 278: 497,499
• Targeting nonclassical oncogenes for therapy in T-ALL.
  Subramaniam PS, Whye DW, Efimenko E, Chen J, Tosello V, De Keersmaecker K, Kashishian A, Thompson MA, Castillo M, Cordon-Cardo C, Davé UP, Ferrando A, Lannutti BJ, Diacovo TG
  (2012) Cancer Cell 21: 459-72
• A live, impaired-fidelity coronavirus vaccine protects in an aged, immunocompromised mouse model of lethal disease.
  Graham RL, Becker MM, Eckerle LD, Bolles M, Denison MR, Baric RS
  (2012) Nat Med 18: 1820-6
• Metabotropic glutamate receptors on peripheral sensory neuron terminals as targets for the development of novel analgesics.
  Karim F, Bhave G, Gereau RW
  (2001) Mol Psychiatry 6: 615-7
• Sign Inversion in Photopharmacology: Incorporation of Cyclic Azobenzenes in Photoswitchable Potassium Channel Blockers and Openers.
  Trads JB, Hüll K, Matsuura BS, Laprell L, Fehrentz T, Görldt N, Kozek KA, Weaver CD, Klöcker N, Barber DM, Trauner D
  (2019) Angew Chem Int Ed Engl 58: 15421-15428
• Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
  Scott SA, Selvy PE, Buck JR, Cho HP, Criswell TL, Thomas AL, Armstrong MD, Arteaga CL, Lindsley CW, Brown HA
  (2009) Nat Chem Biol 5: 108-17
• HCV Broadly Neutralizing Antibodies Use a CDRH3 Disulfide Motif to Recognize an E2 Glycoprotein Site that Can Be Targeted for Vaccine Design.
  Flyak AI, Ruiz S, Colbert MD, Luong T, Crowe JE, Bailey JR, Bjorkman PJ
  (2018) Cell Host Microbe 24: 703-716.e3
• Principles of Broad and Potent Antiviral Human Antibodies: Insights for Vaccine Design.
  Crowe JE
  (2017) Cell Host Microbe 22: 193-206
• NMR-based screening in drug discovery.
  Hajduk PJ, Meadows RP, Fesik SW
  (1999) Q Rev Biophys 32: 211-40
• Designing sequence to control protein function in an EF-hand protein.
  Bunick CG, Nelson MR, Mangahas S, Hunter MJ, Sheehan JH, Mizoue LS, Bunick GJ, Chazin WJ
  (2004) J Am Chem Soc 126: 5990-8
• Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy.
  Szczepankiewicz BG, Liu G, Hajduk PJ, Abad-Zapatero C, Pei Z, Xin Z, Lubben TH, Trevillyan JM, Stashko MA, Ballaron SJ, Liang H, Huang F, Hutchins CW, Fesik SW, Jirousek MR
  (2003) J Am Chem Soc 125: 4087-96
• Rational design of diflunisal analogues with reduced affinity for human serum albumin.
  Mao H, Hajduk PJ, Craig R, Bell R, Borre T, Fesik SW
  (2001) J Am Chem Soc 123: 10429-35
• The rational design and construction of a cuboidal iron-sulfur protein.
  Coldren CD, Hellinga HW, Caradonna JP
  (1997) Proc Natl Acad Sci U S A 94: 6635-40
• Activation of heme biosynthesis by a small molecule that is toxic to fermenting Staphylococcus aureus.
  Mike LA, Dutter BF, Stauff DL, Moore JL, Vitko NP, Aranmolate O, Kehl-Fie TE, Sullivan S, Reid PR, DuBois JL, Richardson AR, Caprioli RM, Sulikowski GA, Skaar EP
  (2013) Proc Natl Acad Sci U S A 110: 8206-11
• Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.
  Kalgutkar AS, Crews BC, Rowlinson SW, Marnett AB, Kozak KR, Remmel RP, Marnett LJ
  (2000) Proc Natl Acad Sci U S A 97: 925-30
• Design of selective inhibitors of cyclooxygenase-2 as nonulcerogenic anti-inflammatory agents.
  Marnett LJ, Kalgutkar AS
  (1998) Curr Opin Chem Biol 2: 482-90
• Allosteric modulation of kinases and GPCRs: design principles and structural diversity.
  Lewis JA, Lebois EP, Lindsley CW
  (2008) Curr Opin Chem Biol 12: 269-80
• Phospholipase D as a therapeutic target in brain disorders.
  Lindsley CW, Brown HA
  (2012) Neuropsychopharmacology 37: 301-2
• Opportunities and challenges of psychiatric drug discovery: roles for scientists in academic, industry, and government settings.
  Conn PJ, Roth BL
  (2008) Neuropsychopharmacology 33: 2048-60
• Muscarinic and nicotinic acetylcholine receptor agonists and allosteric modulators for the treatment of schizophrenia.
  Jones CK, Byun N, Bubser M
  (2012) Neuropsychopharmacology 37: 16-42
• The role of VHL in clear-cell renal cell carcinoma and its relation to targeted therapy.
  Clark PE
  (2009) Kidney Int 76: 939-45
• Cytochromes P450 and drug discovery.
  Lamb DC, Waterman MR, Kelly SL, Guengerich FP
  (2007) Curr Opin Biotechnol 18: 504-12
• Impact of genomics on personalized cancer medicine.
  Arteaga CL, Baselga J
  (2012) Clin Cancer Res 18: 612-8
• Sigma receptors: potential targets for a new class of antidepressant drug.
  Fishback JA, Robson MJ, Xu YT, Matsumoto RR
  (2010) Pharmacol Ther 127: 271-82
• ACR 20: clinical or statistical significance?
  Pincus T, Stein CM
  (1999) Arthritis Rheum 42: 1572-6
• Pineal serotonin is resistant to depletion by serotonergic neurotoxins in rats.
  Champney TH, Matthews RT
  (1991) J Pineal Res 11: 163-7
• Cytochrome P450 proteins and potential utilization in biodegradation.
  Guengerich FP
  (1995) Environ Health Perspect 103 Suppl 5: 25-8
• Factor XI as a target for antithrombotic therapy.
  Bane CE, Gailani D
  (2014) Drug Discov Today 19: 1454-8
• Neurobiological Insights from mGlu Receptor Allosteric Modulation.
  O'Brien DE, Conn PJ
  (2016) Int J Neuropsychopharmacol 19:
• Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.
  Dhanya RP, Sheffler DJ, Dahl R, Davis M, Lee PS, Yang L, Nickols HH, Cho HP, Smith LH, D'Souza MS, Conn PJ, Der-Avakian A, Markou A, Cosford ND
  (2014) J Med Chem 57: 4154-72
• NMR-driven discovery of benzoylanthranilic acid inhibitors of far upstream element binding protein binding to the human oncogene c-myc promoter.
  Huth JR, Yu L, Collins I, Mack J, Mendoza R, Isaac B, Braddock DT, Muchmore SW, Comess KM, Fesik SW, Clore GM, Levens D, Hajduk PJ
  (2004) J Med Chem 47: 4851-7
• Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design.
  Friberg A, Vigil D, Zhao B, Daniels RN, Burke JP, Garcia-Barrantes PM, Camper D, Chauder BA, Lee T, Olejniczak ET, Fesik SW
  (2013) J Med Chem 56: 15-30
• Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.
  Hajduk PJ, Dinges J, Schkeryantz JM, Janowick D, Kaminski M, Tufano M, Augeri DJ, Petros A, Nienaber V, Zhong P, Hammond R, Coen M, Beutel B, Katz L, Fesik SW
  (1999) J Med Chem 42: 3852-9
• Selective mode of action of guanidine-containing non-peptides at human NPFF receptors.
  Findeisen M, Würker C, Rathmann D, Meier R, Meiler J, Olsson R, Beck-Sickinger AG
  (2012) J Med Chem 55: 6124-36
• Structural basis for rational design of inhibitors targeting Trypanosoma cruzi sterol 14α-demethylase: two regions of the enzyme molecule potentiate its inhibition.
  Friggeri L, Hargrove TY, Rachakonda G, Williams AD, Wawrzak Z, Di Santo R, De Vita D, Waterman MR, Tortorella S, Villalta F, Lepesheva GI
  (2014) J Med Chem 57: 6704-17
• NMR-based discovery of lead inhibitors that block DNA binding of the human papillomavirus E2 protein.
  Hajduk PJ, Dinges J, Miknis GF, Merlock M, Middleton T, Kempf DJ, Egan DA, Walter KA, Robins TS, Shuker SB, Holzman TF, Fesik SW
  (1997) J Med Chem 40: 3144-50