Small Molecule Publications

Below is a list of publications that have resulted from small molecule screening efforts at ICCB-Longwood. Please notify us of your publications that involve use of the ICCB-Longwood Screening Facility.

Lee S-W, Tran KT, Vazquez-Uribe R, Gotfredsen CH, Clausen MH, Mendez BL, Montoya G, Bach A, Sommer MOA. Identification and Optimization of Novel Small-Molecule Cas9 Inhibitors by Cell-Based High-Throughput Screening [Internet]. J. Med. Chem. 2022;65(4):3266-3305. Publisher's Version

Zhang H-XB, Heckman L, Niday Z, Jo S, Fujita A, Shim J, Pandey R, Jandal HA, Jayakar S, Barrett LB, Smith J, Woolf CJ, Bean BP. Cannabidiol activates neuronal Kv7 channels [Internet]. Ellife 2022;2022(11:e73246) Publisher's Version

Finardi NF, Hernandez LZ, Russell MRG, Ho CM-K, Sreenu VB, Wenham HA, Merritt A, Strang BL. Identification and characterization of bisbenzimide compounds that inhibit human cytomegalovirus replication. J Gen Virol. 2021;102(12):001702.

Zhou J, Gelot C, Pantelidou C, Li A, Yücel H, Davis RE, Farkkila A, Kochupurakkal B, Syed A, Shapiro GI, Tainer JA, Blagg BSJ, Ceccaldi R, D'Andrea AD. A first-in-class Polymerase Theta Inhibitor selectively targets Homologous-Recombination-Deficient Tumors. Nat Cancer 2021;2(6):598-610.

Zee BM, Poels KE, Yao C-H, Kawabata KC, Wu G, Duy C, Jacobus WD, Senior E, Endress JE, Jambhekar A, Lovitch SB, Ma J, Dhall A, Harris IS, Blanco MA, Sykes DB, Licht JD, Weinstock DM, Melnick A, Haigis MC, Michor F, Shi Y. Combined epigenetic and metabolic treatments overcome differentiation blockade in acute myeloid leukemia [Internet]. iScience 2021;24(6) Publisher's Version

Chang D, Luong P, Li Q, LeBarron J, Anderson M, Barrett L, Lencer WI. Small-molecule modulators of INAVA cytosolic condensate and cell–cell junction assemblies. J Cell Biol 2021;220(9)

Wang ES, Verano AL, Nowak RP, Yuan JC, Donovan KA, Eleuteri NA, Yue H, Ngo KH, Lizotte PH, Gokhale PC, Gray NS, Fischer ES. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol 2021;17(6):711-717.

Martínez-Noel G, Vieira VC, Szajner P, Lilienthal EM, Kramer RE, Boyland KA, Smith JA, Howley PM. Live cell, image-based high-throughput screen to quantitate p53 stabilization and viability in human papillomavirus positive cancer cells. Virology 2021;560:96-109.

Mori Y, Ajay AK, Chang J-H, Mou S, Zhao H, Kishi S, Li J, Brooks CR, Xiao S, Woo H-M, Sabbisetti VS, Palmer SC, Galichon P, Li L, Henderson M, Kuchroo VK, Hawkins J, Ichimura T, Bonventre JV. KIM-1 mediates fatty acid uptake by renal tubular cells to promote progressive diabetic kidney disease. Cell Metab. 2021;33(5):1042-1061.

Bennett CF, O'Malley KE, Perry EA, Balsa E, Latorre-Muro P, Riley CL, Luo C, Jedrychowski M, Gygi SP, Puigserver P. Peroxisomal-derived ether phospholipids link nucleotides to respirasome assembly. Nat Chem Biol 2021;17(6):703-710.

Koduri V, Duplaquet L, Lampson BL, Wang AC, Sabet AH, Ishoey M, Paulk J, Teng M, Harris IS, Endress JE, Liu X, Dasilva E, Paulo JA, Briggs KJ, Doench JG, Ott CJ, Zhang T, Donovan KA, Fischer ES, Gygi SP, Gray NS, Bradner J, Medin JA, Buhrlage SJ, Oser MG, Kaelin WG. Targeting oncoproteins with a positive selection assay for protein degraders. Science Advances 2021;7(6)

Perry EA, Bennett CF, Luo C, Balsa E, Jedrychowski M, KE.O’Malley, Latorre-Muro P, Ladley RP, Reda K, Wright PM, Gygi SP, Myers AG, Puigserver P. Tetracyclines promote survival and fitness in mitochondrial disease models . Nature Metabolism 2021;3:33-42.

Baidin V, Owens TW, Lazarus MB, Kahne D. Simple Secondary Amines Inhibit Growth of Gram-Negative Bacteria through Highly Selective Binding to Phenylalanyl-tRNA Synthetase. J Am Chem Soc 2021;(Jan 7)

Drijvers JM, Gillis JE, Muijlwijk T, Nguyen TH, Gaudiano EF, Harris IS, LaFleur MW, Ringel AE, Yao C-H, Kurmi K, Juneja VR, Trombley JD, Haigis MC, Sharpe AH. Pharmacologic Screening Identifies Metabolic Vulnerabilities of CD8 + T Cells. Cancer Immunol Res 2020;(Dec 4)

Xu D, Zhao H, Jin M, Zhu H, Shan B, Geng J, Dziedzic SA, Amin P, Mifflin L, Naito MG, Najafov A, Xing J, Yan L, Liu J, Qin Y, Hu X, Wang H, Zhang M, Manuel VJ, Tan L, He Z, Sun ZJ, Lee VMY, Wagner G, Yuan J. Modulating TRADD to restore cellular homeostasis and inhibit apoptosis. Nature 2020;587(7832):133-138.

Zervantonakis IK, Poskus MD, Scott AL, Selfors LM, Lin JR, Dillon DA, Pathania S, Sorger PK, Mills GB, Brugge JS. Fibroblast-tumor Cell Signaling Limits HER2 Kinase Therapy Response via Activation of MTOR and Antiapoptotic Pathways. Proc Natl Acad Sci USA 2020;117(28):16500-16508.

Santos DM, Pantano L, Pronzati G, Grasberger P, Probst CK, Black KE, Spinney JJ, Hariri LP, Nichols R, Lin Y, Bieler M, Seither P, Nicklin P, Wyatt D, Tager AM, Medoff BD. Screening for YAP Inhibitors Identifies Statins as Modulators of Fibrosis. Am J Respir Cell Mol Biol 2020;62(4):479-492.

Hu JJ, Liu X, Xia S, Zhang Z, Zhang Y, Zhao J, Ruan J, Luo X, Lou X, Bai Y, Wang J, Hollingsworth LR, Magupalli VG, Zhao L, Luo HR, Kim J, Lieberman J, Wu H. FDA-approved disulfiram inhibits pyroptosis by blocking gasdermin D pore formation. Nature Immunology 2020;21(7):736-745.

Rupaimoole R, Yoon B, Zhang WC, Adams BD, Slack FJ. A High-Throughput Small Molecule Screen Identifies Ouabain as Synergistic with miR-34a in Killing Lung Cancer Cells. iScience 2020;23(2)

Gorgulla C, Boeszoermenyi A, Wang ZF, Fischer PD, Coote P, Padmanabha Das KM, Malets YS, Radchenko DS, Moroz YS, Scott DA, Fackeldey K, Hoffmann M, Iavniuk I, Wagner G, Arthanari H. An open-source drug discovery platform enables ultra-large virtual screens. Nature 2020;580(7805):663-668.

Xiao T, Frey G, Fu Q, Lavine CL, Scott DA, Seaman MS, Chou JJ, Chen B. HIV-1 fusion inhibitors targeting the membrane-proximal external region of Env spikes. Nat Chem Biol 2020;16(5):529-537.

Imberdis T, Negri J, Ramalingam N, Terry-Kantor E, Ho GPH, Fanning S, Stirtz G, Kim TE, Levy OA, Young-Pearse TL, Selkoe D, Dettmer U. Cell Models of Lipid-Rich α-Synuclein Aggregation Validate Known Modifiers of α-Synuclein Biology and Identify stearoyl-CoA Desaturase. Proc Natl Acad Sci U S A 2019;116(41):20760-20769.

Kim W, Zou G, Hari TPA, Wilt IK, Zhu W, Galle N, Faizi HA, Hendricks GL, Tori K, Pan W, Huang X, Steele AD, Csatary EE, Dekarske MM, Rosen JL, Ribeiro NQ, Lee K, Port J, Fuchs BB, Vlahovska PM, Wuest WM, Gao H, Ausubel FM, Mylonakis E. A selective membrane-targeting repurposed antibiotic with activity against persistent methicillin-resistant Staphylococcus aureus. Proc Natl Acad Sci U S A. 2019;116(33):16529-16534.

Wu P, Bjørn-Yoshimoto WE, Staudt M, Jensen AA, Bunch L. Identification and Structure-Activity Relationship Study of Imidazo[1,2-a]pyridine-3-amines as First Selective Inhibitors of Excitatory Amino Acid Transporter Subtype 3 (EAAT3). ACS Chem Neurosci 2019;10(10):4414-4429.

Nicholson HE, Tariq Z, Housden BE, Jennings RB, Stransky LA, Perrimon N, Signoretti S, Kaelin WGJ. HIF-independent synthetic lethality between CDK4/6 inhibition and VHL loss across species. Science Signaling 2019;12(601)

Smith KP, Dowgiallo MG, Chiaraviglio L, Parvatkar P, Kim C, Manetsch R, Kirby JE. A Whole-Cell Screen for Adjunctive and Direct Antimicrobials Active against Carbapenem-Resistant Enterobacteriaceae. SLAS Discovery 2019;24(8):842-853.

Shlevkov E, Basu H, Bray MA, Sun Z, Wei W, Apaydin K, Karhohs K, Chen PF, Smith JLM, Wiskow O, Roet K, Huang X, Eggan K, Carpenter AE, Kleiman RJ, Schwarz TL. A High-Content Screen Identifies TPP1 and Aurora B as Regulators of Axonal Mitochondrial Transport. Cell Reports 2019;28(12):3224-3237.

de Wispelaere M, Du G, Donovan KA, Zhang T, Eleuteri NA, Yuan JC, Kalabathula J, Nowak RP, Fischer ES, Gray NS, Yang PL. Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations. Nature Communications 2019;10(1):3468.

Harris IS, Endress JE, Coloff JL, Selfors LM, McBrayer SK, Rosenbluth JM, Takahashi N, Dhakal S, Koduri V, Oser MG, Schauer NJ, Doherty LM, Hong AL, Kang YP, Younger ST, Doench JG, Hahn WC, Buhrlage SJ, DeNicola GM, Kaelin WGJ, Brugge JS. Deubiquitinases Maintain Protein Homeostasis and Survival of Cancer Cells upon Glutathione Depletion. Cell Metab 2019;29:1-16.

Pitts J, Hsia CY, Lian W, Wang J, Pfeil MP, Kwiatkowski N, Li Z, Jang J, Gray NS, Yang PL. Identification of small molecule inhibitors targeting the Zika virus envelope protein. Antiviral Res 2019;S0166-3542(18):30765-4.

ICCB-Longwood Screening Facility

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