Skip to main content
2025
Leng L, Tu W, Yang L, Huang L, Wang M, Meagher JL, Chinnaswamy K, Allu SR, Rej RK, Tošović J, Harikrishnan L, Li Z, Sui Z, Stuckey JA, Wang S. Discovery of high-affinity SMARCA2/4 bromodomain ligands and development of potent and exceptionally selective SMARCA2 PROTAC degraders . J Med Chem . DOI: 10.1021/acs.jmedchem.4c01903.
Yang L, Tu W, Leng L, Huang L, Jiang W, Wang M, Wang Y, Meagher JL, Chinnaswamy K, Stuckey JA, Wang M, Wen B, Sun D, Harikrishnan L, Strickland C, Rice C, Orth P, Sui Z, Wang S. Discovery of SMD-3236: A potent, highly selective and efficacious SMARCA2 degrader for the treatment of SMARC4-deficient human cancers . J Med Chem . DOI: 10.1021/acs.jmedchem.4c01904.
Pan WW, Weh KM, Chaudhury S, Fernando R, Hager H, Wen B, Chinnaswamy K, Stuckey JA, Rech JC, Besirli CG, Weh E, Wubben TJ. A novel, long-acting, small molecule PKM2 activator and its potential broad application against photoreceptor degeneration . Transl Vis Sci Technol . DOI: 10.1167/tvst.14.7.26.
Kaneshige A, Yang Y, Bai L, Wang M, Xu R, Mallik L, Chinnaswamy K, Metwally H, Wang Y, McEachern D, Tošović J, Yang CY, Kirchhoff PD, Meagher JL, Stuckey JA, Wang S. Discovery of AK-1690: A potent and highly selective STAT6 PROTAC degrader . J Med Chem . DOI: 10.1021/acs.jmedchem.4c01009.
2024
Yuan T, Kumar S, Skinner ME, Victor-Joseph R, Abuaita M, Keijer J, Zhang J, Kunkel TJ, Liu Y, Petrunak EM, Saunders TL, Lieberman AP, Stuckey JA, Neamati N, Al-Murshedi F, Alfadhel M, Spelbrink JN, Rodenburg R, de Boer VCJ, Lombard DB. Human SIRT5 variants with reduced stability and activity do not cause neuropathology in mice . iScience . DOI: 10.1016/j.isci.2024.109991.
Xu R, Zhou H, Bai L, McEachern D, Wu D, Acharyya RK, Wang M, Tošović J, Yang CY, Chinnaswamy K, Meagher JL, Stuckey JA, Liu C, Wang M, Wen B, Sun D, Wang S. Discovery of SD-436: A potent, highly selective and efficacious STAT3 PROTAC degrader capable of achieving complete and long-lasting tumor regression . J Med Chem . DOI: 10.1021/acs.jmedchem.4c01946.
Yeoh ZC, Meagher JL, Kang CY, Bieniasz PD, Smith JL, Ohi MD. A minimal complex of KHNYN and zinc-finger antiviral protein binds and degrades single-stranded RNA . Proc Natl Acad Sci U S A . DOI: 10.1073/pnas.2415048121.
Bohn JA, Meagher JL, Takata MA, Gonçalves-Carneiro D, Yeoh ZC, Ohi MD, Smith JL, Bieniasz PD. Functional anatomy of zinc finger antiviral protein complexes . Nat Commun . DOI: 10.1038/s41467-024-55192-z.
2023
Kaneshige A, Bai L, Wang M, McEachern D, Meagher JL, Xu R, Wang Y, Jiang W, Metwally H, Kirchhoff PD, Zhao L, Jiang H, Wang M, Wen B, Sun D, Stuckey JA, Wang S. A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo . Nat Chem Biol. DOI: 10.1038/s41589-022-01248-4.
Kaneshige A, Bai L, Wang M, McEachern D, Meagher JL, Xu R, Kirchhoff PD, Wen B, Sun D, Stuckey JA, Wang S. Discovery of a potent and selective STAT5 PROTAC degrader with strong antitumor activity in vivo in acute myeloid leukemia . J Med Chem . DOI: 10.1021/acs.jmedchem.2c01665.
Hu J, Hu B, Xu F, Wang M, Qin C, McEachern D, Stuckey J, Wang S. Precise conformational control yielding highly potent and exceptionally selective BRD4 degraders with strong antitumor activity . J Med Chem . DOI: 10.1021/acs.jmedchem.3c00520.
Yuan X, Jiang H, Fu D, Rech JC, Robida A, Rajanayake K, Yuan H, He M, Wen B, Sun D, Liu C, Chinnaswamy K, Stuckey JA, Paczesny S, Yang CY. Prophylactic mitigation of acute graft versus host disease by novel 2-(Pyrrolidin-1-ylmethyl)pyrrole-based stimulation-2 (ST2) inhibitors . ACS Pharmacol Transl Sci . DOI: 10.1021/acsptsci.3c00122.
2022
Liu J, Carlson HA, Scott EE. The structure and characterization of human cytochrome P450 8B1 supports future drug design for nonalcoholic fatty liver disease and diabetes . J Biol Chem. DOI: 10.1016/j.jbc.2022.102344.
Bart AG, Morias G, Vangala VR, Loadman PM, Pors K, Scott, EE. Cytochrome P450 binding and bioactivation of tumor-targeted duocarmycin agents . Drug Metab Dispos. DOI: 10.1124/dmd.121.000642.
Lao Y , Skiba MA, Chun SW, Narayan ARH, Smith JL. Structural basis for control of methylation extent in polyketide synthase metal-dependent C -methyltransferases . ACS Chem Biol . DOI: 10.1021/acschembio.2c00085.
Pham VV, Gao M, Meagher JL, Smith JL, D’Souza VM. A structure-based mechanism for displacement of the HEXIM adapter from 7SK small nuclear RNA . Comms Bio . DOI: 0.1038/s42003-022-03734-w.
Kelly AS, Shende V, Flynn A, Dan Q, Ye Y, Smith JL, Tsukamoto S, Sigman M, Sherman DH. Data science-driven analysis of substrate-permissive diketopiperazine reverse prenyltransferase NotF: Applications in protein engineering and cascade biocatalytic synthesis of (–)-eurotiumin . J Amer Chem Soc . DOI: 10.1021/jacs.2c06631.
Cerqueira, FM, Photenhauer, AL, Doden, HL, Brown, AN, Abdel-Hamid, AM, Moraïs, S, Bayer, E, Wawrzak,Z, Cann, I, Ridlon, JM, Hopkins, J, Koropatkin, NM. Sas20 is a highly flexible starch-binding protein in the Ruminococcus bromii cell-surface amylosome . J Biol Chem . Doi: 10.1016/j.jbc.2022.101896.
Kermani AA, Burata OE, Koff BB, Koide A, Koide S, Stockbridge RB. Crystal structures of bacterial small multidrug resistance transporter EmrE in complex with structurally diverse substrates . eLife. DOI: 10.7554/eLife.76766.
Li B, Jo M, Liu J, Tian J, Canfield R, Bridwell-Rabb. Structural and mechanistic basis for redox sensing by the cyanobacterial transcription regulator RexT . Commun Biol. DOI: 10.1038/s42003-022-03226-x.
2021
Biering SB, Akey DL, Wong MP, Brown WC, Lo NTN, Puerta-Guardo H, Tramontini Gomesde Sousa F, Wang C, Konwerski JR, Espinosa DA, Bockhaus NJ, GlasnerCR, Li J, Blanc SF, Juan EY, Elledge SJ, Mina MJ, Beatty PR, Smith JL, Harris E. Structural basis for antibody inhibition of flavivirus NS1-triggered endothelial dysfunction . Science . DOI: 10.1126/science.abc0.
Park KS, Bazzill JD, Son S, Nam J, Shin SW, Ochyl LJ, Stuckey JA, Meagher JL, Chang L, Song J, Montefiori DC, LaBranche CC, Smith JL, Xu J, Moon JJ. Lipid-based vaccine nanoparticles for induction of humoral immune responses against HIV-1 and SARS-CoV-2 . J Control Release . DOI:10.1016/j.jconrel.2020.12.031.
Pinter TBJ, Ruckthong L, Stuckey JA, Deb A, Penner-Hahn JE, Pecoraro VL. Open reading frame 1 protein of the human long interspersed nuclear element 1 retrotransposon binds multiple equivalents of lead . J Am Chem Soc . DOI: 10.1021/jacs.1c06461.
Rej RK, Wang C, Lu J, Wang M, Petrunak E, Zawacki KP, McEachern D, Yang CY, Wang L, Li R, Chinnaswamy K, Wen B, Sun D, Stuckey JA, Zhou Y, Chen J, Tang G, Wang S. Discovery of EEDi-5273 as an exceptionally potent and orally efficacious EED inhibitor capable of achieving complete and persistent tumor regression . J Med Chem . DOI: 10.1021/acs.jmedchem.1c01059.
Zhou H, Lu J, Liu L, McEachern D, Yang C-Y, Bernard D, Chinnaswamy K, Stuckey J, Shen H, Rui L, Sun Y, Wang S. Selective Cullin-3 inhibition via covalent DCN1binding effectively protects mice from Acetaminophen-induced liver toxicity . Nat Commun . DOI: 10.1038/s41467-021-22924-4.
