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Page 1
Discovery of Nanomolar DCAF1 Small Molecule Ligands.
Li ASM, Kimani S, Wilson B, Noureldin M, González-Álvarez H, Mamai A, Hoffer L, Guilinger JP, Zhang Y, von Rechenberg M, Disch JS, Mulhern CJ, Slakman BL, Cuozzo JW, Dong A, Poda G, Mohammed M, Saraon P, Mittal M, Modh P, Rathod V, Patel B, Ackloo S, Santhakumar V, Szewczyk MM, Barsyte-Lovejoy D, Arrowsmith CH, Marcellus R, Guié MA, Keefe AD, Brown PJ, Halabelian L, Al-Awar R, Vedadi M. Li ASM, et al. Among authors: disch js. J Med Chem. 2023 Apr 13;66(7):5041-5060. doi: 10.1021/acs.jmedchem.2c02132. Epub 2023 Mar 22. J Med Chem. 2023. PMID: 36948210 Free PMC article.
Crystallographic structure of a small molecule SIRT1 activator-enzyme complex.
Dai H, Case AW, Riera TV, Considine T, Lee JE, Hamuro Y, Zhao H, Jiang Y, Sweitzer SM, Pietrak B, Schwartz B, Blum CA, Disch JS, Caldwell R, Szczepankiewicz B, Oalmann C, Yee Ng P, White BH, Casaubon R, Narayan R, Koppetsch K, Bourbonais F, Wu B, Wang J, Qian D, Jiang F, Mao C, Wang M, Hu E, Wu JC, Perni RB, Vlasuk GP, Ellis JL. Dai H, et al. Among authors: disch js. Nat Commun. 2015 Jul 2;6:7645. doi: 10.1038/ncomms8645. Nat Commun. 2015. PMID: 26134520 Free PMC article.
Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy.
Nissink JWM, Bazzaz S, Blackett C, Clark MA, Collingwood O, Disch JS, Gikunju D, Goldberg K, Guilinger JP, Hardaker E, Hennessy EJ, Jetson R, Keefe AD, McCoull W, McMurray L, Olszewski A, Overman R, Pflug A, Preston M, Rawlins PB, Rivers E, Schimpl M, Smith P, Truman C, Underwood E, Warwicker J, Winter-Holt J, Woodcock S, Zhang Y. Nissink JWM, et al. Among authors: disch js. J Med Chem. 2021 Mar 25;64(6):3165-3184. doi: 10.1021/acs.jmedchem.0c01904. Epub 2021 Mar 8. J Med Chem. 2021. PMID: 33683117
Bispecific Estrogen Receptor α Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening.
Disch JS, Duffy JM, Lee ECY, Gikunju D, Chan B, Levin B, Monteiro MI, Talcott SA, Lau AC, Zhou F, Kozhushnyan A, Westlund NE, Mullins PB, Yu Y, von Rechenberg M, Zhang J, Arnautova YA, Liu Y, Zhang Y, McRiner AJ, Keefe AD, Kohlmann A, Clark MA, Cuozzo JW, Huguet C, Arora S. Disch JS, et al. J Med Chem. 2021 Apr 22;64(8):5049-5066. doi: 10.1021/acs.jmedchem.1c00127. Epub 2021 Apr 12. J Med Chem. 2021. PMID: 33844532
Discovery of Small Molecule Interleukin 17A Inhibitors with Novel Binding Mode and Stoichiometry: Optimization of DNA-Encoded Chemical Library Hits to In Vivo Active Compounds.
Ramos AL, Goedken ER, Frank KE, Argiriadi MA, Bazzaz S, Bian Z, Brown JTC, Centrella PA, Chen HJ, Disch JS, Donner PL, Duignan DB, Gikunju D, Greszler SN, Guié MA, Habeshian S, Hartl HE, Hein CD, Hutchins CW, Jetson R, Keefe AD, Khan H, Li HQ, Olszewski A, Ortiz Cardona BJ, Osuma A, Panchal SC, Phelan R, Qiu W, Shotwell JB, Shrestha A, Srikumaran M, Su Z, Sun C, Upadhyay AK, Wood MD, Wu H, Zhang R, Zhang Y, Zhao G, Zhu H, Webster MP. Ramos AL, et al. Among authors: disch js. J Med Chem. 2024 Apr 25;67(8):6456-6494. doi: 10.1021/acs.jmedchem.3c02397. Epub 2024 Apr 4. J Med Chem. 2024. PMID: 38574366
A Target Class Ligandability Evaluation of WD40 Repeat-Containing Proteins.
Ackloo S, Li F, Szewczyk M, Seitova A, Loppnau P, Zeng H, Xu J, Ahmad S, Arnautova YA, Baghaie AJ, Beldar S, Bolotokova A, Centrella PA, Chau I, Clark MA, Cuozzo JW, Dehghani-Tafti S, Disch JS, Dong A, Dumas A, Feng JA, Ghiabi P, Gibson E, Gilmer J, Goldman B, Green SR, Guié MA, Guilinger JP, Harms N, Herasymenko O, Houliston S, Hutchinson A, Kearnes S, Keefe AD, Kimani SW, Kramer T, Kutera M, Kwak HA, Lento C, Li Y, Liu J, Loup J, Machado RAC, Mulhern CJ, Perveen S, Righetto GL, Riley P, Shrestha S, Sigel EA, Silva M, Sintchak MD, Slakman BL, Taylor RD, Thompson J, Torng W, Underkoffler C, von Rechenberg M, Walsh RT, Watson I, Wilson DJ, Wolf E, Yadav M, Yazdi AK, Zhang J, Zhang Y, Santhakumar V, Edwards AM, Barsyte-Lovejoy D, Schapira M, Brown PJ, Halabelian L, Arrowsmith CH. Ackloo S, et al. Among authors: disch js. J Med Chem. 2024 Nov 4. doi: 10.1021/acs.jmedchem.4c02010. Online ahead of print. J Med Chem. 2024. PMID: 39495097
Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.
Vu CB, Bemis JE, Disch JS, Ng PY, Nunes JJ, Milne JC, Carney DP, Lynch AV, Smith JJ, Lavu S, Lambert PD, Gagne DJ, Jirousek MR, Schenk S, Olefsky JM, Perni RB. Vu CB, et al. Among authors: disch js. J Med Chem. 2009 Mar 12;52(5):1275-83. doi: 10.1021/jm8012954. J Med Chem. 2009. PMID: 19199480
Discovery of a selective c-MET inhibitor with a novel binding mode.
Collie GW, Barlind L, Bazzaz S, Börjesson U, Dale IL, Disch JS, Habeshian S, Jetson R, Khurana P, Madin A, Michaelides IN, Peng L, Snijder A, Stubbs CJ. Collie GW, et al. Among authors: disch js. Bioorg Med Chem Lett. 2022 Nov 1;75:128948. doi: 10.1016/j.bmcl.2022.128948. Epub 2022 Aug 17. Bioorg Med Chem Lett. 2022. PMID: 35987508 Free article.
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes.
Milne JC, Lambert PD, Schenk S, Carney DP, Smith JJ, Gagne DJ, Jin L, Boss O, Perni RB, Vu CB, Bemis JE, Xie R, Disch JS, Ng PY, Nunes JJ, Lynch AV, Yang H, Galonek H, Israelian K, Choy W, Iffland A, Lavu S, Medvedik O, Sinclair DA, Olefsky JM, Jirousek MR, Elliott PJ, Westphal CH. Milne JC, et al. Among authors: disch js. Nature. 2007 Nov 29;450(7170):712-6. doi: 10.1038/nature06261. Nature. 2007. PMID: 18046409 Free PMC article.
14 results