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From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors.
Koravovic M, Mayasundari A, Tasic G, Keramatnia F, Stachowski TR, Cui H, Chai SC, Jonchere B, Yang L, Li Y, Fu X, Hiltenbrand R, Paul L, Mishra V, Klco JM, Roussel MF, Pomerantz WC, Fischer M, Rankovic Z, Savic V. Koravovic M, et al. Among authors: fischer m. Eur J Med Chem. 2023 May 5;251:115246. doi: 10.1016/j.ejmech.2023.115246. Epub 2023 Mar 4. Eur J Med Chem. 2023. PMID: 36898329 Free PMC article.
Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators.
Nishiguchi G, Keramatnia F, Min J, Chang Y, Jonchere B, Das S, Actis M, Price J, Chepyala D, Young B, McGowan K, Slavish PJ, Mayasundari A, Jarusiewicz JA, Yang L, Li Y, Fu X, Garrett SH, Papizan JB, Kodali K, Peng J, Pruett Miller SM, Roussel MF, Mullighan C, Fischer M, Rankovic Z. Nishiguchi G, et al. Among authors: fischer m. J Med Chem. 2021 Jun 10;64(11):7296-7311. doi: 10.1021/acs.jmedchem.0c01313. Epub 2021 May 27. J Med Chem. 2021. PMID: 34042448 Free PMC article.
Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia.
Chang Y, Min J, Jarusiewicz JA, Actis M, Yu-Chen Bradford S, Mayasundari A, Yang L, Chepyala D, Alcock LJ, Roberts KG, Nithianantham S, Maxwell D, Rowland L, Larsen R, Seth A, Goto H, Imamura T, Akahane K, Hansen BS, Pruett-Miller SM, Paietta EM, Litzow MR, Qu C, Yang JJ, Fischer M, Rankovic Z, Mullighan CG. Chang Y, et al. Among authors: fischer m. Blood. 2021 Dec 9;138(23):2313-2326. doi: 10.1182/blood.2020006846. Blood. 2021. PMID: 34110416 Free PMC article.
New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.
Zahid H, Buchholz CR, Singh M, Ciccone MF, Chan A, Nithianantham S, Shi K, Aihara H, Fischer M, Schönbrunn E, Dos Santos CO, Landry JW, Pomerantz WCK. Zahid H, et al. Among authors: fischer m. J Med Chem. 2021 Sep 23;64(18):13902-13917. doi: 10.1021/acs.jmedchem.1c01294. Epub 2021 Sep 13. J Med Chem. 2021. PMID: 34515477 Free PMC article.
Phenyl-Glutarimides: Alternative Cereblon Binders for the Design of PROTACs.
Min J, Mayasundari A, Keramatnia F, Jonchere B, Yang SW, Jarusiewicz J, Actis M, Das S, Young B, Slavish J, Yang L, Li Y, Fu X, Garrett SH, Yun MK, Li Z, Nithianantham S, Chai S, Chen T, Shelat A, Lee RE, Nishiguchi G, White SW, Roussel MF, Potts PR, Fischer M, Rankovic Z. Min J, et al. Among authors: fischer m. Angew Chem Int Ed Engl. 2021 Dec 13;60(51):26663-26670. doi: 10.1002/anie.202108848. Epub 2021 Nov 16. Angew Chem Int Ed Engl. 2021. PMID: 34614283 Free PMC article.
Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.
Alcock LJ, Chang Y, Jarusiewicz JA, Actis M, Nithianantham S, Mayasundari A, Min J, Maxwell D, Hunt J, Smart B, Yang JJ, Nishiguchi G, Fischer M, Mullighan CG, Rankovic Z. Alcock LJ, et al. Among authors: fischer m. ACS Med Chem Lett. 2022 Feb 21;13(3):475-482. doi: 10.1021/acsmedchemlett.1c00650. eCollection 2022 Mar 10. ACS Med Chem Lett. 2022. PMID: 35300081 Free PMC article.
Water Networks Repopulate Protein-Ligand Interfaces with Temperature.
Stachowski TR, Vanarotti M, Seetharaman J, Lopez K, Fischer M. Stachowski TR, et al. Among authors: fischer m. Angew Chem Int Ed Engl. 2022 Aug 1;61(31):e202112919. doi: 10.1002/anie.202112919. Epub 2022 Jun 21. Angew Chem Int Ed Engl. 2022. PMID: 35648650 Free PMC article.
6,085 results