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Page 1
Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors.
Zhang T, Kwiatkowski N, Olson CM, Dixon-Clarke SE, Abraham BJ, Greifenberg AK, Ficarro SB, Elkins JM, Liang Y, Hannett NM, Manz T, Hao M, Bartkowiak B, Greenleaf AL, Marto JA, Geyer M, Bullock AN, Young RA, Gray NS. Zhang T, et al. Nat Chem Biol. 2016 Oct;12(10):876-84. doi: 10.1038/nchembio.2166. Epub 2016 Aug 29. Nat Chem Biol. 2016. PMID: 27571479 Free PMC article.
Recent Progress in Histone Demethylase Inhibitors.
McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ. McAllister TE, et al. J Med Chem. 2016 Feb 25;59(4):1308-29. doi: 10.1021/acs.jmedchem.5b01758. Epub 2016 Feb 2. J Med Chem. 2016. PMID: 26710088 Review.
Development of a chemical probe against NUDT15.
Zhang SM, Desroses M, Hagenkort A, Valerie NCK, Rehling D, Carter M, Wallner O, Koolmeister T, Throup A, Jemth AS, Almlöf I, Loseva O, Lundbäck T, Axelsson H, Regmi S, Sarno A, Krämer A, Pudelko L, Bräutigam L, Rasti A, Göttmann M, Wiita E, Kutzner J, Schaller T, Kalderén C, Cázares-Körner A, Page BDG, Krimpenfort R, Eshtad S, Altun M, Rudd SG, Knapp S, Scobie M, Homan EJ, Berglund UW, Stenmark P, Helleday T. Zhang SM, et al. Nat Chem Biol. 2020 Oct;16(10):1120-1128. doi: 10.1038/s41589-020-0592-z. Epub 2020 Jul 20. Nat Chem Biol. 2020. PMID: 32690945 Free PMC article.
The structural basis of fatty acid elongation by the ELOVL elongases.
Nie L, Pascoa TC, Pike ACW, Bushell SR, Quigley A, Ruda GF, Chu A, Cole V, Speedman D, Moreira T, Shrestha L, Mukhopadhyay SMM, Burgess-Brown NA, Love JD, Brennan PE, Carpenter EP. Nie L, et al. Nat Struct Mol Biol. 2021 Jun;28(6):512-520. doi: 10.1038/s41594-021-00605-6. Epub 2021 Jun 10. Nat Struct Mol Biol. 2021. PMID: 34117479 Free PMC article.
Open access chemical probes for epigenetic targets.
Brown PJ, Müller S. Brown PJ, et al. Future Med Chem. 2015;7(14):1901-17. doi: 10.4155/fmc.15.127. Epub 2015 Sep 23. Future Med Chem. 2015. PMID: 26397018 Free PMC article. Review.
Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times.
Heroven C, Georgi V, Ganotra GK, Brennan P, Wolfreys F, Wade RC, Fernández-Montalván AE, Chaikuad A, Knapp S. Heroven C, et al. Angew Chem Int Ed Engl. 2018 Jun 11;57(24):7220-7224. doi: 10.1002/anie.201801666. Epub 2018 May 9. Angew Chem Int Ed Engl. 2018. PMID: 29601130 Free PMC article.
35 results