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Page 1
Acetylation reprograms MITF target selectivity and residence time.
Louphrasitthiphol P, Loffreda A, Pogenberg V, Picaud S, Schepsky A, Friedrichsen H, Zeng Z, Lashgari A, Thomas B, Patton EE, Wilmanns M, Filippakopoulos P, Lambert JP, Steingrímsson E, Mazza D, Goding CR. Louphrasitthiphol P, et al. Nat Commun. 2023 Sep 28;14(1):6051. doi: 10.1038/s41467-023-41793-7. Nat Commun. 2023. PMID: 37770430 Free PMC article.
Discovery of Benzo[d]imidazole-6-sulfonamides as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain.
Cipriano A, Milite C, Feoli A, Viviano M, Pepe G, Campiglia P, Sarno G, Picaud S, Imaide S, Makukhin N, Filippakopoulos P, Ciulli A, Castellano S, Sbardella G. Cipriano A, et al. ChemMedChem. 2022 Oct 19;17(20):e202200343. doi: 10.1002/cmdc.202200343. Epub 2022 Sep 15. ChemMedChem. 2022. PMID: 36040095 Free PMC article.
The structure of nontypeable Haemophilus influenzae SapA in a closed conformation reveals a constricted ligand-binding cavity and a novel RNA binding motif.
Lukacik P, Owen CD, Harris G, Bolla JR, Picaud S, Alibay I, Nettleship JE, Bird LE, Owens RJ, Biggin PC, Filippakopoulos P, Robinson CV, Walsh MA. Lukacik P, et al. PLoS One. 2021 Oct 15;16(10):e0256070. doi: 10.1371/journal.pone.0256070. eCollection 2021. PLoS One. 2021. PMID: 34653190 Free PMC article.
Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain.
Brand M, Clayton J, Moroglu M, Schiedel M, Picaud S, Bluck JP, Skwarska A, Bolland H, Chan AKN, Laurin CMC, Scorah AR, See L, Rooney TPC, Andrews KH, Fedorov O, Perell G, Kalra P, Vinh KB, Cortopassi WA, Heitel P, Christensen KE, Cooper RI, Paton RS, Pomerantz WCK, Biggin PC, Hammond EM, Filippakopoulos P, Conway SJ. Brand M, et al. J Med Chem. 2021 Jul 22;64(14):10102-10123. doi: 10.1021/acs.jmedchem.1c00348. Epub 2021 Jul 13. J Med Chem. 2021. PMID: 34255515 Free PMC article.
Allosteric Antagonist Modulation of TRPV2 by Piperlongumine Impairs Glioblastoma Progression.
Conde J, Pumroy RA, Baker C, Rodrigues T, Guerreiro A, Sousa BB, Marques MC, de Almeida BP, Lee S, Leites EP, Picard D, Samanta A, Vaz SH, Sieglitz F, Langini M, Remke M, Roque R, Weiss T, Weller M, Liu Y, Han S, Corzana F, Morais VA, Faria CC, Carvalho T, Filippakopoulos P, Snijder B, Barbosa-Morais NL, Moiseenkova-Bell VY, Bernardes GJL. Conde J, et al. ACS Cent Sci. 2021 May 26;7(5):868-881. doi: 10.1021/acscentsci.1c00070. Epub 2021 Apr 14. ACS Cent Sci. 2021. PMID: 34079902 Free PMC article.
34 results