Brian K Albrecht
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Explore the profile of Brian K Albrecht including associated specialties, affiliations and a list of published articles.
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41
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1184
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Recent Articles
1.
Taylor A, Bailey C, Belmont L, Campbell R, Cantone N, Cote A, et al.
J Med Chem
. 2022 Aug;
65(16):11177-11186.
PMID: 35930799
Bromodomains are acetyllysine recognition domains present in a variety of human proteins. Bromodomains also bind small molecules that compete with acetyllysine, and therefore bromodomains have been targets for drug discovery...
2.
Gehling V, McGrath J, Duplessis M, Khanna A, Brucelle F, Vaswani R, et al.
ACS Med Chem Lett
. 2020 Jun;
11(6):1213-1220.
PMID: 32551003
Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label...
3.
Wang S, Tsui V, Crawford T, Audia J, Burdick D, Beresini M, et al.
J Med Chem
. 2018 Oct;
61(20):9301-9315.
PMID: 30289257
The biological functions of the dual bromodomains of human transcription-initiation-factor TFIID subunit 1 (TAF1(1,2)) remain unknown, although TAF1 has been identified as a potential target for oncology research. Here, we...
4.
Romero F, Murray J, Lai K, Tsui V, Albrecht B, An L, et al.
J Med Chem
. 2017 Sep;
60(22):9162-9183.
PMID: 28892380
Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. We recently disclosed in vivo chemical tool 1 (GNE-272) for the bromodomain...
5.
Crawford T, Audia J, Bellon S, Burdick D, Bommi-Reddy A, Cote A, et al.
ACS Med Chem Lett
. 2017 Jul;
8(7):737-741.
PMID: 28740608
The biological function of bromodomains, epigenetic readers of acetylated lysine residues, remains largely unknown. Herein we report our efforts to discover a potent and selective inhibitor of the bromodomain of...
6.
Crawford T, Vartanian S, Cote A, Bellon S, Duplessis M, Flynn E, et al.
Bioorg Med Chem Lett
. 2017 Jun;
27(15):3534-3541.
PMID: 28606761
Bromodomain-containing protein 9 (BRD9), an epigenetic "reader" of acetylated lysines on post-translationally modified histone proteins, is upregulated in multiple cancer cell lines. To assess the functional role of BRD9 in...
7.
Vaswani R, Gehling V, Dakin L, Cook A, Nasveschuk C, Duplessis M, et al.
J Med Chem
. 2016 Oct;
59(21):9928-9941.
PMID: 27739677
Polycomb repressive complex 2 (PRC2) has been shown to play a major role in transcriptional silencing in part by installing methylation marks on lysine 27 of histone 3. Dysregulation of...
8.
Crawford T, Romero F, Lai K, Tsui V, Taylor A, De Leon Boenig G, et al.
J Med Chem
. 2016 Sep;
59(23):10549-10563.
PMID: 27682507
The single bromodomain of the closely related transcriptional regulators CBP/EP300 is a target of much recent interest in cancer and immune system regulation. A co-crystal structure of a ligand-efficient screening...
9.
Chen K, Campfield B, Wenzel S, McAleer J, Kreindler J, Kurland G, et al.
JCI Insight
. 2016 Aug;
1(11).
PMID: 27517095
Significant morbidity in cystic fibrosis (CF) results from chronic lung inflammation, most commonly due to infection. Recent data suggest that IL-17 contributes to pathological inflammation in the setting of abnormal...
10.
Gehling V, Bellon S, Harmange J, LeBlanc Y, Poy F, Odate S, et al.
Bioorg Med Chem Lett
. 2016 Aug;
26(17):4350-4.
PMID: 27476424
This communication describes the identification and optimization of a series of pan-KDM5 inhibitors derived from compound 1, a hit initially identified against KDM4C. Compound 1 was optimized to afford compound...