Views provided by UsageCountsProbing BRD Inhibition Substituent Effects in Bulky Analogues of (+)‐JQ1
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Hassell‐Hart, Storm; Picaud, Sarah; Lengacher, Raphael; Csucker, Joshua; Millet, Regis; Gasser, Gilles; Alberto, Roger; +8 Authors
Hassell‐Hart, Storm; Picaud, Sarah; Lengacher, Raphael; Csucker, Joshua; Millet, Regis; Gasser, Gilles; Alberto, Roger; Maple, Hannah; Felix, Robert; Leśnikowski, Zbigniew J; Stewart, Helen J S; Chevassut, Timothy J; Morley, Simon; Filippakopoulos, Panagis; Spencer, John;
Probing BRD Inhibition Substituent Effects in Bulky Analogues of (+)‐JQ1
AbstractA series of bulky organometallic and organic analogues of the bromodomain (BRD) inhibitor (+)‐JQ1 have been prepared. The most potent, N‐[(adamantan‐1‐yl)methyl]‐2‐[(9S)‐7‐(4‐chlorophenyl)‐4,5,13‐trimethyl‐3‐thia‐1,8,11,12‐tetraazatricyclo[8.3.0.02,6]trideca‐2(6),4,7,10,12‐pentaen‐9‐yl]acetamide, 2e, showed excellent potency with an KD=ca. 130 nm vs. BRD4(1) and a ca. 2‐fold selectivity over BRD4(2) (KD=ca. 260 nm). Its binding to the first bromodomain of BRD4 was determined by a protein cocrystal structure.
France, France, Switzerland, France
- University of Zurich Switzerland
- University of Bern Switzerland
- Centre Hospitalier Universitaire de Bordeaux France
- THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD United Kingdom
- Polish Academy of Learning Poland
10120 Department of Chemistry, 1303 Biochemistry, Benzodiazepine, Bioorganic chemistry, 1503 Catalysis, 1604 Inorganic Chemistry, 3002 Drug Discovery, [CHIM.THER] Chemical Sciences/Medicinal Chemistry, Organic Chemistry, epigenetics; cancer; benzodiazepines; bromodomain; bioinorganic chemistry; bioorganometallic chemistry, Biochemistry, Catalysis, Inorganic Chemistry, FOS: Chemical sciences, Drug Discovery, 540 Chemistry, Physical and Theoretical Chemistry, 1606 Physical and Theoretical Chemistry, 1605 Organic Chemistry, Cancer
10120 Department of Chemistry, 1303 Biochemistry, Benzodiazepine, Bioorganic chemistry, 1503 Catalysis, 1604 Inorganic Chemistry, 3002 Drug Discovery, [CHIM.THER] Chemical Sciences/Medicinal Chemistry, Organic Chemistry, epigenetics; cancer; benzodiazepines; bromodomain; bioinorganic chemistry; bioorganometallic chemistry, Biochemistry, Catalysis, Inorganic Chemistry, FOS: Chemical sciences, Drug Discovery, 540 Chemistry, Physical and Theoretical Chemistry, 1606 Physical and Theoretical Chemistry, 1605 Organic Chemistry, Cancer
selected citations These citations are derived from selected sources.This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).1 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Average influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Average impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Average views 18 - 18views
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This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
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This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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