Publication: Probing BRD Inhibition Substituent Effects in Bulky Analogues of (+)‐JQ1
Probing BRD Inhibition Substituent Effects in Bulky Analogues of (+)‐JQ1
Date
Date
Date
2021
Journal Article
Published version
Citations
...
Abstract
Abstract
Abstract
A 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.
Additional indexing
Creators (Authors)
- Hassell‐Hart, Storm
- Picaud, Sarah
- Lengacher, Raphael
- Csucker, Joshua
- Millet, Regis
- Gasser, Gilles
- Maple, Hannah
- Felix, Robert
- Leśnikowski, Zbigniew J
- Stewart, Helen J S
- Chevassut, Timothy J
- Morley, Simon
- Filippakopoulos, Panagis
- Spencer, John
Volume
Volume
Volume
104
Number
Number
Number
3
Page range/Item number
Page range/Item number
Page range/Item number
e2000214
Item Type
Item Type
Item Type
Journal Article
In collections
Dewey Decimal Classifikation
Dewey Decimal Classifikation
Dewey Decimal Classifikation
Keywords
Physical and Theoretical Chemistry, Inorganic Chemistry, Organic Chemistry, Biochemistry, Drug Discovery, Catalysis
Language
Language
Language
English
Publication date
Publication date
Publication date
2021-03-01
Date available
Date available
Date available
2021-05-18
ISSN or e-ISSN
ISSN or e-ISSN
ISSN or e-ISSN
0018-019X
OA Status
OA Status
OA Status
Green
Publisher DOI
Citations
...
Green Open Access
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