1624262-44-7Relevant academic research and scientific papers
Targeting the Gatekeeper MET146 of C-Jun N-Terminal Kinase 3 Induces a Bivalent Halogen/Chalcogen Bond
Lange, Andreas,Günther, Marcel,Büttner, Felix Michael,Zimmermann, Markus O.,Heidrich, Johannes,Hennig, Susanne,Zahn, Stefan,Schall, Christoph,Sievers-Engler, Adrian,Ansideri, Francesco,Koch, Pierre,Laemmerhofer, Michael,Stehle, Thilo,Laufer, Stefan A.,Boeckler, Frank M.
, p. 14640 - 14652 (2015)
We target the gatekeeper MET146 of c-Jun N-terminal kinase 3 (JNK3) to exemplify the applicability of X···S halogen bonds in molecular design using computational, synthetic, structural and biophysical techniques. In a designed series of aminopyrimidine-ba
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma
Jiang, Baishan,Jiang, Jie,Kaltheuner, Ines H.,Iniguez, Amanda Balboni,Anand, Kanchan,Ferguson, Fleur M.,Ficarro, Scott B.,Seong, Bo Kyung Alex,Greifenberg, Ann Katrin,Dust, Sofia,Kwiatkowski, Nicholas P.,Marto, Jarrod A.,Stegmaier, Kimberly,Zhang, Tinghu,Geyer, Matthias,Gray, Nathanael S.
, (2021)
Development of inhibitors targeting CDK12/13 is of increasing interest as a potential therapy for cancers as these compounds inhibit transcription of DNA damage response (DDR) genes. We previously described THZ531, a covalent inhibitor with selectivity fo
INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)
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, (2018/02/28)
The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
