203926-74-3Relevant articles and documents
Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-X
Zhang, Xuan,Zhang, Peiyi,Zheng, Guangrong,Thummuri, Dinesh,He, Yonghan,Liu, Xingui,Zhou, Daohong
, p. 14765 - 14768 (2019)
BCL-XL, an anti-apoptotic BCL-2 family protein, plays a key role in cancer cell survival. However, the potential of BCL-XL as an anti-cancer target has been hampered by the on-target platelet toxicity because platelets depend on BCL-XL to maintain their viability. Here we report the development of a PROTAC BCL-XL degrader, XZ424, which has increased selectivity for BCL-XL-dependent MOLT-4 cells over human platelets compared with conventional BCL-XL inhibitors. This proof-of-concept study demonstrates the potential of utilizing a PROTAC approach to achieve tissue selectivity.
THERAPEUTIC COMPOUNDS AND USES THEREOF
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Page/Page column 48; 58, (2019/07/17)
The present invention relates to compounds useful in the modulation of ion channel activity in cells. The invention also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.
PREPARING AN UNSATURATED CARBOXYLIC ACID SALT FROM AN ALKENE AND CARBON DIOXIDE USING A HETEROGENEOUS BASE
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Page/Page column 32; 33, (2016/01/26)
Process for preparing an α,β-ethylenically unsaturated carboxylic acid salt, comprising, reacting an alkene and carbon dioxide in the presence of a carboxylation catalyst to obtain a catalyst-coordinated carboxylated intermediate, treating the catalyst- c