Optimization of HJB97 for The Design of PROTAC Degraders of BET Proteins

The Bromodomain and Extra-Terminal Domain (BET) family of proteins comprises BRD2, BRD3, BRD4, and BRDT. The BET proteins are epigenetic readers and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer. The targeted degradation of BET proteins...

CF53, a Potent and Orally Active BET Inhibitor

Bromodomain and extra-terminal (BET) family is a well-known member of bromodomain family. Proteins of this family include BRD2, BRD3, BRD4 and a testis-specific protein, BRDT. BET proteins act as important epigenetic “readers” and play a vital role in regulating gene transcription. Thus, they are becoming hot targets for cancer...

A Novel and Efficacious RAF Inhibitor RAF709

The mitogen-activated protein kinase pathway regulates lots of multiple biological functions. In addition, RAF inhibitors activate the MAPK pathway. Interestingly, the MAPK pathway in turn induces the RAS proteins to exchange GDP for GTP. The RAF proteins are serine-threonine specific protein kinases. They activate the MEK/ERK cascade downstream of...

Action Mechanism of a Mcl-1 Inhibitor AZD5991

Apoptosis is a highly regulated program of cell death. Apoptosis occurs in multicellular organisms. Mcl-1 plays an important role in apoptosis. Mechanically, Mcl-1 promotes cell survival by preventing induction of apoptosis in many cancers. In addition, Mcl-1 is a member of the Bcl-2 family of proteins. In contrast to...

Alofanib, An Allosteric Inhibitor of FGFR2

FGF family participates in a variety of physiological processes in adult organism including regulation of angiogenesis. FGF acts via high affinity binding to specific receptors (FGFR) in various cells and stimulates cell proliferation, differentiation, and migration. Angiogenesis plays a pivotal role in the development of various physiological and pathological...

Role of PRMT7 Probe SGC3027 in Cancer

Protein arginine methyltransferases (PRMTs) transfer methyl groups to the arginine residues of histones and other proteins. Fistly, PRMTs add one or two mono-methyl groups to the guanidino nitrogen atoms of arginine residues. And secondly, PRMTs results in epigenetic modification of histones or changes of protein-protein interactions. Lastly, these interactions...

R916562, a Dual Axl/VEGF-R2 Inhibitor for Cancer Therapy

Axl tyrosine kinase is a putative driver of diverse cellular processes that are critical for the development, growth, and spread of tumors. It is a promising therapeutic target for cancer therapy. VEGFR2 is a primary responder to vascular endothelial growth factor signal, and thereby regulates endothelial migration and proliferation....