CGP77675 is an Orally Active Inhibitor of Src Family Kinases
Src kinase family is a nonreceptor tyrosine kinase family. It includs 9 members: SRC, yes, Fyn and FGR, Lck, HCK, BLK, and Lyn. Specifically, Src family kinases interact with many…
Src kinase family is a nonreceptor tyrosine kinase family. It includs 9 members: SRC, yes, Fyn and FGR, Lck, HCK, BLK, and Lyn. Specifically, Src family kinases interact with many…
The activation of FMS like receptor tyrosine kinase 3 (FLT3) is a cytokine receptor that belongs to the receptor tyrosine kinase class III. Specifically, FLT3 signaling is important for the…
The MYC family of oncogenes (MYC, MYCN, and MYCL), encodes basic helix-loop-helix leucine zipper (bHLHZip) transcription factors. Through the HLHZip domain, MYC heterodimerizes with the bHLHZip protein MAX, which enables…
Prostate cancer drugs targeting the androgen receptor (AR) are mainly competitive ligand-binding domain (LBD) binding antagonists. A common mechanism of drug resistance can inactivate it. Specifically, AR is a nuclear…
SHP2 is a non-receptor ubiquitous protein tyrosine phosphatase and has a relatively conserved structure and function. The SHP2 includes the PTP domain, two SH2 domains, and a C-terminal tail containing…
PARP is a family of proteins involved in a number of cellular processes involving mainly DNA repair and programmed cell death. The PARP family comprises 17 members. PARP1, PARP2 (inhibitor…
Prostate cancer is among the most common malignancy in males. Among the various PI3K isoforms, PTEN-loss-induced prostate cancer in the genetically engineered Pten conditional knockout mouse model predominantly activates the…
Multiple myeloma represents a heterogeneous disease with various oncogenic mutations, chromosomal translocations, and copy number variations. The mitotic kinase T-LAK cell‐originated protein kinase/PDZ‐binding kinase ( TOPK/PBK) associates with the proliferation…
Mixed lineage leukemia (MLL) is a very aggressive blood cancer that predominantly occurs in pediatric patients. Especially, MLL is acute leukemia with poor prognosis. Spontaneous translocations at the MLL1 gene…
In this article, we will introduce a potent, selective, and well-tolerated eIF4A inhibitor, Zotatifin. It promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM). Zotatifin…