Scientists find a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor epacadostat through a series of SAR studies. It primarily focused on improving the PK by reducing the rate of…
Tumor-induced angiogenesis, or the formation of new capillary networks between neoplastic cells and endothelial cells of the host, is required for solid tumor growth and metastases. In addition, the Vascular…
On December 1, 2022, FDA approved Rezlidhea (Olutasidenib) to treat adults with relapsed or refractory acute myeloid leukemia (AML) with a susceptible (IDH1) mutation. Olutasidenib (FT2102) is a highly potent,…
The Vanilloid group (TRPV) contains six members, from TRPV1 to TRPV6. TRPV5 and TRPV6 exhibit lower sequence identity to V1-V4, and different properties. Additionally, TRPV5 or TRPV6 is selective for…
SMYD3 is a methyltransferase (MTase) catalyzing the methylation of specific lysine residues. Notably, it induces cell proliferation and regulates gene expression, including histones H3 (Histone H3 Lysine 4, H3K4) and…
Activation of the pathway occurs following activating point mutations or amplification of the PIK3CA gene encoding the p110a PI3K isoform. Oncogenes such as PI3K, AKT, epidermal growth factor receptor (EGFR),…
The fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases (RTKs) comprises four members (FGFR1, FGFR2, FGFR3, and FGFR4) that share significant sequence homology. This family of RTKs serves…
Adenosine receptors (AR), including P1 purinergic receptors, belong to G protein-coupled receptors (GPCR). Specifically, Adenosine is an autogenous acid in all tissues and body fluids. Besides, AR contains four subtypes,…
The pyrrolobenzodiazepines (PBD) are a class of compound that may have antibiotic or anti-tumor properties. They exert their biological activity by binding in the minor groove of DNA. PBD dimers…
PARP is an enzyme that involved in a number of cellular processes such as DNA repair, and programmed cell death. The PARP family comprises 17 members. They have all very…