SOR-C13 is a High-Affinity TRPV6 Antagonist for Advanced Solid Tumors Research
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 calcium ions. The major function of TRPV5/6 is larger-scale calcium homeostasis. Besides, Mice with TRPV6 knock-outs exhibit defective intestinal...
EM127 is a SMYD3 Covalent Inhibitor
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 H4 (Histone H4 Lysine 5, VEGFR1 receptor, AKT1, HER2, and MAP3K2 protein. Importantly, SMYD3 plays a role in transcriptional...
Apitolisib is an Orally Active Class I PI3K and mTORC1/2 Inhibitor
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), and human epithelial growth factor receptor 2 (HER2) stimulate proliferation, growth, and survival by activating mTOR kinase. The mTOR...
Infigratinib (BGJ-398) is an Orally Active FGFR Inhibitor
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 as high-affinity receptors for the fibroblast growth factors (FGFs) that control cell proliferation, apoptosis, and differentiation and are involved...
Inupadenant is an Orally Active and Highly Selective A2A Receptor Antagonist
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, A1, A2A, A2B, and A3. They are activated by extracellular adenosine and play a central role in a wide...
SG3199, an ADC Cytotoxin, is a Cytotoxic DNA Minor Groove Interstrand Crosslinking PDB Dimer
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 are a class of exquisitely potent DNA minor groove interstrand crosslinking agents. An important feature of the interstrand cross-links...
Venadaparib (IDX-1197) is a Potent and Selective PARP Inhibitor
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 different structures and functions in the cell. Importantly, the main role is to detect and signal single-strand DNA breaks...