APS6-45, an Orally Active Tumor-Calibrated Inhibitor, Inhibits RAS/MAPK Signaling

Medullary thyroid cancer is a form of thyroid carcinoma which originates from the parafollicular cells, which produce the hormone calcitonin. Synthetic tailoring of approved drugs for new indications is often difficult, as the most appropriate targets may not be readily apparent and therefore few roadmaps exist to guide chemistry....

MSAB is a Selective Inhibitor of Wnt/β-Catenin Signaling

Wnt/β-catenin signaling regulates key cellular functions including proliferation, differentiation, migration, apoptosis, and stem cell renewal. The β-catenin is a core component of the cadherin protein complex, whose stabilization is essential for the activation of Wnt/β-catenin signaling. In this study, researchers screen for small molecule compounds that act against Wnt/β-catenin...

BSJ-03-204 is a Selective Palbociclib-Based CDK4/6 Dual Degrader (PROTAC)

The chimeric proteolytic enzyme (PROTAC) is a heterobifunctional small molecule. Specifically, it is composed of two active domains and an adaptor that can remove specific proteins that are not needed. Besides, PROTAC does not act as a conventional enzyme inhibitor, but by inducing selective intracellular proteolysis. Moreover, PROTAC includes...

BC-LI-0186 is a Selective Inhibitor of LeuRS and RagD Interaction

BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). It competitively binds to the RagD interacting site of LRS (Kd=42.1 nM). At the same time, it has effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation, or the...

BSJ-04-132 is a Selective Ribociclib-Based CDK4 Degrader (PROTAC)

Targeted protein degradation induced by PROTAC has become a new therapeutic strategy in drug development. Besides, PROTAC has two covalently linked protein binding molecules. One can bind E3 ubiquitin ligases and the other can bind to the target protein to be degraded. Moreover, the recruitment of E3 ligase to...

Telomestatin, a Potent Telomerase Inhibitor, Facilitates the Formation of Intramolecular G-quadruplexes

Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. It selectively facilitates the formation of intramolecular G-quadruplexes, in particular, that produced from the human telomeric sequence d[T2AG3]4. Firstly, in vitro, Telomestatin promotes or stabilizes the formation of the intramolecular G-quadruplex. When the DNA concentrations are at 0.005...