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…
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…
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.…
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…
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…
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 d4. Firstly,…
Glycogen synthase kinase 3 (GSK3) is a key regulatory kinase in the WNT pathway. GSK3 remains a therapeutic target of interest in many diseases. GSK3 represents an example of such…
ATP6V1G, a subunit of the vacuolar H+-ATPase (v-ATPase). In this article, we will introduce a potent ATP6V1G inhibitor, Verucopeptin. Firstly, in vitro. Verucopeptin shows excellent antitumor activity against K562R cells,…
Mutant EGFRs are one of the major drivers of non-small-cell lung cancer (NSCLC). While reversible first-generation EGFR inhibitors are initially an effective treatment. However, a drug-resistant gatekeeper T790M mutation accounts…
NUT midline carcinoma (NMC) is a rare, aggressive subtype of squamous carcinoma. This kind of cancer is usually driven by BRD4-NUT fusion oncoprotein. BRD4, a BET protein, binds to chromatin…