Introduction The anti-apoptotic BCL-2 family proteins, such as BCL-2, BCL-XL, and MCL-1,
are excellent cancer therapeutic targets. The FDA approval of BCL-2 selective inhibitor …

Precision oncology benefits from effective early phase drug discovery decisions. Recently,
drugging inactive protein conformations has shown impressive successes, raising the …

Cancer is a major threat to human life around the globe, and the discovery of novel
biomolecules continue to be an urgent therapeutic need that is still unmet. Precision …

Abstract Poly (ADP-ribose) polymerase (PARP) inhibitors show potent antiproliferative
activity in treatment with triple-negative breast cancer (TNBC) when combined with …

Overexpression of BCL-xL and BCL-2 play key roles in tumorigenesis and cancer drug
resistance. Advances in PROTAC technology facilitated recent development of the first BCL …

SKP2 (S-phase kinase-associated protein 2) is a member of the F-box family of substrate-
recognition subunits in the SCF ubiquitin-protein ligase complexes. It is associated with …

Small molecule induced protein degradation has created tremendous excitement in drug
discovery within recent years. Not being confined to target inhibition and being able to …

VEGFR-2 is an attractive therapeutic target for antitumor drug research by blocking tumor
angiogenesis and PROTAC provides a new technology for targeted protein knockout …

Protease-targeted chimeras (PROTACs) have been employed as a novel therapeutic
approach, utilizing the ubiquitin-proteasome system for targeted protein degradation …

Post-translational modifications, such as ubiquitylation, need to be tightly controlled to
guarantee the accurate localization and activity of proteins. Ubiquitylation is a dynamic …