Within druggable target space, new small-molecule modalities, particularly covalent
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …

Transcriptional deregulation has emerged as a hallmark of several cancer types. In
metastatic castration-resistant prostate cancer, a stage in which systemic androgen …

Covalent protein kinase inhibitors exploit currently noncatalytic cysteines in the adenosine
5′-triphosphate (ATP)-binding site via electrophiles directly appended to a reversible …

Selective degradation of the cyclin-dependent kinases 12 and 13 (CDK12/13) presents a
novel therapeutic opportunity for triple-negative breast cancer (TNBC), but there is still a lack …

In the wake of the development of the concept of cell cycle and its limiting points, cyclin-
dependent kinases (CDKs) are considered to play a central role in regulating cell cycle …

CDK12 is a cyclin-dependent kinase that plays critical roles in DNA replication, transcription,
mRNA splicing, and DNA damage repair. CDK12 genomic changes, including mutation …

Over 20 years after the approval of the first-in-class protein kinase inhibitor imatinib, the
biological function of a significant fraction of the human kinome remains poorly understood …

The cyclin-dependent kinase CDK12 has garnered interest as a cancer therapeutic target as
DNA damage response genes are particularly suppressed by loss of CDK12 activity. In this …

The ERK pathway is one of the most important signaling cascades involved in
tumorigenesis. So far, eight noncovalent inhibitors of RAF and MEK kinases in the ERK …

Abstract Cyclin-dependent kinase 12 (CDK12), a transcription-related cyclin dependent
kinase (CDK), plays a momentous part in multitudinous biological functions, such as …