This led to the belief that covalent inhibitors were not ideal drug candidates resulting in limited development by the pharmaceutical industry. However, covalent drugs have experienced a remarkable ...

Investigators at The Scripps Research Institute and Rensselaer Polytechnic Institute have designed novel covalent inhibitors of SARS-CoV-2 papain-like protease (PLpro) and assessed their drug ...

(A) Major difference between bio TCI (lower) vs. conventional TCI (upper). (B) Our achievements on bio TCI research. Disclaimer: AAAS and EurekAlert! are not responsible for the accuracy of news ...

Aclaris Therapeutics (ACRS) announced the availability of a new publication describing properties of Aclaris Therapeutics’ ATI-2138, a novel ...

2009; Agashe et al., 2022). The publication, entitled “Characterization of the dual ITK/JAK3 small molecule covalent inhibitor ATI-2138,” describes in vitro and in vivo assessments and the clinical ...

KRAS is one of the most frequently mutated oncogenes in human cancer. Despite more than three decades of research, indirect approaches targeting KRAS-mutant cancers have largely failed to show ...

Pirtobrutinib (Jaypirca) is a type of targeted therapy called a non-covalent (reversible) Bruton’s tyrosine kinase (BTK) inhibitor. BTK is an enzyme that helps certain cancer cells grow and survive.

Median progression-free survival (PFS) reached 14 months with pirtobrutinib, an oral non-covalent BTK inhibitor, as compared with 8.7 months with investigator's choice of idelalisib (Zydelig ...

Through a structure-based drug-design approach, we have discovered a selective and potent BTK/MNK dual kinase inhibitor (QL-X-138), which exhibits covalent binding to BTK and noncovalent binding ...

During a Case-Based Roundtable® event, Nitin Jain, MD, and participants discussed treating a patient with CLL after ...