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 ...

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 ...

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 ...

(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 ...

Unique Pharmacological Profile: In biochemical and cellular assays, ATI-2138 demonstrated a similar high potency for inhibiting both ITK and JAK3, compared to ritlecitinib which was markedly less ...

Our work encompasses a broad range of molecular mechanisms of action, spanning covalent inhibitors, allosteric inhibitors, enzyme activators, protein (or protein complex) stabilizers, and protein ...

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 ...

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

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 ...