The identification of molecular agents inhibiting specific functions in cancer cells
progression is considered as one of the most successful plans in cancer treatment. The …

Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

This review fully describes the coronavirus 3CL pro peptidomimetic inhibitors and
nonpeptidic small molecule inhibitors developed from 2010 to 2020. Specifically, the …

In contrast to the traditional mechanism of drug action that relies on the reversible,
noncovalent interaction of a ligand with its biological target, a targeted covalent inhibitor …

Despite significant improvements of new treatment options, cancer continues to represent as
one of the most common and fatal disease. The EGFR signaling pathway is considered as a …

Targeted covalent inhibition of disease-associated proteins has become a powerful
methodology in the field of drug discovery, leading to the approval of new therapeutics …

Additions of cysteine thiols to Michael acceptors underpin the mechanism of action of
several covalent drugs (eg, afatinib, osimertinib, ibrutinib, neratinib, and CC-292) …

We have recently reported on the use of aryl-fluorosulfates in designing water-and plasma-
stable agents that covalently target Lys, Tyr, or His residues in the BIR3 domain of the …

Covalent drugs provide pharmacodynamic and pharmacokinetic advantages over reversible
agents. However, covalent strategies have been developed mostly to target cysteine (Cys) …

The anti-apoptotic members of B-cell lymphoma-2 (Bcl-2) proteins family, such as Bcl-2 and
myeloid cell leukemia-1 (Mcl-1), are the key regulators of the intrinsic pathway of apoptosis …