Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

Cysteine is one of the least abundant amino acids in proteins of many organisms, which
plays a crucial role in catalysis, signal transduction, and redox regulation of gene …

Small molecule drugs that covalently bind irreversibly to their target proteins have several
advantages over conventional reversible inhibitors. They include increased duration of …

This perspective discusses the role of pregnane xenobiotic receptor (PXR) in drug discovery
and the impact of its activation on CYP3A4 induction. The use of structural biology to reduce …

We report herein the design, synthesis, and pharmacological characterization of a library of
novel aryl pyrazol-1-yl-propanamides as selective androgen receptor degraders (SARDs) …

We report bisguanidinium-catalyzed enantioconvergent halogenophilic substitution
reactions (SN2X) that lead to the formation of C (sp3)–O bonds using racemic tertiary …

A catalytic enantioselective synthesis of bicalutamide derivatives with promising potentials in
prostate cancer treatment has been disclosed. The key intermediates, α-hydroxy-β-keto …

Inspired by the chemical reactivity of apalutamide, we have developed an efficient method
for N-terminal cysteine bioconjugation with 2-cyanopyridine derivatives. Systematic …

A novel multicomponent chemoenzymatic strategy for the preparation of enantioenriched β-
acyloxy thioethers has been developed. This robust methodology employs mild bases, air …

Androgen signaling pathway plays an important role in the occurrence and development of
prostate cancer (PCa), and anti-androgen drugs are one of the most effective therapies for …