Aliphatic three-and four-membered rings including cyclopropanes, cyclobutanes, oxetanes,
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …

Bruton's tyrosine kinase (BTK), a cytoplasmic tyrosine kinase, plays a central role in
immunity and is considered an attractive target for treating autoimmune diseases. The use of …

Glioma is one of the most common types of brain tumors, and its high recurrence and
mortality rates threaten human health. In 2008, the frequent isocitrate dehydrogenase 1 …

KRAS regulates many cellular processes including proliferation, survival, and differentiation.
Point mutants of KRAS have long been known to be molecular drivers of cancer. KRAS p …

A comprehensive understanding of structure–reactivity relationships is critical to the design
and optimization of cysteine-targeted covalent inhibitors. Herein, we report glutathione …

Monoacylglycerol lipase (MAGL) is the main enzyme responsible for degradation of the
endocannabinoid 2-arachidonoylglycerol (2-AG) in the CNS. MAGL catalyzes the …

RAS protein plays a key role in cellular proliferation and differentiation. RAS gene mutation
is a known driver of oncogenic alternation in human cancer. RAS inhibition is an effective …

Covalent drug discovery has undergone a resurgence in recent years due to comprehensive
optimization of the structure–activity relationship (SAR) and the structure–reactivity …

Isocitrate dehydrogenases 1 and 2 (IDH1/2) are homodimeric enzymes that catalyze the
conversion of isocitrate to α-ketoglutarate (α-KG) in the tricarboxylic acid cycle. However …

Telomerase is a ribonuceloprotein complex responsible for maintaining telomeres and
protecting chromosomal integrity. The human telomerase reverse transcriptase (hTERT) is …