Current medicinal chemistry relies heavily on the quality of building blocks, ie reagents used
to introduce chemical diversity into the target molecules. The last decade witnessed an …

Covalent protein inhibitors have found considerable utility in medicinal chemistry and
chemical biology. Chemical probes and drugs have been rationally designed and fine-tuned …

To identify novel targets for acute myeloid leukemia (AML) therapy, we performed genome-
wide CRISPR-Cas9 screening using AML cell lines, followed by a second screen in vivo …

PF-06651600 was developed as an irreversible inhibitor of JAK3 with selectivity over the
other three JAK isoforms. A high level of selectivity toward JAK3 is achieved by the covalent …

Irreversible enzyme inhibitors and covalent chemical biology probes often utilize the
reaction of a protein cysteine residue with an appropriately positioned electrophile (eg …

Abstract Litsea cubeba (Lour.) Pers.(Lauraceae family) has been used as a folk prescription
in China for the treatment of rheumatic diseases for a long time. Previous studies of our …

Neurofibromatosis type 1, a genetic disorder caused by pathogenic germline variations in
NF1, predisposes individuals to the development of tumors, including cutaneous and …

Acute myeloid leukemia (AML) is a devastating disease, and clinical outcomes are still far
from satisfactory. Here, to identify novel targets for AML therapy, we performed a genome …

Identification of the specific protein target (s) of a drug is a critical step in unraveling its
mechanisms of action (MOA) in many natural products. Curcumol, isolated from well known …

Hepatic metastasis develops in∼ 50% of uveal melanoma (UM) patients with scarcely
effective treatment resulting in lethality. The underlying mechanism of liver metastasis …