期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (5)
CXC chemokine receptors 1 (CXCR1) and 2 (CXCR2) have been demonstrated to have critical roles in cancer metastasis. Because they share high homology s......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (5)
The abnormally high expression of glutathione transferases is closely associated with cancer incidence and drug resistance. By introducing a hydrophob......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (2)
In this study, a series of novel hydroxyamidine derivatives were identified as potent and selective IDO1 inhibitors by structure-based drug design. Am......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (6)
BH3 peptide analogues are generally believed to exhibit great potency as cancer therapeutics via targeting antiapoptotic Bcl-2 proteins. Here, we desc......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (5)
We identified nitazoxanide (NTZ) as a moderate STAT3 pathway inhibitor through immunoblot analysis and a cell-based IL-6/JAK/STAT3 pathway activation ......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (7)
Pregnane X receptor (PXR) that orchestrates the intricate network of xeno- and endobiotic metabolism is considered as a promising therapeutic target f......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (4)
Covalent kinase inhibitors are rapidly emerging as a class of therapeutics with clinical benefits. Herein we report a series of selective 2-aminopyrim......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (6)
The voltage-gated sodium channel Na(v)1.7 continues to be a high-profile target for the treatment of various pain afflictions due to its strong human ......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (7)
[F-18]AV-45 (florbetapir f18, Amyvid) is an FDA-approved PET imaging agent targeting A beta plaques in the brain for diagnosis of Alzheimer's disease ......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (6)
We report herein the discovery of quinazolindiones as potent and selective tankyrase inhibitors. Elucidation of the structure-activity relationship of......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (7)
DNA-encoded library (DEL) technology is a - powerful platform for hit identification in academia and the pharmaceutical industry. When conducting off-......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (5)
TRPM8 antagonists derived from its cognate ligand, (-)-menthol, are underrepresented. We determine the absolute stereochemistry of a well-known TRPM8 ......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (3)
A novel pyrazolone-based copper complex [CuL(phen)(CH3OH)] [CuL(phen)]center dot CH3CH2OH center dot CH3OH (P-FAH-Cu-phen) was synthesized and charact......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (3)
SIRT1, a member of the sirtuin family, catalyzes the deacetylation of proteins with the transformation of NAD(+) into nicotinamide and 2'-O-acetyl-ADP......
期刊： ACS MEDICINAL CHEMISTRY LETTERS, 2021; 12 (1)
Interleukin-1 receptor associated kinase 4 (IRAK4) is a promising therapeutic target for diffuse large B-cell lymphoma driven by MYD88 L265P mutant, a......
