Chen, Junjun published the artcileSelective and Cell-Active Inhibitors of the USP1/ UAF1 Deubiquitinase Complex Reverse Cisplatin Resistance in Non-small Cell Lung Cancer Cells, Related Products of indole-building-block, the publication is Chemistry & Biology (Cambridge, MA, United States) (2011), 18(11), 1390-1400, database is CAplus and MEDLINE.
Summary: Ubiquitin-specific proteases (USPs) have in recent years emerged as a promising therapeutic target class. We identified selective small-mol. inhibitors against a deubiquitinase complex, the human USP1/UAF1, through quant. high throughput screening (qHTS) of a collection of bioactive mols. The top inhibitors, pimozide and GW7647, inhibited USP1/UAF1 noncompetitively with a K i of 0.5 and 0.7 μM, resp., and displayed selectivity against a number of deubiquitinases, deSUMOylase, and cysteine proteases. The USP1/UAF1 inhibitors act synergistically with cisplatin in inhibiting cisplatin-resistant non-small cell lung cancer (NSCLC) cell proliferation. USP1/UAF1 represents a promising target for drug intervention because of its involvement in translesion synthesis and Fanconi anemia pathway important for normal DNA damage response. Our results support USP1/UAF1 as a potential therapeutic target and provide an example of targeting the USP/WD40 repeat protein complex for inhibitor discovery.
Chemistry & Biology (Cambridge, MA, United States) published new progress about 330161-87-0. 330161-87-0 belongs to indole-building-block, auxiliary class Protein Tyrosine Kinase/RTK,Src, name is SU6656, and the molecular formula is C19H21N3O3S, Related Products of indole-building-block.
Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles