1381868-50-3

Upstream product

• 1381868-49-0 tert-butyl N-[1-({1-[(1-{[1-(1,3-benzothiazol-2-yl)-1-hydroxy-5-{3-[(4-methoxy-2,3,6trimethylbenzene)sulfonyl]carbamimidamido}penta-2-yl]carbamoyl}ethyl)carbamoyl]-3-[(triphenylmethyl)carbamoyl]propyl}carbamoyl)-4-{1-[(4-methoxy-2,3,6-trimethylbenzene)sulfonyl]carbamimidamido}butyl]carbamate 

Relevant academic research and scientific papers

Design and synthesis of potent, selective inhibitors of matriptase

Matriptase is a member of the type II transmembrane serine protease family. Several studies have reported deregulated matriptase expression in several types of epithelial cancers, suggesting that matriptase constitutes a potential target for cancer therapy. We report herein a new series of slow, tight-binding inhibitors of matriptase, which mimic the P1-P4 substrate recognition sequence of the enzyme. Preliminary structure-activity relationships indicate that this benzothiazole-containing RQAR-peptidomimetic is a very potent inhibitor and possesses a good selectivity for matriptase versus other serine proteases. A molecular model was generated to elucidate the key contacts between inhibitor 1 and matriptase.

MATRIPTASE INHIBITORS AND USES THEREOF AGAINST ORTHOMYXOVIRIDAE INFECTIONS

The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flu infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and preventing orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.