title: Discovery of novel 2-hydroxydiarylamide derivatives as TMPRSS4 inhibitors.
abstract: TMPRSS4 is a novel type II transmembrane serine protease that has been implicated in the invasion and metastasis of colon cancer cells. In this study, a novel series of 2-hydroxydiarylamide derivatives were synthesized and evaluated for inhibiting TMPRSS4 serine protease activity and suppressing cancer cell invasion. These derivatives demonstrated good inhibitory activity against TMPRSS4 serine protease, which correlated with the promising anti-invasive activity of colon cancer cells overexpressing TMPRSS4.
authors: Biomedical Proteomics Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejon 305-806, Republic of Korea.
authors: Sunghyun
authors: S
authors: Kang
authors: Hye-Jin
authors: HJ
authors: Min
authors: Min-Seo
authors: MS
authors: Kang
authors: Myung-Geun
authors: MG
authors: Jung
authors: Semi
authors: S
authors: Kim
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000378:metabolism / Q000633:toxicity; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008565:Membrane Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011485:Protein Binding; D012697:Serine Endopeptidases / Q000378:metabolism; D015842:Serine Proteinase Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D008565:Membrane Proteins; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; C528837:TMPRSS4 protein, human