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Selective inactivation of protein tyrosine phosphatase PTP1B by sulfone analogue of naphthoquinone
- Authors
- Ham, Seung Wook; Park, Junguk; Lee, Soo-Jin; Yoo, Ji Sang
- Issue Date
- Jan-1999
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- antitumour compds; enzyme inhibitors; kinetics; phosphorylaton
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.9, no.2, pp 185 - 186
- Pages
- 2
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 9
- Number
- 2
- Start Page
- 185
- End Page
- 186
- ISSN
- 0960-894X
1464-3405
- Abstract
- Protein tyrosine phosphatase inactivators are of interest as research tools and as therapeutic agents. In this study, the effect of sulfone analogue of naphthoquinone on the activities of PTP1B and other PTPs was examined. The results indicated that this compound selectively and irreversibly inactivated the PTP1B with the dissociation constant K-i of 3.5 mu M and the inactivation rate constant k(inact) of 2.2 x 10(-2) sec(-1). (C) 1999 Elsevier Science Ltd. All rights reserved.
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