지원사업
학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
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연구자들이 자신의 연구와 전문성을 널리 알리고, 새로운 협력의 기회를 만들 수 있는 네트워킹 공간이에요.
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Protein tyrosine phosphatases (PTPs), along with protein kinases, mediate phosphorylation signaling in cells and are involved in cancers, diabetes, neural disorders, and immunological diseases. PTP sigma (PTPσ) is a receptor-type PTP with a C-terminal cytoplasmic region being responsible for its enzymatic activity. The inhibitors of the PTPσ catalytic activity promote neural cell growth and hematopoietic stem cell proliferation. In this study, we performed chemical library screening to identify a novel allosteric inhibitor PTPσ and characterized the inhibitor-enzyme interaction. Based on the analyses, we found a novel allosteric inhibitor that binds to a pocket between the two catalytic domains of the cytoplasmic region of PTPσ. Site directed mutagenesis studies identified residues involved in the inhibitor binding and enzyme kinetics experiments proved the allosteric mode of inhibition. The allosteric regulation site in the domain interface could be exploited to develop specific inhibitors for disease therapeutics.
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참고문헌 (23)
참고문헌 신청
Almo, S. C. / 2007 / Structural genomics of protein phosphatases / J Struct Funct Genomics 8:121~140
Alonso, A. / 2016 / The extended human PTPome : a growing tyrosine phosphatase family / FEBS J 283:1404~1429
Andersen, J. N. / 2001 / Structural and evolutionary relationships among protein tyrosine phosphatase domains / Mol Cell Biol 21:7117~7136
Barford, D. / 1994 / Crystal structure of human protein tyrosine phosphatase 1B / Science 263:1397~1404
Barr, A. J. / 2009 / Large-scale structural analysis of the classical human protein tyrosine phosphatome / Cell 136:352~363
Alonso, A. / 2016 / The extended human PTPome : a growing tyrosine phosphatase family / FEBS J 283:1404~1429
Andersen, J. N. / 2001 / Structural and evolutionary relationships among protein tyrosine phosphatase domains / Mol Cell Biol 21:7117~7136
Barford, D. / 1994 / Crystal structure of human protein tyrosine phosphatase 1B / Science 263:1397~1404
Barr, A. J. / 2009 / Large-scale structural analysis of the classical human protein tyrosine phosphatome / Cell 136:352~363
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