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서지반출
Virtual Screening and Biochemical Evaluation of Mitogen-activated Protein Kinase Phosphatase 4 Inhibitors
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  • Virtual Screening and Biochemical Evaluation of Mitogen-activated Protein Kinase Phosphatase 4 Inhibitors
  • Virtual Screening and Biochemical Evaluation of Mitogen-activated Protein Kinase Phosphatase 4 Inhibitors
저자명
Park. Hwangseo,Jeon. Jeong-Yi,Ryu. Seong Eon
간행물명
Bulletin of the Korean Chemical Society
권/호정보
2012년|33권 11호|pp.3772-3776 (5 pages)
발행정보
대한화학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

Mitogen-activated protein kinase phosphatase 4 (MKP4) has proved to be a promising target for the development of therapeutics for the treatment of diabetes and the other metabolic diseases. Here, we report an example for a successful application of the structure-based virtual screening to identify three novel inhibitors of MKP4. These inhibitors have desirable physicochemical properties as a drug candidate and reveal a moderate potency with $IC_{50}$ values ranging from 4.9 to $32.3{mu}M$. Therefore, they deserve consideration for further development by structure-activity relationship studies to optimize the inhibitory and antidiabetic activities. Structural features relevant to the stabilization of the newly identified inhibitors in the active site of MKP4 are discussed in detail.