title: Small molecules as potent protein tyrosine phosphatase 1B (PTP1B) inhibitors documented in patents from 2009 to 2013.
abstract: Diabetes mellitus, including type 1 and type 2 diabetes mellitus (2-DM) are the main threats to human health in the worldwide. Protein tyrosine phosphatase 1B (PTP1B) is a promising molecular level legitimate therapeutic target in the effective management of 2-DM. For the search of potent PTP1B inhibitors, much investigation has revealed a large number of small-molecule compounds obtained from natural sources or prepared by synthesis/semi-synthesis with various skeletons and promising anti-PTP1B activities in the treatment of 2-DM. Although some reviews on the development of PTP1B inhibitors have been published, they were mainly concentrated on the results reported in journal articles. In this review, we will provide an overview of the developments of the potent PTP1B inhibitors claimed in recent patents during the past five years (2009-2013) with their structural features and biological features, as well as the structure-activity relationships (SARs) and strategies for finding potent and specific PTP1B inhibitors. This paper will provide valuable information for understanding the current anti-PTP1B investigation and developing potent PTP1B inhibitors as treating 2-DM drugs.
authors: Li-Jun
authors: LJ
authors: Wang
authors: Bo
authors: B
authors: Jiang
authors: Ning
authors: N
authors: Wu
authors: Shuai-Yu
authors: SY
authors: Wang
authors: Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China. shidayong@qdio.ac.cn.
authors: Da-Yong
authors: DY
authors: Shi
mesh_terms: D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy* / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1