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.
Keywords: Chemical modification, diabetes mellitus, natural products, patents, PTP1B inhibitors, synthesized compounds,
type 2 diabetes mellitus (2-DM).
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