PTP1B inhibitors as potential therapeutics in the treatment of Type 2 diabetes and obesity

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• ••A landmark PTP1B knockout study, whichprovides the much needed 'proof-of-concept' in the field to target PTPs for therapeutic development. This in vivo work shows that mice lacking functional PTP1B exhibit increased sensitivity toward insulin and are resistant to obesity, identifying PTP1B as a promising drug target in diabetes and obesity.
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• ••This paper proposes a novel strategy todevelop potent and selective PTP inhibitors by the tethering together of two small ligands that can simultaneously occupy both the active site and a nearby unique peripheral site.
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• •This paper describes a classical medicinal effort that aimed at improving the cell permeability of PTP1B inhibitors by replacing carboxyl groups with tetrazole analogues.
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• ••A nice example of applying structure-baseddesign approach to derive PTP1B selective small-molecule inhibitors.
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• ••Identification of the most potent andspecific PTP1B inhibitor to date.
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• ••This study provides the molecular basis forpotent and selective PTP1B inhibition and further establishes the feasibility of acquiring potent, yet highly selective, PTP inhibitory agents.
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