1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors |
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| Authors: | Klopfenstein Sean R Evdokimov Artem G Colson Anny-Odile Fairweather Neil T Neuman Jeffrey J Maier Matthew B Gray Jeffrey L Gerwe Gina S Stake George E Howard Brian W Farmer Julie A Pokross Matthew E Downs Thomas R Kasibhatla Bhavani Peters Kevin G |
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| Institution: | Procter & Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Road, Mason, OH 45040, USA. klopfenstein.sr@pg.com |
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| Abstract: | High-throughput screening of the P&GP corporate repository against several protein tyrosine phosphatases identified the sulfamic acid moiety as potential phosphotyrosine mimetic. Incorporation of the sulfamic acid onto a 1,2,3,4-tetrahydroisoquinoline scaffold provided a promising starting point for PTP1B inhibitor design. |
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