메뉴 건너뛰기




Volumn 5, Issue 4, 2002, Pages 500-512

Recent advances in the development of small molecule inhibitors of PTP1B for the treatment of insulin resistance and type 2 diabetes

Author keywords

Diabetes; Insulin resistance; Insulin sensitivity; Protein tyrosine phosphatases; PTP1B; Signa1 transduction; Small molecule

Indexed keywords

4 (PHOSPHONODIFLUOROMETHYL)PHENYLALANINE; 4' O [2 (2 FLUOROMALONYL)]TYROSINE; 5 CARBOXY 2 NAPHTHOIC ACID; 6 (PHOSPHONODIFLUOROMETHYL) 2 NAPHTHOIC ACID; ERTIPROTAFIB; INSULIN; ISIS 113715; ISIS 1137515; N [6 (PHOSPHONODIFLUOROMETHYL) 2 NAPHTHOYL]GLUTAMIC ACID; O MALONYLTYROSINE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST; PHENYL PHOSPHATE; PHOSPHORUS ACID DERIVATIVE; PROTEIN TYROSINE PHOSPHATASE 1B; PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR; PROTEIN TYROSINE PHOSPHATASE INHIBITOR; ROSIGLITAZONE; TENTAGEL; UNCLASSIFIED DRUG; PROTEIN SYNTHESIS INHIBITOR; PROTEIN TYROSINE PHOSPHATASE;

EID: 0036654436     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review
Times cited : (38)

References (119)
  • 1
    • 0034614490 scopus 로고    scopus 로고
    • Signaling - 2000 and beyond
    • Hunter T: Signaling - 2000 and beyond. Cell (2000) 100:113-127. An excellent review and introduction to the role of phosphorylation in signal transduction.
    • (2000) Cell , vol.100 , pp. 113-127
    • Hunter, T.1
  • 2
    • 0035856949 scopus 로고    scopus 로고
    • Insulin signaling and the regulation of glucose and lipid metabolism
    • Saltiel AR, Kahn CR: Insulin signaling and the regulation of glucose and lipid metabolism. Nature (2001) 414:799-806.
    • (2001) Nature , vol.414 , pp. 799-806
    • Saltiel, A.R.1    Kahn, C.R.2
  • 3
    • 0035313868 scopus 로고    scopus 로고
    • Combinatorial control of the specificity of protein tyrosine phosphatases
    • Tonks NK, Neel BG: Combinatorial control of the specificity of protein tyrosine phosphatases. Curr Opin Cell Biol (2001) 13:182-195.
    • (2001) Curr Opin Cell Biol , vol.13 , pp. 182-195
    • Tonks, N.K.1    Neel, B.G.2
  • 4
    • 0033778926 scopus 로고    scopus 로고
    • Protein tyrosine phosphatases (PTPs) as drug targets: Inhibitors of PTP-1B for the treatment of diabetes
    • Hundahl-Møller NP, Iversen LF, Andersen HS, McCormack JG: Protein tyrosine phosphatases (PTPs) as drug targets: Inhibitors of PTP-1B for the treatment of diabetes. Curr Opin Drug Discovery Dev (2000) 3:527-540. One of the first and best reviews of the progress and challenges of developing phosphatase inhibitors, especially inhibitors of PTP1B, as drugs.
    • (2000) Curr Opin Drug Discovery Dev , vol.3 , pp. 527-540
    • Hundahl-Møller, N.P.1    Iversen, L.F.2    Andersen, H.S.3    McCormack, J.G.4
  • 5
    • 0035936763 scopus 로고    scopus 로고
    • New perspectives into the molecular pathogenesis and treatment of type 2 diabetes
    • Saltiel AR: New perspectives into the molecular pathogenesis and treatment of type 2 diabetes. Cell (2001) 104:517-529.
    • (2001) Cell , vol.104 , pp. 517-529
    • Saltiel, A.R.1
  • 6
    • 0035856920 scopus 로고    scopus 로고
    • Global and societal implications of the diabetes epidemic
    • Zimmet P, Alberti KGM, Shaw J: Global and societal implications of the diabetes epidemic. Nature (2001) 414:782-787.
    • (2001) Nature , vol.414 , pp. 782-787
    • Zimmet, P.1    Alberti, K.G.M.2    Shaw, J.3
  • 7
    • 0031893253 scopus 로고    scopus 로고
    • Protein-tyrosine phosphatases: Biological function, structural characteristics, and mechanism of catalysis
    • Zhang Z-Y: Protein-tyrosine phosphatases: Biological function, structural characteristics, and mechanism of catalysis. Crit Rev Biochem Mol Biol (1998) 33:1-52.
    • (1998) Crit Rev Biochem Mol Biol , vol.33 , pp. 1-52
    • Zhang, Z.-Y.1
  • 8
    • 0002258614 scopus 로고
    • The low-Mr cytosolic phosphotyrosine protein phosphatases
    • Ramponi G: The low-Mr cytosolic phosphotyrosine protein phosphatases. Adv Prot Phosphates (1994) 8:1-25.
    • (1994) Adv Prot Phosphates , vol.8 , pp. 1-25
    • Ramponi, G.1
  • 9
    • 0028858055 scopus 로고
    • Transition state and rate-limiting step of the reaction catalyzed by the human dual-specificity phosphatase VHR
    • Zhang Z-Y, Wu L, Chen L: Transition state and rate-limiting step of the reaction catalyzed by the human dual-specificity phosphatase VHR. Biochemistry (1995) 34:16088-16096.
    • (1995) Biochemistry , vol.34 , pp. 16088-16096
    • Zhang, Z.-Y.1    Wu, L.2    Chen, L.3
  • 10
    • 0026766356 scopus 로고
    • A thousand and two protein tyrosine phosphatases
    • Pot DA, Dixon JE: A thousand and two protein tyrosine phosphatases. Biochem Biophys Acta (1992) 1136:35-43.
    • (1992) Biochem Biophys Acta , vol.1136 , pp. 35-43
    • Pot, D.A.1    Dixon, J.E.2
  • 12
    • 0032576529 scopus 로고    scopus 로고
    • Protein tyrosine phosphatases: Counting the trees in the forest
    • Van Huijsduijen RH: Protein tyrosine phosphatases: Counting the trees in the forest. Gene (1998) 225:1-8.
    • (1998) Gene , vol.225 , pp. 1-8
    • Van Huijsduijen, R.H.1
  • 14
    • 0035943403 scopus 로고    scopus 로고
    • A comparison of the Celera and Ensembl predicted gene sets reveals little overlap in novel genes
    • Hogenesch JB, Ching KA, Batalov S, Su AI, Walker JR, Zhou Y, Kay SA, Schultz PG, Cooke MP: A comparison of the Celera and Ensembl predicted gene sets reveals little overlap in novel genes. Cell (2001) 106:413-415. An important contribution to gene counting exercises based on the human genome sequence indicates that existing estimates of the total number of genes may be low.
    • (2001) Cell , vol.106 , pp. 413-415
    • Hogenesch, J.B.1    Ching, K.A.2    Batalov, S.3    Su, A.I.4    Walker, J.R.5    Zhou, Y.6    Kay, S.A.7    Schultz, P.G.8    Cooke, M.P.9
  • 15
    • 0035856943 scopus 로고    scopus 로고
    • Diabetes mellitus and genetically programmed defects in β-cell function
    • Bell GI, Polonsky KS: Diabetes mellitus and genetically programmed defects in β-cell function. Nature (2001) 414:788-791.
    • (2001) Nature , vol.414 , pp. 788-791
    • Bell, G.I.1    Polonsky, K.S.2
  • 16
    • 0025146562 scopus 로고
    • Structural diversity and evolution of human receptor-like protein tyrosine phosphatase
    • Krueger NX, Steuli M, Saito H: Structural diversity and evolution of human receptor-like protein tyrosine phosphatase. EMBO J (1990) 9:3241-3252.
    • (1990) EMBO J , vol.9 , pp. 3241-3252
    • Krueger, N.X.1    Steuli, M.2    Saito, H.3
  • 17
    • 0024211451 scopus 로고
    • A new member of the immunoglobulin superfamily that has a cytoplasmic region homologous to the leukocyte common antigen
    • Streuli M, Krueger NX, Hall LR, Schlossman SF, Saito H: A new member of the immunoglobulin superfamily that has a cytoplasmic region homologous to the leukocyte common antigen. J Exp Med (1988) 168:1523-1530.
    • (1988) J Exp Med , vol.168 , pp. 1523-1530
    • Streuli, M.1    Krueger, N.X.2    Hall, L.R.3    Schlossman, S.F.4    Saito, H.5
  • 18
    • 0023924803 scopus 로고
    • Purification of the major protein-tyrosine-phosphatases of human placenta
    • Tonks NK, Diltz CD, Fischer EH: Purification of the major protein-tyrosine-phosphatases of human placenta. J Biol Chem (1988) 263:6722-6730. This study initiated the field of protein tyrosine phosphatase research.
    • (1988) J Biol Chem , vol.263 , pp. 6722-6730
    • Tonks, N.K.1    Diltz, C.D.2    Fischer, E.H.3
  • 20
    • 0028932005 scopus 로고
    • Purification, identification and subcellular distribution of three predominant protein-tyrosine phosphatase enzymes in skeletal muscle tissue
    • Ahmad F, Goldstein BJ: Purification, identification and subcellular distribution of three predominant protein-tyrosine phosphatase enzymes in skeletal muscle tissue. Biochem Biophys Acta (1995) 1248:57-69.
    • (1995) Biochem Biophys Acta , vol.1248 , pp. 57-69
    • Ahmad, F.1    Goldstein, B.J.2
  • 21
    • 0033573953 scopus 로고    scopus 로고
    • Overexpression of protein tyrosine phosphatase-α (PTP-α) but not PTP-κ inhibits translocation of GLUT4 in rat adipose cells
    • Cong LN, Chen H, Li Y, Lin CH, Sap J, Quon MJ: Overexpression of protein tyrosine phosphatase-α (PTP-α) but not PTP-κ inhibits translocation of GLUT4 in rat adipose cells. Biochem Biophys Res Commun (1999) 255:200-207.
    • (1999) Biochem Biophys Res Commun , vol.255 , pp. 200-207
    • Cong, L.N.1    Chen, H.2    Li, Y.3    Lin, C.H.4    Sap, J.5    Quon, M.J.6
  • 23
    • 0029130199 scopus 로고
    • Osmotic loading of neutralizing antibodies demonstrates a role for protein-tyrosine phosphatase 1B in negative regulation of the insulin action pathway
    • Ahmad F, Li P-M, Meyerovicht J, Goldstein BJ: Osmotic loading of neutralizing antibodies demonstrates a role for protein-tyrosine phosphatase 1B in negative regulation of the insulin action pathway. J Biol Chem (1995) 270:20503-20508.
    • (1995) J Biol Chem , vol.270 , pp. 20503-20508
    • Ahmad, F.1    Li, P.-M.2    Meyerovicht, J.3    Goldstein, B.J.4
  • 24
    • 0028816605 scopus 로고
    • Insulin receptor signaling is augmented by antisense inhibition of the protein tyrosine phosphatase LAR
    • Kulas DT, Zhang W-R, Goldstein BJ, Furlanetto RW, Mooney RA: Insulin receptor signaling is augmented by antisense inhibition of the protein tyrosine phosphatase LAR. J Biol Chem (1995) 270:2435-2438.
    • (1995) J Biol Chem , vol.270 , pp. 2435-2438
    • Kulas, D.T.1    Zhang, W.-R.2    Goldstein, B.J.3    Furlanetto, R.W.4    Mooney, R.A.5
  • 25
    • 0033587069 scopus 로고    scopus 로고
    • Receptor protein tyrosine phosphatase alpha activates Src-family kinases and controls integrin-mediated responses in fibroblasts
    • Su J, Muranjan M, Sap J: Receptor protein tyrosine phosphatase alpha activates Src-family kinases and controls integrin-mediated responses in fibroblasts. Curr Biol (1999) 9:505-511.
    • (1999) Curr Biol , vol.9 , pp. 505-511
    • Su, J.1    Muranjan, M.2    Sap, J.3
  • 30
    • 0031055324 scopus 로고    scopus 로고
    • Development of "substrate-trapping" mutants to identify physiological substrates of protein tyrosine phosphatases
    • Flint AJ, Tiganis T, Barford D, Tonks NK: Development of "substrate-trapping" mutants to identify physiological substrates of protein tyrosine phosphatases. Proc Natl Acad Sci USA (1997) 94:1680-1685.
    • (1997) Proc Natl Acad Sci USA , vol.94 , pp. 1680-1685
    • Flint, A.J.1    Tiganis, T.2    Barford, D.3    Tonks, N.K.4
  • 33
    • 0028785789 scopus 로고
    • Why is phosphonodifluoromethyl phenylalanine a more potent inhibitory moiety than phosphonomethyl phenylalanine toward protein-tyrosine phosphatases?
    • Chen L, Wu L, Otaka A, Smyth MS, Roller PP, Burke TR Jr, den Hertog J, Zhang Z-Y: Why is phosphonodifluoromethyl phenylalanine a more potent inhibitory moiety than phosphonomethyl phenylalanine toward protein-tyrosine phosphatases? Biochem Biophy Res Commun (1995) 216:976-984.
    • (1995) Biochem Biophy Res Commun , vol.216 , pp. 976-984
    • Chen, L.1    Wu, L.2    Otaka, A.3    Smyth, M.S.4    Roller, P.P.5    Burke T.R., Jr.6    Den Hertog, J.7    Zhang, Z.-Y.8
  • 34
    • 0028882428 scopus 로고
    • Phosphonate inhibitors of protein-tyrosine and serine/threonine phosphatases
    • Kole HK, Smyth MS, Russ PL, Burke TR Jr: Phosphonate inhibitors of protein-tyrosine and serine/threonine phosphatases. Biochemistry (1995) 311:1025-1031.
    • (1995) Biochemistry , vol.311 , pp. 1025-1031
    • Kole, H.K.1    Smyth, M.S.2    Russ, P.L.3    Burke T.R., Jr.4
  • 36
    • 0030467887 scopus 로고    scopus 로고
    • Small molecule interactions with protein-tyrosine phosphatase PTP1B and their use in inhibitor design
    • Burke TR Jr, Ye B, Yan X, Wang S, Jia Z, Chen L, Zhang Z-Y, Barford D: Small molecule interactions with protein-tyrosine phosphatase PTP1B and their use in inhibitor design. Biochemistry (1996) 35:15989-15996.
    • (1996) Biochemistry , vol.35 , pp. 15989-15996
    • Burke T.R., Jr.1    Ye, B.2    Yan, X.3    Wang, S.4    Jia, Z.5    Chen, L.6    Zhang, Z.-Y.7    Barford, D.8
  • 37
    • 0033586791 scopus 로고    scopus 로고
    • Nuclear magnetic resonance and restrained molecular dynamics studies of the interaction of an epidermal growth factor-derived peptide with protein tyrosine phosphatase 1B
    • Glover NR, Tracey AS: Nuclear magnetic resonance and restrained molecular dynamics studies of the interaction of an epidermal growth factor-derived peptide with protein tyrosine phosphatase 1B. Biochemistry (1999) 38:5256-5271.
    • (1999) Biochemistry , vol.38 , pp. 5256-5271
    • Glover, N.R.1    Tracey, A.S.2
  • 38
    • 0034696863 scopus 로고    scopus 로고
    • Preparation of chiral α-monofluoroalkyphosphonic acids and their evaluation as inhibitors of protein tyrosine phosphatase 1B
    • Kotoris CC, Wen W, Lough A, Taylor SD: Preparation of chiral α-monofluoroalkyphosphonic acids and their evaluation as inhibitors of protein tyrosine phosphatase 1B. J Chem Soc Perkin Trans I (2000) 8:1271-1282.
    • (2000) J Chem Soc Perkin Trans I , vol.8 , pp. 1271-1282
    • Kotoris, C.C.1    Wen, W.2    Lough, A.3    Taylor, S.D.4
  • 39
    • 0035169222 scopus 로고    scopus 로고
    • ((α-monofluoroalkyl)phosphonates: A class of isoacidic and 'tunable' mimics of biological phosphates
    • Berkowitz DB, Bose M: ((α-Monofluoroalkyl)phosphonates: A class of isoacidic and 'tunable' mimics of biological phosphates. J Fluorine Chem (2001) 112:13-33.
    • (2001) J Fluorine Chem , vol.112 , pp. 13-33
    • Berkowitz, D.B.1    Bose, M.2
  • 40
    • 0036170309 scopus 로고    scopus 로고
    • Molecular modeling of protein tyrosine phosphatase 1B (PTP1B) inhibitors
    • Murthy VS, Kulkami VM: Molecular modeling of protein tyrosine phosphatase 1B (PTP1B) inhibitors. Bioorg Med Chem (2002) 10:897-906.
    • (2002) Bioorg Med Chem , vol.10 , pp. 897-906
    • Murthy, V.S.1    Kulkami, V.M.2
  • 41
    • 0033593914 scopus 로고    scopus 로고
    • Synthesis and biological evaluation of α,αdifluorobenzylphosphonic acid derivatives as small molecular inhibitors of protein-tyrosine phosphatase 1B
    • Yokomatsu T, Murano T, Umesue I, Soeda S, Shimeno H, Shibuya S: Synthesis and biological evaluation of α,αdifluorobenzylphosphonic acid derivatives as small molecular inhibitors of protein-tyrosine phosphatase 1B. Bioorg Med Chem Lett (1999) 9:529-532.
    • (1999) Bioorg Med Chem Lett , vol.9 , pp. 529-532
    • Yokomatsu, T.1    Murano, T.2    Umesue, I.3    Soeda, S.4    Shimeno, H.5    Shibuya, S.6
  • 42
    • 0028990357 scopus 로고
    • Protein-tyrosine phosphatase inhibition by a peptide containing the phosphotyrosyl mimetic, L-Omalonyltyrosine (L-OMT)
    • Kole HK, Akamatsu M, Ye B, Yan X, Barford D, Roller PP, Burke TR Jr. Protein-tyrosine phosphatase inhibition by a peptide containing the phosphotyrosyl mimetic, L-Omalonyltyrosine (L-OMT). Biochem Biophys Res Commun (1995) 209:817-822.
    • (1995) Biochem Biophys Res Commun , vol.209 , pp. 817-822
    • Kole, H.K.1    Akamatsu, M.2    Ye, B.3    Yan, X.4    Barford, D.5    Roller, P.P.6    Burke T.R., Jr.7
  • 43
    • 0029930442 scopus 로고    scopus 로고
    • 4′-O-[2-(2-fluoromalonyl)]-Ltyrosine: A phosphotyrosyl mimic for the preparation of signal transduction inhibitory peptides
    • Burke TR Jr, Ye B, Akamatsu M, Ford H Jr, Yan X, Kole HK, Wolf G, Shoelson SE, Roller PP: 4′-O-[2-(2-fluoromalonyl)]-Ltyrosine: A phosphotyrosyl mimic for the preparation of signal transduction inhibitory peptides. J Med Chem (1996) 39:1021-1027.
    • (1996) J Med Chem , vol.39 , pp. 1021-1027
    • Burke T.R., Jr.1    Ye, B.2    Akamatsu, M.3    Ford H., Jr.4    Yan, X.5    Kole, H.K.6    Wolf, G.7    Shoelson, S.E.8    Roller, P.P.9
  • 44
    • 0034193474 scopus 로고    scopus 로고
    • Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains
    • Gao Y, Wu L, Luo JH, Guo R, Yang D, Zhang Z-Y, Burke TR Jr. Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains. Bioorg Med Chem Lett (2000) 10:923-927.
    • (2000) Bioorg Med Chem Lett , vol.10 , pp. 923-927
    • Gao, Y.1    Wu, L.2    Luo, J.H.3    Guo, R.4    Yang, D.5    Zhang, Z.-Y.6    Burke T.R., Jr.7
  • 47
    • 0031757577 scopus 로고    scopus 로고
    • Structure-based design and synthesis of small molecule protein-tyrosine phosphatase 1B inhibitors
    • Yao ZJ, Ye B, Wu XW, Wang S, Wu L, Zhang Z-Y, Burke TR Jr: Structure-based design and synthesis of small molecule protein-tyrosine phosphatase 1B inhibitors. Bioorg Med Chem (1998) 6:1799-1810.
    • (1998) Bioorg Med Chem , vol.6 , pp. 1799-1810
    • Yao, Z.J.1    Ye, B.2    Wu, X.W.3    Wang, S.4    Wu, L.5    Zhang, Z.-Y.6    Burke T.R., Jr.7
  • 48
    • 0031457541 scopus 로고    scopus 로고
    • Identification of a second aryl phosphate-binding site in protein-tyrosine phosphatase 1B: A paradigm for inhibitor design
    • Puius YA, Zhao Y, Sullivan M, Lawrence DS, Almo SC, Zhang ZY: Identification of a second aryl phosphate-binding site in protein-tyrosine phosphatase 1B: A paradigm for inhibitor design. Proc Natl Acad Sci USA (1997) 94:13420-13425.
    • (1997) Proc Natl Acad Sci USA , vol.94 , pp. 13420-13425
    • Puius, Y.A.1    Zhao, Y.2    Sullivan, M.3    Lawrence, D.S.4    Almo, S.C.5    Zhang, Z.Y.6
  • 49
    • 0033596855 scopus 로고    scopus 로고
    • Potent and highly selective inhibitors of the protein tyrosine phosphatase 1B
    • Taing M, Keng Y-F, Shen K, Wu L, Lawrence DS, Zhang Z-Y: Potent and highly selective inhibitors of the protein tyrosine phosphatase 1B. Biochemistry (1999) 38:3793-3803.
    • (1999) Biochemistry , vol.38 , pp. 3793-3803
    • Taing, M.1    Keng, Y.-F.2    Shen, K.3    Wu, L.4    Lawrence, D.S.5    Zhang, Z.-Y.6
  • 50
    • 0032539505 scopus 로고    scopus 로고
    • Naphthalenebis[α,α-difluoromethylenephosphonates] as potent inhibitors of protein tyrosine phosphatases
    • Wang Q, Huang Z, Ramachandran C, Dinaut AN, Taylor SD: Naphthalenebis[α,α-difluoromethylenephosphonates] as potent inhibitors of protein tyrosine phosphatases. Bioorg Med Chem Lett (1998) 8:345-350.
    • (1998) Bioorg Med Chem Lett , vol.8 , pp. 345-350
    • Wang, Q.1    Huang, Z.2    Ramachandran, C.3    Dinaut, A.N.4    Taylor, S.D.5
  • 51
    • 0035924182 scopus 로고    scopus 로고
    • Structure of protein tyrosine phosphatase 1B in complex with inhibitors bearing two phosphotyrosine mimetics
    • Jia Z, Ye Q, Dinaut AN, Wang Q, Waddleton D, Payette P, Ramachandran C, Kennedy B, Hum G, Taylor SD: Structure of protein tyrosine phosphatase 1B in complex with inhibitors bearing two phosphotyrosine mimetics. J Med Chem (2001) 44:4584-4594. Discussion of the binding modes of bis-difluoromethylenephosphonate inhibitors.
    • (2001) J Med Chem , vol.44 , pp. 4584-4594
    • Jia, Z.1    Ye, Q.2    Dinaut, A.N.3    Wang, Q.4    Waddleton, D.5    Payette, P.6    Ramachandran, C.7    Kennedy, B.8    Hum, G.9    Taylor, S.D.10
  • 52
    • 0034507958 scopus 로고    scopus 로고
    • Molecular basis for the dephosphorylation of the activation segment of the insulin receptor by protein tyrosine phosphatase 1B
    • Salmeen A, Andersen JN, Myers MP, Tonks NK, Barford D: Molecular basis for the dephosphorylation of the activation segment of the insulin receptor by protein tyrosine phosphatase 1B. Mol Cell (2000) 6:1401-1412.
    • (2000) Mol Cell , vol.6 , pp. 1401-1412
    • Salmeen, A.1    Andersen, J.N.2    Myers, M.P.3    Tonks, N.K.4    Barford, D.5
  • 53
    • 0034723343 scopus 로고    scopus 로고
    • Assessment of protein-tyrosine phosphatase 1B substrate specificity using "inverse alanine scanning"
    • Vetter SW, Keng YF, Lawrence DS, Zhang Z-Y: Assessment of protein-tyrosine phosphatase 1B substrate specificity using "inverse alanine scanning". J Biol Chem (2000) 275:2265-2268.
    • (2000) J Biol Chem , vol.275 , pp. 2265-2268
    • Vetter, S.W.1    Keng, Y.F.2    Lawrence, D.S.3    Zhang, Z.-Y.4
  • 54
    • 0034682562 scopus 로고    scopus 로고
    • Structural basis of plasticity in protein tyrosine phosphatase 1B substrate recognition
    • Sarmiento M, Puius YA, Vetter SW, Keng Y, Wu L, Zhoa Y, Lawrence DS, Almo SC, Zhang Z-Y: Structural basis of plasticity in protein tyrosine phosphatase 1B substrate recognition. Biochemistry (2000) 39:8171-8179. Discussion of the structural basis of plasticity in PTP1B substrate recognition.
    • (2000) Biochemistry , vol.39 , pp. 8171-8179
    • Sarmiento, M.1    Puius, Y.A.2    Vetter, S.W.3    Keng, Y.4    Wu, L.5    Zhoa, Y.6    Lawrence, D.S.7    Almo, S.C.8    Zhang, Z.-Y.9
  • 55
    • 0032544162 scopus 로고    scopus 로고
    • Potent inhibition of protein-tyrosine phosphatase-1B using the phosphotyrosyl mimetic fluoro-O-malonyl tyrosine (FOMT)
    • Roller PP, Wu L, Zhang Z-Y, Burke TR Jr. Potent inhibition of protein-tyrosine phosphatase-1B using the phosphotyrosyl mimetic fluoro-O-malonyl tyrosine (FOMT). Bioorg Med Chem Lett (1998) 8:2149-2150.
    • (1998) Bioorg Med Chem Lett , vol.8 , pp. 2149-2150
    • Roller, P.P.1    Wu, L.2    Zhang, Z.-Y.3    Burke T.R., Jr.4
  • 56
    • 0035861668 scopus 로고    scopus 로고
    • Acquisition of a specific and potent PTP1B inhibitor from a novel combinatorial library and screening procedure
    • Shen K, Keng YF, Wu L, Guo XL, Lawrence DS, Zhang Z-Y: Acquisition of a specific and potent PTP1B inhibitor from a novel combinatorial library and screening procedure. J Biol Chem (2001) 276:47311-47319. Development of the most potent and specific PTP 1B inhibitor to date.
    • (2001) J Biol Chem , vol.276 , pp. 47311-47319
    • Shen, K.1    Keng, Y.F.2    Wu, L.3    Guo, X.L.4    Lawrence, D.S.5    Zhang, Z.-Y.6
  • 59
    • 0032552183 scopus 로고    scopus 로고
    • Enantioselective synthesis of nonphosphorous-containing phosphotyrosyl mimetics and their use in the preparation of tyrosine phosphatase inhibitory peptides
    • Burke TR Jr, Yao ZJ, He Z, Milne GWA, Li W, Zhang Z-Y, Voigt JH: Enantioselective synthesis of nonphosphorous-containing phosphotyrosyl mimetics and their use in the preparation of tyrosine phosphatase inhibitory peptides. Tetrahedron (1998) 54:9981-9994.
    • (1998) Tetrahedron , vol.54 , pp. 9981-9994
    • Burke T.R., Jr.1    Yao, Z.J.2    He, Z.3    Milne, G.W.A.4    Li, W.5    Zhang, Z.-Y.6    Voigt, J.H.7
  • 70
    • 13044270997 scopus 로고    scopus 로고
    • PTP1B inhibition and anti-hyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes
    • Wrobel J, Sredy J, Moxham C, Dietrich A, Li Z, Sawicki DR, Seestaller L, Wu L, Katz A, Sullivan D, Tio C, Zhang Z-Y: PTP1B inhibition and anti-hyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes. J Med Chem (1999) 42:3199-3202.
    • (1999) J Med Chem , vol.42 , pp. 3199-3202
    • Wrobel, J.1    Sredy, J.2    Moxham, C.3    Dietrich, A.4    Li, Z.5    Sawicki, D.R.6    Seestaller, L.7    Wu, L.8    Katz, A.9    Sullivan, D.10    Tio, C.11    Zhang, Z.-Y.12
  • 75
    • 0037116638 scopus 로고    scopus 로고
    • Oral antihyperglycemic therapy for type 2 diabetes: Scientific review
    • Inzucchi SE: Oral antihyperglycemic therapy for type 2 diabetes: Scientific review. J Am Med Assoc (2002) 287:360-372.
    • (2002) J Am Med Assoc , vol.287 , pp. 360-372
    • Inzucchi, S.E.1
  • 76
    • 0035124186 scopus 로고    scopus 로고
    • New oral therapies for type 2 diabetes mellitus: The glitazones or insulin sensitizers
    • Mudaliar S, Henry RR: New oral therapies for type 2 diabetes mellitus: The glitazones or insulin sensitizers. Annu Rev Med (2001) 52:239-257.
    • (2001) Annu Rev Med , vol.52 , pp. 239-257
    • Mudaliar, S.1    Henry, R.R.2
  • 77
    • 0038592558 scopus 로고    scopus 로고
    • Amino (oxo) acetic acid protein tyrosine phosphatase inhibitors. WO-00218323 (2002)
    • ABBOT LABORATORIES (Liu G, Szczepankiewicz BG, PEI Z, Xin Z, Oost TK, Janowick DA): Amino (oxo) acetic acid protein tyrosine phosphatase inhibitors. WO-00218323 (2002).
    • Liu, G.1    Szczepankiewicz, B.G.2    Pei, Z.3    Xin, Z.4    Oost, T.K.5    Janowick, D.A.6
  • 78
    • 0037916403 scopus 로고    scopus 로고
    • Biphenyl sulfonyl aryl carboxylic acids useful in the treatment of insulin resistance and hyperglycemia. US-06221902 (2001)
    • AMERICAN HOME PRODUCTS CORPORATION (Malamas MS, Adebayo F, Dollings PJ): Biphenyl sulfonyl aryl carboxylic acids useful in the treatment of insulin resistance and hyperglycemia. US-06221902 (2001).
    • Malamas, M.S.1    Adebayo, F.2    Dollings, P.J.3
  • 79
    • 0037578442 scopus 로고    scopus 로고
    • Furan, benzofurans and thiophene useful in the treatment of insulin resistance and hyperglycemia. US-06103708 (2000)
    • AMERICAN HOME PRODUCTS CORPORATION (Dollings PJ, McDevitt RE, Adebayo FO): Furan, benzofurans and thiophene useful in the treatment of insulin resistance and hyperglycemia. US-06103708 (2000).
    • Dollings, P.J.1    McDevitt, R.E.2    Adebayo, F.O.3
  • 80
    • 0038253962 scopus 로고    scopus 로고
    • Biphenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia. WO-09958518 (1999)
    • AMERICAN HOME PRODUCTS CORPORATION (Malamas MS, McDevitt RE, Adebayo FO): Biphenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia. WO-09958518 (1999).
    • Malamas, M.S.1    McDevitt, R.E.2    Adebayo, F.O.3
  • 82
    • 0038592559 scopus 로고    scopus 로고
    • 11-aryl-benzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes useful in the treatment of insulin resistance and hyperglycemia. US-06110962 (2000)
    • AMERICAN HOME PRODUCTS CORPORATION (Wrobel JE, Dietrich AJ, Li Z): 11-aryl-benzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes useful in the treatment of insulin resistance and hyperglycemia. US-06110962 (2000).
    • Wrobel, J.E.1    Dietrich, A.J.2    Li, Z.3
  • 83
    • 0038592560 scopus 로고    scopus 로고
    • Naphtho[2,3-b]heteroar-4-yl derivatives. WO-09958522 (1999)
    • AMERICAN HOME PRODUCTS CORPORATION (Dollings PJ, Dietrich AJ, Wrobel JE): Naphtho[2,3-b]heteroar-4-yl derivatives. WO-09958522 (1999).
    • Dollings, P.J.1    Dietrich, A.J.2    Wrobel, J.E.3
  • 84
    • 0038592562 scopus 로고    scopus 로고
    • 2-(Acylaminothiazole-4-yl)acetic acid derivatives. WO-09958514 (1999)
    • AMERICAN HOME PRODUCTS CORPORATION (Kees KL): 2-(Acylaminothiazole-4-yl)acetic acid derivatives. WO-09958514 (1999).
    • Kees, K.L.1
  • 85
    • 0037916404 scopus 로고    scopus 로고
    • 4-aryl-1-oxa-9-thia-cylopenta[b]fluorenes. US-06281238 (2001)
    • AMERICAN HOME PRODUCTS CORPORATION (Li Z): 4-aryl-1-oxa-9-thia-cylopenta[b]fluorenes. US-06281238 (2001).
    • Li, Z.1
  • 86
    • 0038253963 scopus 로고    scopus 로고
    • 4-Aryl-1-oxa-9-thia-cyclopenta[b]fluorene. US-20010020037 (2001)
    • AMERICAN HOME PRODUCTS CORPORATION (Li Z, Wrobel JE): 4-Aryl-1-oxa-9-thia-cyclopenta[b]fluorene. US-20010020037 (2001).
    • Li, Z.1    Wrobel, J.E.2
  • 87
    • 0038253964 scopus 로고    scopus 로고
    • Aryloxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia. US-06110963 (2000)
    • AMERICAN HOME PRODUCTS CORPORATION (Malamas MS): Aryloxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia. US-06110963 (2000).
    • Malamas, M.S.1
  • 88
    • 0038253967 scopus 로고    scopus 로고
    • Oxazole-aryl-carboxylic acids useful in the treatment of insulin resistance and hyperglycemia. WO-09958511 (1999)
    • AMERICAN HOME PRODUCTS CORPORATION (Malamas MS): Oxazole-aryl-carboxylic acids useful in the treatment of insulin resistance and hyperglycemia. WO-09958511 (1999).
    • Malamas, M.S.1
  • 89
    • 0038592564 scopus 로고    scopus 로고
    • 11-aryl-benzo[b]naphtha [2,3-d] furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes useful in the treatment of insulin resistance and hyperglycemia. WO-09958521 (1999)
    • AMERICAN HOME PRODUCTS CORPORATION (Wrobel JE, Dietrich AJ, Li Z): 11-aryl-benzo[b]naphtha [2,3-d] furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes useful in the treatment of insulin resistance and hyperglycemia. WO-09958521 (1999).
    • Wrobel, J.E.1    Dietrich, A.J.2    Li, Z.3
  • 91
    • 0038592565 scopus 로고    scopus 로고
    • Benzothiophenes, benzofurans and indoles useful in tfle the treatment of insulin resistance and hyperglycemia. WO-09961435 (1999)
    • AMERICAN HOME PRODUCTS CORPORATION (Wrobel JE, Dietrich AJ, Antane MM): Benzothiophenes, benzofurans and indoles useful in tfle the treatment of insulin resistance and hyperglycemia. WO-09961435 (1999).
    • Wrobel, J.E.1    Dietrich, A.J.2    Antane, M.M.3
  • 92
    • 0037916410 scopus 로고    scopus 로고
    • Sulfur substituted aryldifluoromethyl phosphonic acids as PTP-1B inhibitors. WO-00170754 (2001)
    • MERCK FROSST GANADA & CO/BANYU & CO/BANYU PHARM CO LTD (Bayly C, Ohkubo M): Sulfur substituted aryldifluoromethyl phosphonic acids as PTP-1B inhibitors. WO-00170754 (2001).
    • Bayly, C.1    Ohkubo, M.2
  • 94
    • 0038253965 scopus 로고    scopus 로고
    • Phosphonic acid biaryl derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B). WO-00146203 (2001)
    • MERCK FROSST CANADA & CO (Lau CK, Bayly C, Gauthier JY, Leblanc Y, Li CS, Roy P, Therien M, Wang Z): Phosphonic acid biaryl derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B). WO-00146203 (2001).
    • Lau, C.K.1    Bayly, C.2    Gauthier, J.Y.3    Leblanc, Y.4    Li, C.S.5    Roy, P.6    Therien, M.7    Wang, Z.8
  • 95
    • 0038592575 scopus 로고    scopus 로고
    • Aromatic phosphonates as protein tyrosine phosphatase 1 B (PTP-1 B) inhibitors. WO-00146204 (2001)
    • MERCK FROSST CANADA & CO (Leblanc Y, Dufresne C, Gauthier JY, Young R): Aromatic phosphonates as protein tyrosine phosphatase 1 B (PTP-1 B) inhibitors. WO-00146204 (2001).
    • Leblanc, Y.1    Dufresne, C.2    Gauthier, J.Y.3    Young, R.4
  • 97
    • 0037578447 scopus 로고    scopus 로고
    • Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B). WO-00146205 (2001)
    • MERCK FROSST CANADA & Co (Leblanc Y, Lau CK, Dufresne C, Li CS, Roy P, Wang Z, Scheigetz J, Boyd M): Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B). WO-00146205 (2001).
    • Leblanc, Y.1    Lau, C.K.2    Dufresne, C.3    Li, C.S.4    Roy, P.5    Wang, Z.6    Scheigetz, J.7    Boyd, M.8
  • 99
    • 0038253969 scopus 로고    scopus 로고
    • Protein tyrosine phosphatase-1 B (PTP-1 B) deficient mice and uses thereof. WO-00006712 (2000)
    • MERCK FROSST CANADA & CO (Kennedy B, Payette P, Gresser M, Ramachandran C, Tremblay ML, Elchebly M): Protein tyrosine phosphatase-1 B (PTP-1 B) deficient mice and uses thereof. WO-00006712 (2000).
    • Kennedy, B.1    Payette, P.2    Gresser, M.3    Ramachandran, C.4    Tremblay, M.L.5    Elchebly, M.6
  • 100
    • 0038592568 scopus 로고    scopus 로고
    • Phosphonic and carboxylic acid derivatives as inhibitors of protein tyrosine phosphatase-1B (PTP-1B). WO-00069889 (2000)
    • MERCK FROSST CANADA & CO (Leblanc Y, Dufresne C, Roy P, Wang Z): Phosphonic and carboxylic acid derivatives as inhibitors of protein tyrosine phosphatase-1B (PTP-1B). WO-00069889 (2000).
    • Leblanc, Y.1    Dufresne, C.2    Roy, P.3    Wang, Z.4
  • 101
    • 0037916405 scopus 로고    scopus 로고
    • Phosphonic and carboxylic acid derivatives as inhibitors of protein tyrosine phosphatase-1B (PTP1B). US-06365592 (2002)
    • MERCK FROSST CANADA & CO (Leblanc Y, Claude D, Roy P, Wang Z): Phosphonic and carboxylic acid derivatives as inhibitors of protein tyrosine phosphatase-1B (PTP1B). US-06365592 (2002).
    • Leblanc, Y.1    Claude, D.2    Roy, P.3    Wang, Z.4
  • 102
    • 0038592574 scopus 로고    scopus 로고
    • Process for obtaining inhibitors/activators of an enzyme. WO-00164939 (2001)
    • MORPHOCHEM AG (Liu Y, Wang S, Zhang Z-Y): Process for obtaining inhibitors/activators of an enzyme. WO-00164939 (2001).
    • Liu, Y.1    Wang, S.2    Zhang, Z.-Y.3
  • 105
    • 0037578444 scopus 로고    scopus 로고
    • Modulators of protein tyrosine phosphatases (PTPases). US-200200019412 (2002)
    • NOVO NORDISK AS (Andersen HS, Jones TK, Holsworth DD): Modulators of protein tyrosine phosphatases (PTPases). US-200200019412 (2002).
    • Andersen, H.S.1    Jones, T.K.2    Holsworth, D.D.3
  • 110
    • 0038592573 scopus 로고    scopus 로고
    • Modulators of protein tyrosine phosphatases (PTPases). WO-09946268 (1999)
    • ONTOGEN CORPORATION (Andersen HS, Jones TK, Holsworth DD): Modulators of protein tyrosine phosphatases (PTPases). WO-09946268 (1999).
    • Andersen, H.S.1    Jones, T.K.2    Holsworth, D.D.3
  • 114
    • 0037916407 scopus 로고    scopus 로고
    • Modulators of proteins with phosphotyrosine recognition units. US-05965558 (1999)
    • ONTOGEN CORPORATION (Mjalli A, Sarshar S, Cao X, Bakir F): Modulators of proteins with phosphotyrosine recognition units. US-05965558 (1999).
    • Mjalli, A.1    Sarshar, S.2    Cao, X.3    Bakir, F.4
  • 117
    • 0038253961 scopus 로고    scopus 로고
    • Tyrosine phosphatase inhibitors. WO-00190067 (2001)
    • TAKEDA CHEMICAL INDUSTRIES LTD (Matsumoto T, Katayama N, Mabuchi H): Tyrosine phosphatase inhibitors. WO-00190067 (2001).
    • Matsumoto, T.1    Katayama, N.2    Mabuchi, H.3
  • 118
    • 0038253966 scopus 로고    scopus 로고
    • O-Malonyltyrosyl compounds, O-malonyltyrosyl compound-containing peptides and uses thereof. WO-9630332 (1996)
    • THE GOVERNMENT OF THE UNITED STATES OF AMERICA (Burke TR Jr, Akamatsu M, Kole HK, Yan X, Roller PR, Ye B): O-Malonyltyrosyl compounds, O-malonyltyrosyl compound-containing peptides and uses thereof. WO-9630332 (1996).
    • Burke T.R., Jr.1    Akamatsu, M.2    Kole, H.K.3    Yan, X.4    Roller, P.R.5    Ye, B.6
  • 119
    • 0037578449 scopus 로고    scopus 로고
    • Method for treatment of insulin resistance. WO-09732595 (1997)
    • UNIVERSITY OF CALIFORNIA (Olefsky JM): Method for treatment of insulin resistance. WO-09732595 (1997).
    • Olefsky, J.M.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.