Protein tyrosine phosphatases: Structure and function, substrate specificity, and inhibitor development

Annual Review of Pharmacology and Toxicology

Volumn 42, Issue , 2002, Pages 209-234

  Zhang, Zhong Yin ^a  

^a ALBERT EINSTEIN COLLEGE OF MEDICINE   (United States)

Author keywords

Cdc25; Drug discovery; MKP3; Molecular recognition; PTP1B; Tyrosine phosphorylation

Indexed keywords

CD45 ANTIGEN; CYCLIN DEPENDENT KINASE; MITOGEN ACTIVATED PROTEIN KINASE; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE PHOSPHATASE; PROTEIN TYROSINE PHOSPHATASE INHIBITOR; RNA;

BINDING AFFINITY; DRUG DESIGN; DRUG MECHANISM; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME SPECIFICITY; ENZYME STRUCTURE; HUMAN; MOLECULAR RECOGNITION; MUTAGENESIS; NONHUMAN; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; REVIEW; STRUCTURE ACTIVITY RELATION;

ANIMALS; BINDING SITES; ENZYME INHIBITORS; HUMANS; PROTEIN-TYROSINE-PHOSPHATASE; SUBSTRATE SPECIFICITY;

EID: 0036181649     PISSN: 03621642     EISSN: None     Source Type: Book Series    
DOI: 10.1146/annurev.pharmtox.42.083001.144616     Document Type: Review

References (99)

1. The regulation of protein function by multisite phosphorylation - A 25 year update
2. Transforming gene product of Rous sarcoma virus phosphorylates tyrosine
3. Signaling-2000 and beyond
4. Protein tyrosine phosphatases in signal transduction
5. Form, function, and regulation of protein tyrosine phosphatases and their involvement in human diseases
6. Genetic analysis of protein tyrosine phosphatases
7. Protein tyrosine phosphatases: Prospects for therapeutics
8. Increased insulin sensitivity and obesity resistance in mice lacking the protein tyrosine phosphatase-1B gene
9. Increased energy expenditure, decreased adiposity, and tissue-specific insulin sensitivity in proteintyrosine phosphatase 1B-deficient mice
10. Protein-tyrosine phosphatases: Biological function, structural characteristics, and mechanism of catalysis
11. Initial sequencing and analysis of the human genome
12. Structural studies of reversible protein phosphorylation and protein phosphatases
13. Structural basis for phosphotyrosine peptide recognition by protein tyrosine phosphatase 1B
14. The active-site specificity of the Yersinia protein-tyrosine phosphatase
15. Crystal structure of the dual specificity protein phosphatase VHR
16. Crystal structure of the MAPK phosphatase Pyst1 catalytic domain and implications for regulated activation
17. Crystal structure of Yersinia protein tyrosine phosphatase at 2.5 Å and the complex with tungstate
18. Evidence for protein-tyrosine phosphatase catalysis proceeding via a cysteine-phosphate intermediate
19. Isolation and structural elucidation of a novel phosphocysteine intermediate in the LAR protein tyrosine phosphatase enzymatic pathway
20. Distinct functional roles of the two intracellular phosphatase like domains of the receptor-linked protein tyrosine phosphatases LCA and LAR
21. a of the active site cysteine and the function of the conserved histidine 402
22. Dissecting the catalytic mechanism of protein tyrosine phosphatases
23. Nature of the transition state of the protein-tyrosine phosphatase-catalyzed reaction
24. Probing the function of Asp 128 in the low molecular weight protein-tyrosine phosphatase catalyzed reaction. A pre-steady-state and steady-state kinetic investigation
25. Visualization of intermediate and transition-state structures in protein-tyrosine phosphatase catalysis
26. Impaired transition state complementarity in the hydrolysis of O-arylphosphorothioates by protein-tyrosine phosphatases
27. Does positive charge at the active site of a phosphatase cause a change in mechanism? The effect of the conserved arginine on the transition state for enzymatic phosphoryl transfer in the protein-tyrosine phosphatase from Yersinia
28. Molecular basis of substrate specificity of protein tyrosine phosphatase 1B
29. Probing the function of the invariant tryptophan in the flexible loop of the Yersinia proteintyrosine phosphatase
30. The effects on general acid catalysis from mutations of the invariant tryptophan and arginine residues in the protein-tyrosine phosphatase from Yersinia
31. Altering the nucleophile specificity of a protein-tyrosine phosphatase-catalyzed reaction: Probing the function of the invariant glutamine residues
32. A continuous spectrophotometric and fluorimetric assay for protein tyrosine phosphatase using phosphotyrosine containing peptides
33. Substrate specificity of the protein tyrosine phosphatases
34. Protein tyrosine phosphatase substrate specificity: The minimum size of the peptide and the positioning of the phosphotyrosine
35. Affinity selection from peptide libraries to determine substrate specificity of protein tyrosine phosphatases
36. Mapping the subsite preferences of protein tyrosine phosphatase PTP-1B using combinatorial chemistry approaches
37. Assessment of protein tyrosine phosphatse 1B substrate specificity using "inverse alanine scanning."
38. Structural basis of plasticity in protein tyrosine phosphatase 1B substrate recognition
39. Osmotic loading of neutralizing antibodies demonstrates a role for protein-tyrosine phosphatase 1B in negative regulation of the insulin action pathway
40. Protein-tyrosine phospharase 1B is a negative regulator of insulin- and insulin-like growth factor-I-stimulated signaling
41. Protein-tyrosine phosphatase 1B complexes with the insulin receptor in vivo and is tyrosine-phosphorylated in the presence of insulin
42. Tyrosine dephosphorylation and deactivation of insulin receptor substrate-1 by protein-tyrosine phosphatase 1B. Possible facilitation by the formation of a ternary complex with the Grb2 adaptor protein
43. Dynamics of protein-tyrosine phosphatases in rat adipocytes
44. c-erbB-2 protein expression
45. Overexpression of the tyrosine phosphatase PTP1B is associated with human ovarian carcinomas
46. Effect of protein tyrosine phosphatase 1B expression on transformation by the human neu oncogene
47. Protein tyrosine phosphatase 1B negatively regulates integrin signaling
48. Expression of a protein tyrosine phosphatase in normal and v-src-transformed mouse 3T3 fibroblasts
49. Identification of protein-tyrosine phosphatase 1B as the major tyrosine phosphatase activity capable of dephosphorylating and activating c-Src in several human breast cancer cell lines
50. Protein tyrosine phosphatase 1B interacts with and is tyrosine phosphorylated by the epidermal growth factor receptor
51. Development of "substrate-trapping" mutants to identify physiological substrates of protein tyrosine phosphatases
52. Protein tyrosine phosphatase 1B antagonizes signalling by oncoprotein tyrosine kinase p210 bcr-abl in vivo
53. The nonreceptor protein tyrosine phosphatase PTP1B binds to the cytoplasmic domain of N-cadherin and regulates the cadherin-actin linkage
54. Cas
55. A cytosolic protein-tyrosine phosphatase PTP1B specifically dephosphorylates and deactivates prolactin-activated STAT5a and STAT5b
56. The nontrans-membrane tyrosine phosphatase PTP-1B localizes to the endoplasmic reticulum via its 35 amino acid C-terminal sequence
57. Differential activities of protein-tyrosine phosphatases in intact cells
58. Dephosphorylation of Cdk2 Thrl60 by the cyclin-dependent kinase-interacting phosphatase KAP in the absence of cyclin
59. Phosphoprotein-protein interactions revealed by the crystal structure of kinase-associated phosphatase in complex with phosphoCDK2
60. Mechanism of mitogen-activated protein kinase phosphatase-3 activation by ERK2
61. Purification and kinetic characterization of the mitogen-activated protein kinase phosphatase rVH6
62. The mechanism of dephosphorylation of extracellular signal-regulated kinase 2 by mitogen-actived protein kinase phosphatase 3
63. Mechanistic basis for catalytic activation of mitogen-activated protein kinase phosphatase 3 by extracellular signal-regulated kinase
64. Catalytic activation of the phosphatase MKP-3 by ERK2 mitogen-activated protein kinase
65. Multiple regions of MAP kinase phosphatase 3 are involved in its recognition and activation by ERK2
66. Specificity of T-cell protein tyrosine phosphatase toward phosphorylated synthetic peptides
67. Protein tyrosine phosphatases: Structure, mechanism and inhibitor discovery
68. Preparation of fluoro- and hydroxy-4-(phosphonomethyl)-D,L-phenylalanine suitable protected for solid-phase synthesis of peptides containing hydrolytically stable analogues of O-phosphotyrosine
69. Why is phosphono-difluoromethyl phenylalanine a more potent inhibiting moiety than phosphonomethyl phenylalanine toward protein-tyrosine phosphatases?
70. Thermodynamic study of ligand binding to proteintyrosine phosphatase 1B and its substrate-trapping mutants
71. Small molecule interactions with protein-tyrosine phosphatase PTP1B and their use in inhibitor design
72. Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward GRB2 SH2 domains
73. Protein kinase inhibitors: The tyrosine-specific protein kinases
74. The development and therapeutic potential of protein kinase inhibitors
75. Potent low molecular weight substrates for protein-tyrosine phosphatase
76. Identification of a second aryl phosphate-binding site in protein-tyrosine phosphatase 1B: A paradigm for inhibitor design
77. Potent non-peptidyl inhibitors of protein tyrosine phosphatase 1B
78. Potent and highly selective inhibitors of the protein tyrosine phosphatase 1B
79. [Difluro(phosphono)methyl]phenylalanine-containing peptide inhibitors of protein tyrosine phosphatases
80. Acquisition of a specific and potent PTP1B inhibitor from a novel combinatorial library and screening procedure
81. Structure-based design of an osteoclast-selective, nonpeptide src homology 2 inhibitor with in vivo antiresorptive activity
82. Protein-tyrosine phosphatase inhibition by a peptide containing the phosphotyrosyl mimetic, L-O-malonyltyrosine
83. Radio frequency tag encoded combinatorial library method for the discovery of tripeptide- substituted cinnamic acid inhibitors of the protein tyrosine phosphatase PTP1B
84. Enantioselective synthesis of nonphosphorous-containing phosphotyrosyl mimetics and their use in the preparation of tyrosine phosphatase inhibitory peptides
85. Structure-based discovery of small molecule inhibitors targeted to protein tyrosine phosphatase 1B
86. 2-(Oxalylamino)-benzoic acid is a general, competitive inhibitor of protein-tyrosine phosphatases
87. Utilization of a peptide lead for the discovery of a novel PTP1B-binding motif
88. Novel benzofuran and benzothiophene biphenyls as inhibitors of protein tyrosine phosphatase 1B with antihyperglycemic properties
89. Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin action
90. Structure-based design and synthesis of small molecule protein-tyrosine phosphatase 1B inhibitors
91. Structure-based design of a low molecular weight, nonphosphorus, nonpeptide, and highly selective inhibitor of proteintyrosine phosphatase 1B
92. PTP1B inhibition and antihyperglycemic activity of novel 11-aryl-benzo[b]naphtho[2,3-d]furans and 11-aryl-benzo[b]naphtho[2,3-d]thiophenes
93. Cdc25 phosphatases as potential human oncogenes
94. Role of Cdc25A phosphatase in human breast cancer
95. Synthesis and phosphatase inhibitory activity of analogs of sulfircin
96. Dysidiolide: A novel protein phosphatase inhibitor from the Caribbean sponge Dysidea etheria de Laubenfels
97. Cdc25 inhibition and cell cycle arrest by a synthetic thioalkyl vitamin K analogue
98. Identification of new Cdc25 dual specificity phosphatase inhibitors in a targeted small molecule array
99. Synthesis and biological activities of a novel group of steroidal derived inhibitors for human Cdc25A protein phosphatase