The structure of PTP-1B in complex with a peptide inhibitor reveals an alternative binding mode for bisphosphonates

Biochemistry

Volumn 41, Issue 29, 2002, Pages 9043-9051

  Asante Appiah, Ernest ^a   Patel, Sangita ^b   Dufresne, Claude ^a   Roy, Patrick ^a   Wang, Qingping ^a   Patel, Vira ^a   Friesen, Richard W ^a   Ramachandran, Chidambaram ^a   Becker, Joseph W ^b   Leblanc, Yves ^a   Kennedy, Brian P ^a   Scapin, Giovanna ^b  

^a MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DIABETES;

AMINO ACIDS; CRYSTAL STRUCTURE; MUTAGENESIS; PHOSPHORUS COMPOUNDS; PROTEINS;

BIOCHEMISTRY;

ARGININE; ASPARTIC ACID; N BENZOYLGLUTAMYL[4 PHOSPHONO(DIFLUOROMETHYL)]PHENYLALANINE[4 PHOSPHONO(DIFLUOROMETHYL)]PHENYLALANINAMIDE; PHENYLALANINE DERIVATIVE; PHOSPHONIC ACID DERIVATIVE; PROTEIN INHIBITOR; PROTEIN TYROSINE PHASPHATASE INHIBITOR; PROTEIN TYROSINE PHOSPHATASE; PROTEIN TYROSINE PHOSPHATASE 1B; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ARTICLE; COMPLEX FORMATION; CRYSTAL STRUCTURE; DRUG STRUCTURE; NON INSULIN DEPENDENT DIABETES MELLITUS; PRIORITY JOURNAL; PROTEIN PROTEIN INTERACTION; PROTEIN STRUCTURE; SITE DIRECTED MUTAGENESIS;

BASE SEQUENCE; DIPEPTIDES; DIPHOSPHONATES; DNA PRIMERS; ENZYME INHIBITORS; MUTAGENESIS, SITE-DIRECTED; PHOSPHONIC ACIDS; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN-TYROSINE-PHOSPHATASE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 18444370551     PISSN: 00062960     EISSN: None     Source Type: Journal    
DOI: 10.1021/bi0259554     Document Type: Article

References (44)

1. PPAR-gamma agonists: Therapeutic role in diabetes, inflammation and cancer
2. Protein tyrosine phosphatases: Their role in insulin action and potential as drug targets
3. Increased insulin sensitivity and obesity resistance in mice lacking the protein tyrosine phosphatase 1B gene
4. Increased energy expenditure, decreased adiposity, and tissue-specific insulin sensitivity in protein tyrosine phosphatase 1B-deficient mice
5. [Difluoro(phosphono)methyl]phenylalanine-containing inhibitors of protein tyrosine phosphatases
6. Potent and highly selective inhibitors of Protein tyrosine phosphatase 1B
7. 2-(Oxalylamino)-benzoic acid is a general, competitive inhibitor of protein tyrosine phosphatases
8. Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin action
9. Novel phosphate mimetics for the design of nonpeptidyl inhibitors of protein tyrosine phosphatases
10. Synthesis and biological activity of a novel class of small molecular weight peptidomimetic competitive inhibitors of protein tyrosine phosphatase 1B
11. Potent non-peptidyl inhibitors of ptotein tyrosine phosphatase 1B
12. Naphthalene-bis-[alpha, alpha-difluoromethylenephosphonates] as potent inhibitors of protein tyrosine phosphatases
13. PTP1B inhibition and antihyperglycemic 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
14. Inhibition of protein tyrosine phosphatases by low-molecularweight S-nitrosothiols and S-nitrosylated human serum albumin
15. Synthesis and PTP1B inhibition of novel 4-aryl-1-oxa-9-thiacyclopenta[b]fluorenes
16. Potent inhibition of insulin receptor dephosphorylation by a hexamer peptide containing the phosphotyrosyl mimetic F2Pmp
17. Identification of a second aryl phosphate-binding site in protein tyrosine-phosphatse 1B: A pardigm for inhibitor design
18. Molecular Basis for dephosphorylation of the active segment of the insulin receptor by protein tyrosine phosphatase 1B
19. The YRD motif is a major determinant of substrate and inhibitor specificity in T-cell protein tyrosine phosphatase
20. Develeopment of a robust scintillation proximity assay for protein tyrosine phosphatase 1B using the catalytically inactive (C215S) mutant
21. Processing of x-ray diffraction data collected in oscillation mode
22. Data processing in macromolecular crystallography
23. Solvent content of protein crystals
24. AMoRe: An automated package for molecular replacement
25. Crystallographic R-factor refinement by Molecular Dynamics
26. The free-R value: A novel statistical quantity for assesing the accuracy of crystal structures
27. Phase improvement by cross-validated Density Modification
28. Checking your imagination: Applications of the free R value
29. Improved methods for building protein models in electron density maps and the location of errors in these models
30. Electron- density Map Interpretation
31. The CCP4 suite: Programs for protein crystallography
32. Crystallography & NMR system: A new software suite for macromolecular structure determination
33. Torsion angle dynamics: Reduced variable conformational sampling enhances crystallographic structure refinement
34. PROCHECK: A programme to check the stereochemical quality of protein structure coordinates
35. Molecular basis for substrate specificity of protein tyrosinephosphatase 1B
36. Structural basis for phosphotyrosine peptide recognition by protein tyrosine phosphatase 1B
37. Structure of protein tyrosine phosphatase 1B in complex with inhibitors bearing two phosphotyrosine mimetics
38. Structural basis of plasticity in protein tyrosine phosphatase 1b substrate recognition
39. Assessment of protein tyrosine phosphatase 1B substrate specificity using "inverse alanine scanning"
40. TYK2 and JAK2 are substrates of protein tyrosine phosphatase 1B
41. Structure-based design of a low molecular weight, nonphosphorus, non-peptide, and highly selective inhibitor of protein tyrosine phosphatase 1B