Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening

Acta Pharmacologica Sinica

Volumn 29, Issue 2, 2008, Pages 278-284

  Shi, Lei ^a   Yu, Hai Ping ^a   Zhou, Yue Yang ^a   Du, Jun Qin ^a   Shen, Qiang ^a   Li, Jing Ya ^a   Li, Jia ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

Author keywords

Competitive inhibitor; High throughput screening; Insulin receptor; Phosphoryaltion; PTP1B

Indexed keywords

PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR;

ANIMAL CELL; ARTICLE; CATALYSIS; CELL FUNCTION; DRUG STRUCTURE; HIGH THROUGHPUT SCREENING; NONHUMAN; NUCLEOTIDE SEQUENCE; PROTEIN ANALYSIS; PROTEIN DOMAIN;

ANIMALS; CATALYSIS; CHO CELLS; CRICETINAE; CRICETULUS; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HUMANS; PHOSPHORYLATION; PROTEIN TYROSINE PHOSPHATASE, NON-RECEPTOR TYPE 1; TYROSINE;

EID: 38749150385     PISSN: 16714083     EISSN: 17457254     Source Type: Journal    
DOI: 10.1111/j.1745-7254.2008.00737.x     Document Type: Article

References (18)

1. Lee JH, Reed DR, Li WD, Xu W, Joo EJ, Kilker RL, et al. Genome scan for human obesity and linkage to markers in 20q13. Am J Hum Genet 1999 64 : 196 209.
2. Di Paola R, Frittitta L, Miscio G, Bozzali M, Barratta R, Centra M, et al. A variation in 30 UTR of hPTP1B increases specific gene expression and associates with insulin resistance. Am J Hum Genet 2002 70 : 806 12.
3. Mok A, Cao H, Zinman B, Hanley AJ, Harris SB, Kennedy BP, et al. A single nucleotide polymorphism in protein tyrosine phosphatase PTP1B is associated with protection from diabetes or impaired glucose tolerance in Oji-Cree. J Clin Endocrinol Metab 2002 87 : 724 7.
4. Echwald SM, Bach H, Vestergaard H, Richelsen B, Kristensen K, Drivsholm T, et al. A P387L variant in protein tyrosine phos-phatase-1B (PTP1B) is associated with type 2 diabetes and impaired serine phosphorylation of PTP1B in vitro. Diabetes 2002 51 : 1 6.
5. Elchebly M, Payette P, Michaliszyn E, Cromlish W, Collins S, Loy AL, et al. Increased insulin sensitivity and obesity resistance in mice lacking the protein tyrosine phosphatase-1B gene. Science 1999 283 : 1544 8.
6. Klaman LD, Boss O, Peroni OD, Kim JK, Martino JL, Zabolotny JM, et al. Increases energy expenditure, decreased adiposity, and tissue-specific insulin sensitivity in protein-tyrosine phosphatase 1B-deficient mice. Mol Cell Biol 2000 20 : 5479 89.
7. Wu X, Hoffstedt J, Deeb W, Singh R, Sedkova N, Zilbering A, et al. Depot-specific variation in protein tyrosine phosphatases activities in human omental and subcutaneous adipose tissue: a potential contribution to differential insulin sensitivity. J Clin Endocrinol Metab 2001 86 : 5973 80.
8. Ahmad F, Considine RV, Bauer TL, Ohannesian JP, Marco CC, Goldstein BJ, et al. Improved sensitivity to insulin in obese subjects following weight loss is accompanied by reduced protein tyrosine phosphatase in adipose tissue. Metabolism 1997 46 : 1140 5.
9. Chen H, Cong LN, Li Y, Yao ZJ, Wu L, Zhang ZY, et al. A phosphotyrosyl mimetic peptide reverses impairment of insulin-stimulated translocation of GLUT4 caused by overexpression of PTP-1B in rat adipose cells. Biochemistry 1999 38 : 384 9.
10. Venable CL, Frevert EU, Kim YB, Fisher BM, Kamatkar S, Nee BG, et al. Overexpression of protein tyrosine phosphatase 1B in adipocytes inhibits insulin-stimulated phosphoinositide 3-kinase activity without altering glucose transport or Akt/protein kinase B activation. J Biol Chem 2000 275 : 18318 26.
11. Ukkola O, Santaniemi M. Protein tyrosine phosphatase 1B: a new target for the treatment of obesity and associated co-morbidities. J Intern Med 2002 251 : 467 75.
12. Zhang JH, Chung TD, Oldenburg KR. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999 4 : 67 73.
13. Egawa K, Maegawa H, Kashiwagi A. Protein-tyrosine phos-phatase-1B negatively regulates insulin signaling in L6 myocytes and Fao hepatoma cells. J Biol Chem 2001 276 : 10207 11.
14. Zabolotny JM, Haj FG, Kahn BB. Transgenic overexpression of PTP1B in muscle causes insulin resistance but overexpression with LAR does not additively impair insulin action. J Biol Chem 2004 279 : 24844 51.
15. Clampit JE, Meuth JL, Rondinone CM. Reduction of protein-tyrosine phosphatase-1B increase insulin signaling in FAO hepatoma cells. J Biol Chem 2003 300 : 261 7.
16. Ahmad F, Li PM, 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 170 : 20503 8.
17. Issad T, Boute N, Boubekeur S, Lacasa D. Interaction of PTP1B with the insulin receptor precursor during its biosynthesis in the endoplasmic reticulum. Biochemie 2005 87 : 111 6.
18. Xie LP, Lee SY, Zhang ZY. Cellular effects of small molecule PTP1B inhibitors on insulin signaling. Biochemistry 2003 42 : 12792 804.