Substrate profiling of IGF-1R and InsR: Identification of a potent pentamer substrate

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 23, 2011, Pages 7030-7033

  Chapelat, Julien ^a   Berst, Frédéric ^a   Marzinzik, Andreas L ^a   Moebitz, Henrik ^a   Drueckes, Peter ^a   Fabbro, Doriano ^a   Trappe, Joerg ^a   Seebach, Dieter ^b  

^a NOVARTIS PHARMA AG   (Switzerland)

^b ETH ZURICH   (Switzerland)

Author keywords

Insulin like Growth Factor 1 Receptor; Michaelis Menten kinetics; Protein tyrosine kinases; Protein protein interactions; Substrate specificity

Indexed keywords

ADENOSINE TRIPHOSPHATE; INSULIN RECEPTOR; SOMATOMEDIN C RECEPTOR;

AMINO ACID SEQUENCE; ARTICLE; CRYSTAL STRUCTURE; ENZYME SPECIFICITY; PEPTIDE ANALYSIS; PROTEIN PHOSPHORYLATION; PROTEIN STRUCTURE; SOLID PHASE SYNTHESIS;

AMINO ACID SEQUENCE; CRYSTALLOGRAPHY, X-RAY; MODELS, MOLECULAR; MOLECULAR PROBES; MOLECULAR SEQUENCE DATA; PEPTIDES; PHOSPHORYLATION; PROTEIN BINDING; RECEPTOR, IGF TYPE 1; RECEPTOR, INSULIN; SUBSTRATE SPECIFICITY;

EID: 80255140366     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.09.101     Document Type: Article

References (10)

1. P. Cohen Nat. Rev. Drug Disc. 1 2002 309
2. D. Pouchain, J.J. Diaz-Mochon, L. Bialy, and M. Bradley Chem. Biol. 2 2007 810
3. A.J. Poot, J. van Ameijde, M. Slijper, A. van den Berg, R. Hilhorst, R. Ruijtenbeek, D.T.S. Rijkers, and R.M.J. Liskamp Chem. Bio. Chem. 10 2009 2042
4. X. Han, T. Sonoda, T. Mori, G. Yamanouchi, T. Yamaji, S. Shigaki, T. Niidome, and Y. Katayama Comb. Chem. High Throughput Screening 13 2010 777
5. N.W. Charter, L. Kauffman, R. Singh, and R.M. Eglen J. Biomol. Screen 11 2006 390 Briefly, ADP and phosphoenolpyruvate (PEP) are converted by pyruvate kinase to ATP and pyruvate, and pyruvate is oxidized by pyruvate oxidase to generate hydrogen peroxide. Peroxidase uses hydrogen peroxide to fuel the oxidation of Amplex Red to resorufin, the concentration of which is measured by standard fluorimetry
6. B. Xu, V.G. Bird, and W.T. Miller J. Biol. Chem. 270 1995 29825
7. I.M. Bell, S.M. Stirdivant, J. Ahern, J.C. Culberson, P.L. Darke, C.J. Dinsmore, R.A. Drakas, S.N. Gallicchio, S.L. Graham, D.C. Heimbrook, D.L. Hall, J. Hua, N.R. Kett, A.S. Kim, M. Kornienko, L.C. Kuo, S.K. Munshi, A.G. Quigley, J.C. Reid, B.W. Trotter, L.H. Waxman, T.M. Williams, and C.B. Zartman Biochemistry 44 2005 9430
8. The {3-[(methyl-Fmoc-amino)-methyl]-indol-1-yl}-acetyl AM resin was purchased from EMD Chemicals Inc.
9. 6-InsR and 1.5 mM ATP. Reactions were allowed to react for 60 min at 25 °C, then aliquoted and frozen at -80 °C
10. G. Siemeister, H. Al-Hasani, H.W. Klein, S. Kellnert, R. Streicher, W. Krone, and D. Müller-Wieland J. Biol. Chem. 270 1995 4870