1992
DOI: 10.1111/j.1432-1033.1992.tb17196.x
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Kinase inhibition by a phosphorylated peptide corresponding to the major insulin receptor autophosphorylation domain

Abstract: We studied the inhibitory effect of non-phosphorylated and triphosphorylated synthetic peptides, corresponding to amino acids 1143-1155 of the insulin proreceptor (domain 1151) on autophosphorylation and kinase of the insulin receptor. Tyrosine-phosphorylated peptides were synthesized using the N-(9-fluorenylmethoxycarbonyl)-O-dibenzylphosphono-~-tyr0~~ne.The triphosphorylated peptide (1 1 51-P3) and the non-phosphorylated peptide (1 151-NP), respectively, inhibited insulin receptor autophosphorylation by 65% … Show more

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Cited by 5 publications
(4 citation statements)
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References 42 publications
(10 reference statements)
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“…Peptide synthesis was carried out on a fluorenemethoxycarbonyl (Fmoc) PAL-PEG resin, or a Fmoc Arg(Pmc)-PEG resin (Millipore), by Fmoc strategy on an automatic apparatus (9050 Pepsynthesiser, Milligen). Peptide synthesis was performed as described elsewhere [9]. Then, the crude peptide-amide was precipitated with ether, filtered and dried in a desiccator.…”
Section: Peptide Synthesmentioning
confidence: 99%
“…Peptide synthesis was carried out on a fluorenemethoxycarbonyl (Fmoc) PAL-PEG resin, or a Fmoc Arg(Pmc)-PEG resin (Millipore), by Fmoc strategy on an automatic apparatus (9050 Pepsynthesiser, Milligen). Peptide synthesis was performed as described elsewhere [9]. Then, the crude peptide-amide was precipitated with ether, filtered and dried in a desiccator.…”
Section: Peptide Synthesmentioning
confidence: 99%
“…The phosphorylated peptide RRDIYETDYpYRK (YYpY) was synthesised using the FmocTyr-0-PO,-(benzyl), method (Chavanieu et al, 1992). Subsequent deblocking and HPLC purification of all peptides were performed as previously described (Chavanieu et al, 1991(Chavanieu et al, , 1992, except that the anion-exchange chromatography step was omitted.…”
Section: Peptide Synthesis and Purificationmentioning
confidence: 99%
“…The phosphorylated peptide RRDIYETDYpYRK (YYpY) was synthesised using the FmocTyr-0-PO,-(benzyl), method (Chavanieu et al, 1992). Subsequent deblocking and HPLC purification of all peptides were performed as previously described (Chavanieu et al, 1991(Chavanieu et al, , 1992, except that the anion-exchange chromatography step was omitted. The composition of each peptide was confirmed after acid hydrolysis using a Beckman Model 6300 amino acid analyser, and additionally analysed by electrospray mass spectrometry (VG TRIO 2000, Fison Instruments) as well as by two-dimensional NMR methods.…”
Section: Peptide Synthesis and Purificationmentioning
confidence: 99%
“…This region is located close to the active site in known PTK structures and has been dubbed as the regulatory segment in kinase activation (Marshall, 1994). In the case of the insulin receptor, the corresponding peptide is indeed an effective inhibitor of autophosphorylation (Cobb et al, 1989;Shoelson et al, 1989;Chavanieu et al, 1992). Two further sites of tyrosine autophosphorylation are located in the IRPTK C-terminal tail region (Tyr1328 and Tyr1334).…”
mentioning
confidence: 99%