pubmed-article:10479306 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:10479306 | lifeskim:mentions | umls-concept:C0030956 | lld:lifeskim |
pubmed-article:10479306 | lifeskim:mentions | umls-concept:C0070948 | lld:lifeskim |
pubmed-article:10479306 | lifeskim:mentions | umls-concept:C1333707 | lld:lifeskim |
pubmed-article:10479306 | lifeskim:mentions | umls-concept:C0282534 | lld:lifeskim |
pubmed-article:10479306 | lifeskim:mentions | umls-concept:C0332256 | lld:lifeskim |
pubmed-article:10479306 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
pubmed-article:10479306 | lifeskim:mentions | umls-concept:C0205250 | lld:lifeskim |
pubmed-article:10479306 | lifeskim:mentions | umls-concept:C0205117 | lld:lifeskim |
pubmed-article:10479306 | lifeskim:mentions | umls-concept:C0920591 | lld:lifeskim |
pubmed-article:10479306 | pubmed:issue | 18 | lld:pubmed |
pubmed-article:10479306 | pubmed:dateCreated | 1999-10-14 | lld:pubmed |
pubmed-article:10479306 | pubmed:abstractText | A series of small peptides with the sequence mAZ-pTyr-Xaa-Asn-NH(2), where Xaa denotes alpha-methylphosphotyrosine or its carboxylic mimetics, were synthesized as inhibitors of the Grb2 SH2 domain. Peptide 3 with (alpha-Me)pTyr as Xaa has the highest affinity for Grb2 (K(d) = 3 +/- 1 nM) and exhibits to date the best inhibitory activity (IC(50) = 11 +/- 1 nM) to displace PSpYVNVQN-Grb2 interaction in an ELISA test. The lower affinities of peptides with (alpha-Me)Tyr, (alpha-Me)Phe(4-CO(2)H), or (alpha-Me)Phe(4-CH(2)CO(2)H) as Xaa demonstrate the importance of a double charged phosphate group at the pY+1 position. Molecular modeling showed additional hydrogen bond interactions provided by the (alpha-Me)pTyr residue with the Grb2 SH2 domain. These results thus show that the effect of hydrophobic pY+1 residues, initially put forth to increased the binding affinities, can be further enhanced by a (-Me)pTyr residue which has both hydrophobic and hydrophilic properties. | lld:pubmed |
pubmed-article:10479306 | pubmed:language | eng | lld:pubmed |
pubmed-article:10479306 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10479306 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:10479306 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10479306 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10479306 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10479306 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10479306 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:10479306 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:10479306 | pubmed:month | Sep | lld:pubmed |
pubmed-article:10479306 | pubmed:issn | 0022-2623 | lld:pubmed |
pubmed-article:10479306 | pubmed:author | pubmed-author:RoquesB PBP | lld:pubmed |
pubmed-article:10479306 | pubmed:author | pubmed-author:LinW JWJ | lld:pubmed |
pubmed-article:10479306 | pubmed:author | pubmed-author:VidalMM | lld:pubmed |
pubmed-article:10479306 | pubmed:author | pubmed-author:GarbayCC | lld:pubmed |
pubmed-article:10479306 | pubmed:author | pubmed-author:GreshNN | lld:pubmed |
pubmed-article:10479306 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:10479306 | pubmed:day | 9 | lld:pubmed |
pubmed-article:10479306 | pubmed:volume | 42 | lld:pubmed |
pubmed-article:10479306 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:10479306 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:10479306 | pubmed:pagination | 3737-41 | lld:pubmed |
pubmed-article:10479306 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
pubmed-article:10479306 | pubmed:meshHeading | pubmed-meshheading:10479306... | lld:pubmed |
pubmed-article:10479306 | pubmed:meshHeading | pubmed-meshheading:10479306... | lld:pubmed |
pubmed-article:10479306 | pubmed:meshHeading | pubmed-meshheading:10479306... | lld:pubmed |
pubmed-article:10479306 | pubmed:meshHeading | pubmed-meshheading:10479306... | lld:pubmed |
pubmed-article:10479306 | pubmed:meshHeading | pubmed-meshheading:10479306... | lld:pubmed |
pubmed-article:10479306 | pubmed:meshHeading | pubmed-meshheading:10479306... | lld:pubmed |
pubmed-article:10479306 | pubmed:meshHeading | pubmed-meshheading:10479306... | lld:pubmed |
pubmed-article:10479306 | pubmed:meshHeading | pubmed-meshheading:10479306... | lld:pubmed |
pubmed-article:10479306 | pubmed:meshHeading | pubmed-meshheading:10479306... | lld:pubmed |
pubmed-article:10479306 | pubmed:year | 1999 | lld:pubmed |
pubmed-article:10479306 | pubmed:articleTitle | Small peptides containing phosphotyrosine and adjacent alphaMe-phosphotyrosine or its mimetics as highly potent inhibitors of Grb2 SH2 domain. | lld:pubmed |
pubmed-article:10479306 | pubmed:affiliation | Département de Pharmacochimie Moléculaire et Structurale, INSERM U266-CNRS UMR 8600, UFR des Sciences Pharmaceutiques et Biologiques, 4, avenue de l'Observatoire, 75270 Paris Cedex 06, France. | lld:pubmed |
pubmed-article:10479306 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:10479306 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:10479306 | lld:chembl |
http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:10479306 | lld:pubmed |
http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:10479306 | lld:pubmed |