| http://purl.uniprot.org/citations/14632929 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/14632929 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/14632929 | http://www.w3.org/2000/01/rdf-schema#comment | "The cytoplasmic protein p60c-src, an ubiquitous non-receptor protein tyrosine kinase (PTK) is a potential anticancer target as it is over-expressed and/or constitutively active in several cancer types. In addition, the phenotype of c-src knock-out mice is consistent with osteopetrosis, which suggests that inhibitors against this enzyme may also be therapeutic for osteoporosis. Using a known peptide substrate for c-src, MIYKYYF, as a template, we have developed a series of pseudosubstrate-based peptide inhibitors. Structure-activity relationship studies have been performed on one of these inhibitors, CIYKYYF. In a kinase assay using YIYGSFK as the substrate, CIYKYY has been demonstrated to inhibit p60c-src, with an IC50 of 0.6 microm. Further truncation has led to the determination that even the smaller peptide, CIYK, is a moderately potent inhibitor with IC50 of 15 microm. Some improvement in inhibitory potency (IC50 = 11.8 microm) has been observed with the replacement of Tyr3 in CIYK with beta-phenylalanine (beta-Phe). The tetrapeptide CI(beta-Phe)K will be used as a lead compound for future development of peptidomimetics and small molecule inhibitors that have the capacity to penetrate the plasma membrane of intact cells."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.org/dc/terms/identifier | "doi:10.1046/j.1399-3011.2003.00094.x"xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.org/dc/terms/identifier | "doi:10.1046/j.1399-3011.2003.00094.x"xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/author | "Liu R."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/author | "Liu R."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/author | "Lam K.S."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/author | "Lam K.S."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/author | "Lou Q."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/author | "Lou Q."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/author | "Enstrom A.M."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/author | "Enstrom A.M."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/author | "Kamath J.R."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/author | "Kamath J.R."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/date | "2003"xsd:gYear |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/date | "2003"xsd:gYear |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/name | "J. Pept. Res."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/name | "J. Pept. Res."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/pages | "260-268"xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/pages | "260-268"xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/title | "Development and characterization of potent and specific peptide inhibitors of p60c-src protein tyrosine kinase using pseudosubstrate-based inhibitor design approach."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/title | "Development and characterization of potent and specific peptide inhibitors of p60c-src protein tyrosine kinase using pseudosubstrate-based inhibitor design approach."xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/volume | "62"xsd:string |
| http://purl.uniprot.org/citations/14632929 | http://purl.uniprot.org/core/volume | "62"xsd:string |