pf-3758309 and Triple-Negative-Breast-Neoplasms

pf-3758309 has been researched along with Triple-Negative-Breast-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for pf-3758309 and Triple-Negative-Breast-Neoplasms

Article	Year
Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors. Journal of medicinal chemistry, 2014, Feb-13, Volume: 57, Issue:3 Structure-based methods were used to design a potent and highly selective group II p21-activated kinase (PAK) inhibitor with a novel binding mode, compound 17. Hydrophobic interactions within a lipophilic pocket past the methionine gatekeeper of group II PAKs approached by these type I 1/2 binders were found to be important for improving potency. A structure-based hypothesis and strategy for achieving selectivity over group I PAKs, and the broad kinome, based on unique flexibility of this lipophilic pocket, is presented. A concentration-dependent decrease in tumor cell migration and invasion in two triple-negative breast cancer cell lines was observed with compound 17. Topics: Alkynes; Antineoplastic Agents; Benzimidazoles; Binding Sites; Cell Line, Tumor; Cell Movement; Cell Survival; Drug Screening Assays, Antitumor; Female; Humans; p21-Activated Kinases; Pyrimidines; Structure-Activity Relationship; Triple Negative Breast Neoplasms	2014

Article

Year

Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.

Journal of medicinal chemistry, 2014, Feb-13, Volume: 57, Issue:3

Structure-based methods were used to design a potent and highly selective group II p21-activated kinase (PAK) inhibitor with a novel binding mode, compound 17. Hydrophobic interactions within a lipophilic pocket past the methionine gatekeeper of group II PAKs approached by these type I 1/2 binders were found to be important for improving potency. A structure-based hypothesis and strategy for achieving selectivity over group I PAKs, and the broad kinome, based on unique flexibility of this lipophilic pocket, is presented. A concentration-dependent decrease in tumor cell migration and invasion in two triple-negative breast cancer cell lines was observed with compound 17.

Topics: Alkynes; Antineoplastic Agents; Benzimidazoles; Binding Sites; Cell Line, Tumor; Cell Movement; Cell Survival; Drug Screening Assays, Antitumor; Female; Humans; p21-Activated Kinases; Pyrimidines; Structure-Activity Relationship; Triple Negative Breast Neoplasms

2014