CAS: 122520-90-5; (Z)-Tyrphostin A51

上下游产品

gallaldehyde 1,1,3-tricyano-2-amino-1-propene

📜3,4,5-三羟基苯甲醛,2-氨基-1-丙烯基-1,1,3-三甲腈置于哌啶体系中,用 乙醇 用作溶剂,以87%的收率获得酪氨酸磷酸化抑制剂a51
参考文献:Tyrphostins I: Synthesis And Biological Activity Of Protein Tyrosine Kinase Inhibitors
标题:Tyrphostins I: Synthesis And Biological Activity Of Protein Tyrosine Kinase Inhibitors
摘要:A Novel Class Of Low Molecular Weight Protein Tyrosine Kinase Inhibitors Is Described. These Compounds Constitute A Systematic Series Of Molecules With A Progressive Increase In Affinity Toward The Substrate Site Of The Egf Receptor Kinase Domain. These Competitive Inhibitors Also Effectively Block The Egf-Dependent Autophosphorylation Of The Receptor. The Potent Egf Receptor Kinase Blockers Examined Were Found To Competitively Inhibit The Homologous Insulin Receptor Kinase At 10(2)-10(3) Higher Inhibitor Concentrations In Spite Of The Significant Homology Between These Protein Tyrosine Kinases. These Results Demonstrate The Ability To Synthesize Selective Tyrosine Kinase Inhibitors. The Most Potent Egf Receptor Kinase Inhibitors Also Inhibit The Egf-Dependent Proliferation Of A431/clone 15 Cells With Little Or No Effect On Egf Independent Cell Growth. These Results Demonstrate The Potential Use Of Protein Tyrosine Kinase Inhibitors As Selective Antiproliferative Agents For Proliferative Diseases Caused By The Hyperactivity Of Protein Tyrosine Kinases. We Have Suggested The Name "Tyrphostins" For This Class Of Antiproliferative Compounds Which Act As Protein Tyrosine Kinase Blockers.
Doi:10.1021/jm00130A020

专利信息

专利号:US-11406709-B2
优先权日:2014-09-15
标 题 :Therapeutic and research application of PDCL3
发明人：RAHIMI NADER
权利人:UNIV BOSTON
摘要:Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

专利号:US-7052692-B1
优先权日:1997-09-02
标题:Role of tyrosine phosphorylation of a cellular protein in adeno-associated virus 2-mediated transgene expression
发明人：SRIVASTAVA ARUN; QING KEYUN; WANG XU-SHAN; PONNAZHAGAN SELVARANGAN; BAJPAI ANIL
权利人:ADVANCED RES & TECH INST
摘要:The present invention identifies a protein, designated the D-sequence-binding protein (D-BP), is phosphorylated at tyrosine residues and blocks AAV-mediated transgene expression in infected cells by inhibiting the leading strand viral DNA synthesis. More particularly, the present invention demonstrates that D-BP is phosphorylated by EGF-R protein tyrosine kinase. Methods of increasing transcription and promoting replication of transgenes exploiting this information are disclosed herein.