The Experts below are selected from a list of 119580 Experts worldwide ranked by ideXlab platform
Siu Wa Tang - One of the best experts on this subject based on the ideXlab platform.
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Tyrosine Kinase Inhibitors regulate serotonin uptake in platelets
European journal of pharmacology, 1995Co-Authors: Daiga M. Helmeste, Siu Wa TangAbstract:Uptake of tritiated serotonin into human platelets was found to be rapidly inhibited by the Tyrosine Kinase Inhibitors, genistein and methyl 2,5-dihydroxycinnamate. Binding studies indicated that uptake inhibition did not correlate with direct binding of these Inhibitors to the transporter. Chelation of mobilizable intracellular Ca2+ did not inhibit the effects of genistein on uptake. These results suggest a more direct, non-Ca2+ mediated effect of Tyrosine Kinase Inhibitors on uptake.
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Tyrosine Kinase Inhibitors regulate serotonin uptake in platelets
European Journal of Pharmacology, 1995Co-Authors: Daiga M. Helmeste, Siu Wa TangAbstract:Abstract Uptake of tritiated serotonin into human platelets was found to be rapidly inhibited by the Tyrosine Kinase Inhibitors, genistein and methyl 2,5-dihydroxycinnamatc. Binding studies indicated that uptake inhibition did not correlte with direct binding of these Inhibitors to the transporter. Chelation of mobilizable intracellular Ca2+ did not inhibit the effects of genistein on uptake. These results suggest a more direct, non-Ca2+ mediated effect of Tyrosine Kinase Inhibitors on uptake.
Anand C. Burman - One of the best experts on this subject based on the ideXlab platform.
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Synthesis of Quinazolines as Tyrosine Kinase Inhibitors
Anti-cancer Agents in Medicinal Chemistry, 2009Co-Authors: Sanjay K Srivastava, Shiv K. Agarwal, Rama Mukherjee, Vivek Kumar, Anand C. BurmanAbstract:In the present review, the discovery and development of quinazoline as Tyrosine Kinase Inhibitors has been described. The synthesis of most potent quinazoline Inhibitors of EGFR, VEGFR and PDGRF has been discussed. Structure activity relationship for quinazoline as Tyrosine Kinase Inhibitors has been established. It was found that C-4, C-6 and C-7 positions in quinazoline are appropriate sites for designing new Tyrosine Kinase Inhibitors. This review should help the medicinal chemist in designing more effective Tyrosine Kinase Inhibitors.
Zhou Hua - One of the best experts on this subject based on the ideXlab platform.
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Progress on the research of protein Tyrosine Kinase Inhibitors
Chinese Journal of Medicinal Chemistry, 2010Co-Authors: Zhou HuaAbstract:Protein Tyrosine Kinase Inhibitors are a kind of molecular-targeted agents acting on the cell signal transduction pathway,and play their antitumor role in the appropriate targets.More than ten of such Inhibitors have been revealed to be potent on solid tumors and approved by FDA.Recent advances on protein Tyrosine Kinase Inhibitors are reviewed in this paper.
Neeltje Steeghs - One of the best experts on this subject based on the ideXlab platform.
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Tyrosine Kinase Inhibitors and QTc intervals: A class effect.
Journal of Clinical Oncology, 2014Co-Authors: Jacqueline S. L. Kloth, Anna Pagani, Michiel C. Verboom, Alberto Malovini, Carlo Napolitano, Willem H.j. Kruit, Stefan Sleijfer, Neeltje Steeghs, Alberto Zambelli, Ron H.j. MathijssenAbstract:2590 Background: Tyrosine Kinase Inhibitors (TKIs) are reported to be associated with prolongation of the QTc interval on the ECG. QTc interval prolongation increases the risk for life threatening ...
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Tyrosine Kinase Inhibitors and QTc intervals: A class effect.
Journal of Clinical Oncology, 2014Co-Authors: Jacqueline S. L. Kloth, Anna Pagani, Michiel C. Verboom, Alberto Malovini, Carlo Napolitano, Willem H.j. Kruit, Stefan Sleijfer, Neeltje Steeghs, Alberto Zambelli, Ron H.j. MathijssenAbstract:2590 Background: Tyrosine Kinase Inhibitors (TKIs) are reported to be associated with prolongation of the QTc interval on the ECG. QTc interval prolongation increases the risk for life threatening ...
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small molecule Tyrosine Kinase Inhibitors in the treatment of solid tumors an update of recent developments
Annals of Surgical Oncology, 2007Co-Authors: Neeltje Steeghs, Johan W R Nortier, Hans GelderblomAbstract:Small molecule Tyrosine Kinase Inhibitors (TKIs) are developed to block intracellular signaling pathways in tumor cells, leading to deregulation of key cell functions such as proliferation and differentiation. Over 25 years ago, Tyrosine Kinases were found to function as oncogenes in animal carcinogenesis; however, only recently TKIs were introduced as anti cancer drugs in human cancer treatment. Tyrosine Kinase Inhibitors have numerous good qualities. First, in many tumor types they tend to stabilize tumor progression and may create a chronic disease state which is no longer immediately life threatening. Second, side effects are minimal when compared to conventional chemotherapeutic agents. Third, synergistic effects are seen in vitro when TKIs are combined with radiotherapy and/or conventional chemotherapeutic agents. In this article, we will give an update of the Tyrosine Kinase Inhibitors that are currently registered for use or in an advanced stage of development, and we will discuss the future role of TKIs in the treatment of solid tumors. The following TKIs are reviewed: Imatinib (Gleevec/Glivec), Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva), Lapatinib (GW-572016, Tykerb), Canertinib (CI-1033), Sunitinib (SU 11248, Sutent), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).
Daiga M. Helmeste - One of the best experts on this subject based on the ideXlab platform.
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Tyrosine Kinase Inhibitors regulate serotonin uptake in platelets
European journal of pharmacology, 1995Co-Authors: Daiga M. Helmeste, Siu Wa TangAbstract:Uptake of tritiated serotonin into human platelets was found to be rapidly inhibited by the Tyrosine Kinase Inhibitors, genistein and methyl 2,5-dihydroxycinnamate. Binding studies indicated that uptake inhibition did not correlate with direct binding of these Inhibitors to the transporter. Chelation of mobilizable intracellular Ca2+ did not inhibit the effects of genistein on uptake. These results suggest a more direct, non-Ca2+ mediated effect of Tyrosine Kinase Inhibitors on uptake.
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Tyrosine Kinase Inhibitors regulate serotonin uptake in platelets
European Journal of Pharmacology, 1995Co-Authors: Daiga M. Helmeste, Siu Wa TangAbstract:Abstract Uptake of tritiated serotonin into human platelets was found to be rapidly inhibited by the Tyrosine Kinase Inhibitors, genistein and methyl 2,5-dihydroxycinnamatc. Binding studies indicated that uptake inhibition did not correlte with direct binding of these Inhibitors to the transporter. Chelation of mobilizable intracellular Ca2+ did not inhibit the effects of genistein on uptake. These results suggest a more direct, non-Ca2+ mediated effect of Tyrosine Kinase Inhibitors on uptake.
