Thiazolidine-diones. Biochemical and biological activity of a novel class of tyrosine protein kinase inhibitors
Various derivatives of thiazolidine-diones have been identified as tyrosine protein kinase inhibitors. The epidermal growth factor (EGF) receptor kinase and c-src kinase were inhibited in vitro with IC50 values in the range of 1-7 microM. The v-abl tyrosine protein kinase was not inhibited by thiazo...
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| Veröffentlicht in: | The Journal of biological chemistry 1990-12, Vol.265 (36), p.22255-22261 |
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| container_title | The Journal of biological chemistry |
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| creator | Geissler, J F Traxler, P Regenass, U Murray, B J Roesel, J L Meyer, T McGlynn, E Storni, A Lydon, N B |
| description | Various derivatives of thiazolidine-diones have been identified as tyrosine protein kinase inhibitors. The epidermal growth factor (EGF) receptor kinase and c-src kinase were inhibited in vitro with IC50 values in the range of 1-7 microM. The v-abl tyrosine protein kinase was not inhibited by thiazolidine-diones. Inhibition was found to be specific for tyrosine protein kinases. Inhibition of serine/threonine protein kinases was not observed. The active derivatives were shown to inhibit EGF-induced receptor autophosphorylation, either in vitro or in intact cells, and were also found to inhibit growth of the EGF-dependent BALB/MK and A431 cell lines (IC50 1-3 microM). Growth of the interleukin-3-dependent myeloid cell line FDC-P1 was inhibited with equal efficiency. Thus, in these cell lines, members of the c-src kinase family are also potential targets for inhibition by the compounds. |
| doi_str_mv | 10.1016/S0021-9258(18)45697-9 |
| format | Article |
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The active derivatives were shown to inhibit EGF-induced receptor autophosphorylation, either in vitro or in intact cells, and were also found to inhibit growth of the EGF-dependent BALB/MK and A431 cell lines (IC50 1-3 microM). Growth of the interleukin-3-dependent myeloid cell line FDC-P1 was inhibited with equal efficiency. 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Psychology ; Humans ; Hydrolases ; Indicators and Reagents ; Kinetics ; Protein Kinase Inhibitors ; Protein-Tyrosine Kinases - antagonists & inhibitors ; Src protein ; Structure-Activity Relationship ; Substrate Specificity ; Thiazoles - chemical synthesis ; Thiazoles - pharmacology ; v-Abl protein</subject><ispartof>The Journal of biological chemistry, 1990-12, Vol.265 (36), p.22255-22261</ispartof><rights>1990 © 1990 ASBMB. 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Biochemical and biological activity of a novel class of tyrosine protein kinase inhibitors</title><title>The Journal of biological chemistry</title><addtitle>J Biol Chem</addtitle><description>Various derivatives of thiazolidine-diones have been identified as tyrosine protein kinase inhibitors. The epidermal growth factor (EGF) receptor kinase and c-src kinase were inhibited in vitro with IC50 values in the range of 1-7 microM. The v-abl tyrosine protein kinase was not inhibited by thiazolidine-diones. Inhibition was found to be specific for tyrosine protein kinases. Inhibition of serine/threonine protein kinases was not observed. The active derivatives were shown to inhibit EGF-induced receptor autophosphorylation, either in vitro or in intact cells, and were also found to inhibit growth of the EGF-dependent BALB/MK and A431 cell lines (IC50 1-3 microM). Growth of the interleukin-3-dependent myeloid cell line FDC-P1 was inhibited with equal efficiency. Thus, in these cell lines, members of the c-src kinase family are also potential targets for inhibition by the compounds.</description><subject>Analytical, structural and metabolic biochemistry</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cell Division - drug effects</subject><subject>Cell Line</subject><subject>Enzymes and enzyme inhibitors</subject><subject>epidermal growth factor</subject><subject>ErbB Receptors - drug effects</subject><subject>ErbB Receptors - metabolism</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Humans</subject><subject>Hydrolases</subject><subject>Indicators and Reagents</subject><subject>Kinetics</subject><subject>Protein Kinase Inhibitors</subject><subject>Protein-Tyrosine Kinases - antagonists & inhibitors</subject><subject>Src protein</subject><subject>Structure-Activity Relationship</subject><subject>Substrate Specificity</subject><subject>Thiazoles - chemical synthesis</subject><subject>Thiazoles - pharmacology</subject><subject>v-Abl protein</subject><issn>0021-9258</issn><issn>1083-351X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1990</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1v1DAQQC0EKkvhJ1TyARAcUjJ2HMcnBBVfUiUOFImb5Tjj7kDWbuPsouXX421W5chcrPG8GY8fY2dQn0MN7ZtvdS2gMkJ1r6B73ajW6Mo8YCuoO1lJBT8estU98pg9yflnXaIxcMJOBOhWQL1i6WpN7k8aaaCI1UApYj7n7yn5NW7Iu5G7OPCe0piul9TPtKN5z1Pgjse0w5H70eV8uJj3U8plEL-Z0owU-S-KLiOnuKae5jTlp-xRcGPGZ8fzlH3_-OHq4nN1-fXTl4t3l5VvjJ6rRgTpRWiUroNsvVGixz6gUR2UPJgW2kZLLZ2WAbxTJXSAbjDahybIRp6yl8vcssntFvNsN5Q9jqOLmLbZgjKqAegKqBbQl9XzhMHeTLRx095CbQ-i7Z1oe7BoobN3oq0pfWfHB7b9Bof7rqPZUn9xrLtcvIXJRU_533DTgS7fKtzzhVvT9fo3TWj7Rb4VrbKytUIIpQr2dsGwSNsRTjZ7wuhxKC1-tkOi_yz8F8FkpzI</recordid><startdate>19901225</startdate><enddate>19901225</enddate><creator>Geissler, J F</creator><creator>Traxler, P</creator><creator>Regenass, U</creator><creator>Murray, B J</creator><creator>Roesel, J L</creator><creator>Meyer, T</creator><creator>McGlynn, E</creator><creator>Storni, A</creator><creator>Lydon, N B</creator><general>Elsevier Inc</general><general>American Society for Biochemistry and Molecular Biology</general><scope>6I.</scope><scope>AAFTH</scope><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QL</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>M81</scope><scope>P64</scope></search><sort><creationdate>19901225</creationdate><title>Thiazolidine-diones. Biochemical and biological activity of a novel class of tyrosine protein kinase inhibitors</title><author>Geissler, J F ; Traxler, P ; Regenass, U ; Murray, B J ; Roesel, J L ; Meyer, T ; McGlynn, E ; Storni, A ; Lydon, N B</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c497t-42f3c2f4570f36c952bebfe9581f36f961647373a73f1ca55557f18d97cf4f343</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1990</creationdate><topic>Analytical, structural and metabolic biochemistry</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cell Division - drug effects</topic><topic>Cell Line</topic><topic>Enzymes and enzyme inhibitors</topic><topic>epidermal growth factor</topic><topic>ErbB Receptors - drug effects</topic><topic>ErbB Receptors - metabolism</topic><topic>Fundamental and applied biological sciences. 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Biochemical and biological activity of a novel class of tyrosine protein kinase inhibitors</atitle><jtitle>The Journal of biological chemistry</jtitle><addtitle>J Biol Chem</addtitle><date>1990-12-25</date><risdate>1990</risdate><volume>265</volume><issue>36</issue><spage>22255</spage><epage>22261</epage><pages>22255-22261</pages><issn>0021-9258</issn><eissn>1083-351X</eissn><coden>JBCHA3</coden><abstract>Various derivatives of thiazolidine-diones have been identified as tyrosine protein kinase inhibitors. The epidermal growth factor (EGF) receptor kinase and c-src kinase were inhibited in vitro with IC50 values in the range of 1-7 microM. The v-abl tyrosine protein kinase was not inhibited by thiazolidine-diones. Inhibition was found to be specific for tyrosine protein kinases. Inhibition of serine/threonine protein kinases was not observed. 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| source | MEDLINE; EZB-FREE-00999 freely available EZB journals; Alma/SFX Local Collection |
| subjects | Analytical, structural and metabolic biochemistry Animals Biological and medical sciences Cell Division - drug effects Cell Line Enzymes and enzyme inhibitors epidermal growth factor ErbB Receptors - drug effects ErbB Receptors - metabolism Fundamental and applied biological sciences. Psychology Humans Hydrolases Indicators and Reagents Kinetics Protein Kinase Inhibitors Protein-Tyrosine Kinases - antagonists & inhibitors Src protein Structure-Activity Relationship Substrate Specificity Thiazoles - chemical synthesis Thiazoles - pharmacology v-Abl protein |
| title | Thiazolidine-diones. Biochemical and biological activity of a novel class of tyrosine protein kinase inhibitors |
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