Interaction of Epothilone Analogs with the Paclitaxel Binding Site
نویسندگان
چکیده
منابع مشابه
Interaction of epothilone analogs with the paclitaxel binding site: relationship between binding affinity, microtubule stabilization, and cytotoxicity.
The interactions of epothilone analogs with the paclitaxel binding site of microtubules were studied. The influence of chemical modifications in the C15 side chain and in C12 on binding affinity and microtubule elongation was characterized. Modifications favorable for binding affinity are (1). a thiomethyl group at C21 of the thiazole side chain, (2). a methyl group at C12 in S configuration, (...
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The epothilones represent a new class of bacterial natural products with broad spectrum of antiproliferative activity against various types of human tumors and tumor cell lines. The attractive preclinical profile of epothilones has made them promising lead compounds for novel anticancer agents and has spurred a strong interest in obtaining different derivatives to fully evaluate their therapeut...
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Department of Immunology, Beckman Research Institute of the City of Hope, CA 91010, USA Division of Applied Life Science (BK21 Program), Systems and Synthetic Agrobiotech Center (SSAC), Plant Molecular Biology and Biotechnology Research Center (PMBBRC), Research Institute of Natural Science (RINS), Gyeongsang National University (GNU), Jinju 660-701, Korea. E-mail: [email protected] Department of...
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برهمکنش dnaتیموس گاوی طبیعی (ct-dna) با اتیلن دی آمین تترااستات (edta)در بافرtris-hcl با 8/7 ph ( دراین ph،edta به نمک دی سدیم تبدیل می شود) وسسامول در بافر tris-hcl با4/7 ph مورد بررسی قرار گرفته است. edta و سسامول استفاده فراوانی در تکنولوژی غذایی و صنعت شیمیایی دارند. مدل اتصال dna مربوط بهedta بوسیله اسپکتروفتومتری جذب، دورنگ نمایی حلقوی(cd)، ویسکومتری وژل الکتروفورز بررسی شده است. طیفuv ...
15 صفحه اولBinding of fluorescent analogs of GTP to the exchangeable nucleotide binding site of tubulin.
6 S tubulin from which the exchangeably bound guanine nucleotide had been removed was examined for its ability to bind two fluorescent analogs of GTP. One analog, (y-AmNS)GTP, contains the fluorophore l-aminonaphthalene 5-sulfonate attached to the y phosphate of GTP via a phosphoamidate bond. The second analog contains the same fluorophore attached to the sulfur atom of GTP-y-S via a 5-atom lin...
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ژورنال
عنوان ژورنال: Chemistry & Biology
سال: 2004
ISSN: 1074-5521
DOI: 10.1016/j.chembiol.2004.01.014