Cryptophycin
WebCryptophycin 1 is a natural product that was initially isolated from blue-green algae which has shown potent broad spectrum antitumor activity in preclinical in vitro and in vivo models. The drug strongly binds to tubulin and disrupts microtubule assembly for more than 24 hours after its removal. WebCryptophycin is a potent antitumor agent that depletes microtubules in intact cells, including cells with the multidrug resistance phenotype. To determine the mechanism of action of …
Cryptophycin
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WebMay 11, 2000 · An efficient and highly stereoselective synthesis of cryptophycin B (2), a potent cytotoxic agent, is described. The ester-derived titanium-enolate-mediated syn-aldol reaction was employed to generate the stereocenters C(5) and C(6). The route is convergent and provides a convenient access to the synthesis of structural variants of cryptophycin B … WebCryptophycin 1 is one of the most potent tubulin-destabilizing agents ever discovered, resulting in cellular arrest at the G2/M phase via hyperphosphorylation of Bcl-2, thereby …
WebFeb 6, 2007 · The bioactivity of cryptophycins is based on their ability to interact with tubulin. They display considerable tumour-selective cytotoxicity both against multidrug-resistant tumour cell lines and... WebCryptophycin-309 (C-309) is a glycinate ester of the chlorohydrin Cryptophycin-296. The glycinate derivative provided both chemical stability and improved aqueous solubility. After the examination of 81 different Cryptophycin analogs in tumor bearing animals, C-309 has emerged as superior to all others. ...
WebJun 7, 2024 · The cryptophycin conjugates display high in vitro potency with IC 50 values between 22.3–287.5 n M, showing slightly reduced activity compared to cryptophycin-55 glycinate. Moreover, conjugates bearing cleavable linker ( 10, 11) are more cytotoxic than the corresponding uncleavable conjugates ( 13, 14 ). WebThe invention provides methods and compositions to detect expression of one or more biomarkers for identifying and treating patients having glioblastomas who are likely to be responsive to VEGF antagonist therapy. The invention also provides kits and articles of manufacture for use in the methods.
WebCryptophycin 1 is a natural product that was initially isolated from blue-green algae which has shown potent broad spectrum antitumor activity in preclinical in vitro and in vivo …
WebJun 29, 2024 · Hence, cryptophycin-52 is a very active antitumor agent with superior cytotoxicity compared with many of the conventional drugs used in oncology. Therefore, … scrap metal knoxvilleWebThe cryptophycins are a unique family of 16-membered macrolide antimitotic agents isolated from the cyanobacteria Nostoc sp. Their molecular target is tubulin protein … scrap metal lakewood coWebCryptophycin is a new anticancer drug discovered from micro-algae by researchers of the University of Hawaii and Wayne State University. Some of the cryptophycin analogs are … scrap metal knowsleyWebThe TE domain on the enzymatic assembly line converts the intermediate shown below to Cryptophycin 24. In 1-2 sentences, specify whether the TE domain catalyzes the hydrolysis or the cyclization (macrolactonization) to generate Cryptophycin 24 and explain one feature of the TE domain that will enable the desired reaction outcome. scrap metal lancashireWebKR102512597B1 KR1020247033500A KR20247033500A KR102512597B1 KR 102512597 B1 KR102512597 B1 KR 102512597B1 KR 1020247033500 A KR1020247033500 A KR 1020247033500A KR 20247033500 A KR20247033500 A KR 20247033500A KR 102512597 B1 KR102512597 B1 KR 102512597B1 Authority KR South Korea Prior art keywords cmet … scrap metal last day on earth survivalWebSep 21, 2024 · This cryptophycin derivative possesses distinct features, such as high in vitro potency, remarkable in vivo activity against MDR xenografts, 40 excellent stability in … scrap metal lake havasu city azWebDec 1, 2002 · A new addition to the family of microtubule targeting agents is cryptophycin 52 (LY355703), a macrocyclic depsipeptide ().It is a synthetic analogue of naturally occurring cryptophycins isolated from the blue-green algae species Nostoc .Cryptophycin 52 binds to the Vinca domain of microtubules, inhibits microtubule polymerization, and is the … scrap metal lawrence ks