Cryptophycin 中文
WebJun 17, 2024 · Methods: A peptide-drug conjugate (ER-472) composed of Cltx linked to cryptophycin as warhead was developed as a tool to probe the molecular target and mechanism of action of Cltx, using multiple xenograft models. Results: Neuropilin-1 (NRP1), an endocytic receptor on tumor and endothelial cells, was identified as a novel Cltx target, … Web中文名称 念珠藻素 英文名称 cryptophycin 定 义 从念珠藻(Nostoc)分离的一种多肽，有抗肿瘤作用。 应用学科 海洋科技（一级学科），海洋技术（二级学科），海洋生物技术（三 …
Cryptophycin 中文
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WebThe specific aims of the proposed research are: 1) To select mutant strains for enhanced cryptophycin production; 2) To improve the process for cryptophycin production; and 3) … WebAug 4, 1998 · Cryptophycin-52 (LY355703) (Fig. 1) is a new synthetic member of the cryptophycin family that is currently undergoing clinical evaluation (D.W., M. M. Wagner, D. C. Paul, M.A.J., L.W., and C. Shih, unpublished work).It was selected as a clinical candidate from an extensive series of cryptophycin analogs based on its potency, breadth of activity …
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 … WebJun 29, 2024 · Cryptophycin-52 analogs with more than one fluorine substituent have recently been published (Figure 15) 113. The CF 3-functionalized compound is about fivefold less active against the tumor cell line KB-3-1 in comparison with cryptophycin-52, while the pentafluorophenylalanine analog shows a significant loss of cytotoxicity, most likely …
WebNov 1, 2006 · The unit A trifluoromethyl-modified cryptophycin proved to be highly active against KB-3-1 cells and exhibited an IC50 value in the low picomolar range, but the replacement of the 3-chloro-4-methoxyphenyl-substituent in unit B by a pentafluorophenyl moiety resulted in a significant loss of activity. Expand WebTwo efficient protocols for the synthesis of tert-butyl (5S,6R,2E,7E)-5-[(tert-butyldimethylsilyl)oxy]-6-methyl-8-phenyl-2,7-octadienoate, a major component of the cryptophycins, are reported. The first utilized the Noyori reduction and Frater alkylation of methyl 5-benzyloxy-3-oxopentanoate to set two stereogenic centers, which became the …
WebEmbodiments of the disclosure include methods and compositions related to targeting of CD70-expressing cells with NK cells specifically engineered to bind the CD70 antigen. In par
WebAug 1, 2002 · Abstract. The cryptophycin analogue LY355703 is a potent inhibitor of microtubule polymerization that displays in vitro and in vivo activity in cell lines and tumor xenografts displaying the multidrug-resistant phenotype. In a Phase I trial, 25 patients received LY355703 as a 2-h i.v. infusion on day 1 and day 8 repeated every 3 weeks. … billy jean cup 2022 tvWebsynthesis翻译：化学生产, 合成, 混合, 综合，融合。了解更多。 cymbal\u0027s isCryptophycins are potent microtubule inhibitors, with a mechanism of action similar to that of vinca alkaloids. Treatment of cells with cryptophycins depletes microtubules through interaction with tubulin, thereby preventing cell division. Cryptophycins are capable of inducing apoptosis, possibly … See more Cryptophycins are a family of macrolide molecules that are potent cytotoxins and have been studied for potential antiproliferative properties useful in developing chemotherapy. They are members of the See more Cryptophycins were originally discovered in 1990 in cyanobacteria of the genus Nostoc. Cryptophycins were patented as antifungal agents with an unknown mechanism of action and … See more Cryptophycins were first isolated from cyanobacteria but have subsequently been produced by chemical synthesis. Chemoenzymatic … See more Members of the cryptophycin family have been studied as anti-tumor agents. Cryptophycin-52, a synthetic analog of natural product cryptophycins also known as LY355703, reached phase II clinical trials but was withdrawn due to side effects. See more cymbal\u0027s hfWebCryptophycin-52 (Cp-52) is potentially the most potent anticancer drug known, with IC50 values in the low picomolar range, but its binding site on tubulin and mechanism of action are unknown. Here, we have determined the binding site of Cp-52, and its parent compound, cryptophycin-1, on HeLa tubulin, to a resolution of 3.3 Å and 3.4 Å, respectively, by cryo … billy jean king net worth 2022WebCryptophycin 52 has demonstrated a broad range of antitumor activity against both murine and human tumors. In the human MX-1 breast carcinoma xenograft cryptophycin 55 produced greater-than- additive tumor response in combination with 5-fluorouracil. In human non-small cell lung carcinoma and human small cell carcinoma xenografts ... billy jean king age todayWebAug 1, 2024 · Cryptophycin-52 (CR52), a tubulin inhibitor, exhibits promising antitumor activity in vitro (picomolar level) and in mouse xenograft models. However, the narrow … billy jean king cup 2022 resultsWebMay 10, 2024 · The synthesis of an aza-cryptophycin analogue is described, featuring a highly trans-selective ring-closing metathesis reaction and an asymmetric Corey–Chaykovsky-type reaction to install the epoxide function. This latter reaction is an answer to the long-standing synthetic challenged posed by the efficient formation of the … cymbal\u0027s kin crossword clue