Cryptophycin-52
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a synthetic analog of natural product cryptophycins also known as LY355703, reached phase II clinical trials but was withdrawn due to side effects. Web优先权声明. 本申请要求于2024年7月3日提交的美国临时申请62/693,768和2024年6月14日提交的美国临时申请62/861,825的权益，这些 ...
Cryptophycin-52
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WebFeb 3, 2024 · A synthetic analog, cryptophycin-52 (Figure 1) that contains a geminal dimethyl functionality in unit C entered clinical trials for both the treatment of platinum resistant ovarian cancer and non-small cell lung cancer. 10–12 Despite showing significant disease stabilization and an overall positive result, the trials were discontinued due to ... 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 …
WebAug 4, 1998 · Cryptophycin-52 (LY355703) is a new synthetic member of the cryptophycin family of antimitotic antitumor agents that is currently undergoing clinical evaluation. At …
WebNov 2, 2010 · Figure 1: The four building blocks (units) A–D of cryptophycin-1 (1) and cryptophycin-52 (2). Jump to Figure 1 The previously published synthetic route to unit B precursor 4 involves a three-step modification of D-tyrosine by chlorination, protecting group introduction and double methylation followed by a final saponification reaction to give ... WebDec 15, 2006 · Consequently, cryptophycin 52 (Figure 2, panel b), a synthetic analogue, was developed and reached phase 2 clinical trials (15-17). The synthetic analogue 52 was chosen because no large-scale biotechnological production method existed for …
WebApr 25, 2002 · A synthesis of cryptophycin 52 is reported using a Shi epoxidation strategy to install the epoxide moiety in a diastereoselective fashion. Several epoxidation results for …
WebFor instance, the synthetic analog cryptophycin 52 (1), which progressed to Phase II clinical trials for the treatment of patients with platinum-resistant ovarian cancer, is based on the cryptophycin 1 (2) which was isolated from terrestrial cyanobacteria [7,8]. … eagle family dental new orleans eastWebCryptophycin-52 (Cp-52), a biologically more stable analog of the parent compound cryptophycin-1 (Cp-1), has progressed to phase 2 clinical trials for use against both advanced non–small-cell lung cancer ( 6 ) and platinum-resistant ovarian cancer ( 7 csi of mdWebCryptophycin-52 had been investigated in phase II clinical trials but failed because of its high neurotoxicity. Recently, cryptophycin conjugates with peptides and antibodies have been developed for targeted delivery in tumor therapy. Copyright © 2024 European Peptide Society and John Wiley & Sons, Ltd. eagle family foods clevelandWebBackground: Cryptophycin 52 is a novel antitubulin drug with in vitro and in vivo activity in non-small cell lung cancer. Based upon promising Phase 1 data, a multicenter trial was performed to evaluate the drug in previously treated non-small cell lung cancer (NSCLC). csi of ladWebConformational changes in tubulin upon binding Cryptophycin-52 reveal its mechanism of action Conformational changes in tubulin upon binding Cryptophycin-52 reveal its mechanism of action J Biol Chem. 2024 Aug 27;101138. doi: 10.1016/j.jbc.2024.101138. Online ahead of print. Authors csi of montanaWebMar 15, 2024 · 7LXB, 7M18, 7M20. PubMed Abstract: Cryptophycin-52 (Cp-52) is potentially the most potent anticancer drug known, with IC 50 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 ... csi of omaha agent loginWebCryptophycin-52 (Cp-52), a biologically more stable analog of the parent compound cryptophycin-1 (Cp-1), has progressed to phase 2 clinical trials for use against both … csi of kentucky