Cryptophycin-52
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 … WebConformational 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
Cryptophycin-52
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WebMar 1, 2003 · 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... WebJul 3, 2003 · Cryptophycin 52 is a synthetic derivative of Cryptophycin 1, a potent antimicrotubule agent isolated from cyanobacteria. In an effort to increase the potency …
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 … WebGenerally, these compounds exhibit interesting biological properties, including antibacterial and antifungal activities or can be used in the synthesis of many bioactive compounds such as phosphapeptides (acting as enzyme inhibitors), oligonucleotides, cytotoxic agents (for example Cryptophycin 52) or 2,4,5-imidazolidinetriones (herbicides and ...
WebJul 1, 2000 · Cryptophycin 52 (0.3 mg/kg IV given on days 7, 9, and 11) is also efficacious in rats bearing the 13762 mammary carcinoma (104). Additive and supra-additive effects are noted in human tumor... WebJan 1, 2024 · Cryptophycin 1 and 52 is another such compound with a similar effect. Cryptophycins, also known for microtubule targeting, activates cysteine proteases CPP32, that is, caspase-3, YAMA, apopain (an ICE/CED-3-like a protease member of apoptosis effector family) and causes irregular mitotic spindles formation culminated in the …
WebAug 1, 2024 · Cryptophycin-52 (CR52), a tubulin inhibitor, exhibits promising antitumor activity in vitro (picomolar level) and in mouse xenograft models. However, the narrow therapeutic window in clinical trials limits its further development. Antibody-drug conjugate (ADC), formed by coupling cytotoxic compound (payload) to an antibody via a linker, can ...
WebMar 1, 2003 · 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 … losing stomach fat on treadmillWebSummary. Dr. Eren received her Ph.D. from Worcester Polytechnic Institute (WPI), where she studied metal transport mechanisms across membranes by P-type ATPases. Mutations in Cu-ATPases, a subfamily of ATPases, are associated with Menkes and Wilson’s diseases in humans. During her postdoctoral studies at the University of Massachusetts ... horlofabWebCryptophycin 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 … horloffer seeMembers 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. losing strength crosswordWebCryptophycin-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. losing stomach fat when skinny fatWebCryptophycin-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 … losing students private schools try to changeWebJul 1, 2000 · Cryptophycin 52 (0.3 mg/kg IV given on days 7, 9, and 11) is also efficacious in rats bearing the 13762 mammary carcinoma (104). Additive and supra-additive effects … horloffstimmen