TY  - JOUR
AB  - Cryptophycins are a class of 16-membered highly cytotoxic macrocyclic depsipeptides isolated from cyanobacteria. The biological activity is based on their ability to interact with tubulin. They interfere with microtubule dynamics and prevent microtubules from forming correct mitotic spindles, which causes cell-cycle arrest and apoptosis. Their strong antiproliferative activities with 100-fold to 1000-fold potency compared with those of paclitaxel and vinblastine have been observed. Cryptophycins are highly promising drug candidates, as their biological activity is not negatively affected by P-glycoprotein, a drug efflux system commonly found in multidrug-resistant cancer cell lines and solid tumors. Cryptophycin-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 © 2017 European Peptide Society and John Wiley & Sons, Ltd.
DA  - 2017
DO  - 10.1002/psc.3015
KW  - natural product
KW  - depsipeptide
KW  - total synthesis
KW  - biological activity
KW  - SAR
KW  - antimitotic agent
KW  - drug conjugate
KW  - bioconjugation
KW  - warhead
LA  - eng
IS  - 7-8
M2  - 514
PY  - 2017
SN  - 1075-2617
SP  - 514-531
T2  - Journal of Peptide Science
TI  - Cryptophycins: cytotoxic cyclodepsipeptides with potential for tumor targeting
UR  - https://nbn-resolving.org/urn:nbn:de:0070-pub-29169811
Y2  - 2024-11-22T07:06:06
ER  -