Auristatin F
Aug 27, 2019 ·
1m 10s
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Description
Auristatins are a family of complex analogues to the native antineoplastic product dolastatin 10, for instance, Auristatin F. They are 100 to 1000 times more toxic than Doxorubicin, a conventional...
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Auristatins are a family of complex analogues to the native antineoplastic product dolastatin 10, for instance, Auristatin F. They are 100 to 1000 times more toxic than Doxorubicin, a conventional cancer chemotherapy medication. The potent agent, dolastatin 10 is a five-subunit penta-peptide discroverde by Pettit et al. from the sea hare Dolabella auricularia in 1987 and chemical modification to dolastatin 10 were applied to generate auristatins. It was later realized that the remarkable cytotoxicity of auristatins owes to their powerful capability to inhibit microtubule formation through the interaction with tubulin at the "peptide sub-site" of tubulin's "Vinca domain" and disrupt tubulin-dependent GTP hydrolysis. Auristatins lead to the arrest of cancer cells in the mitosis stage and eventually, apoptosis. Unfortunately, due to their high cytotoxicity, harmful side-effects and a narrow therapeutic window were reported in clinical trials of auristatins, rendering them unsuitable as anticancer medications. https://www.creative-biolabs.com/adc/auristatin-f-708.htm
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Information
Author | Bella Smith |
Organization | Bella Smith |
Website | - |
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