Global ETD Search
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Showing 1 to 3 of 3 for “"Aplyronines"”.
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Studies Towards a Second-Generation Synthesis of the Aplyronines
The aplyronines are a family of 24-membered macrolides of polyketide origin, isolated from the Japanese sea hare Aplysia kurodai. They exhibit an exceptional biological activity profile, acting through an actin and tubulin dual-targeting mechanism, with subnanomolar growth inhibitory potency …
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Designed analogues of the aplyronines for use in antibody-drug conjugates
The aplyronines are a family of structurally complex marine macrolides, isolated from the sea hare Aplysia kurodai, that exhibit picomolar growth inhibitory activity in the NCI 60 cell line panel. An unprecedented heterotrimeric complex has been observed to form between aplyronine A and actin and …
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Rationally designed aplyronine analogues for use in antibody-drug conjugates
The aplyronines are a family of antimitotic marine macrolides which show highly potent antiproliferative effects at picomolar concentrations in human cancer cell lines. Through a novel dual protein-targeting mechanism of action, their exquisite potency renders the aplyronines promising drug …