AI Article Synopsis
- A neutral-loss scanning mass method helped identify new kynurenine-containing cycloheptapeptides, named phakefustatins A-C, from a marine sponge.
- Their structures were determined using spectroscopic analysis and advanced techniques like Marfey's method.
- Phakefustatin A was found to act as an RXRα modulator, potentially inhibiting cancer cell growth, with key pharmacophore groups being kynurenine and guanidine.
Article Abstract
A neutral-loss scanning mass method was used to explore new kynurenine-containing cycloheptapeptides, phakefustatins A-C (-), from the marine sponge . Their structures were elucidated by spectroscopic analysis and the advanced Marfey's method. was total synthesized via a final-stage ozonolysis strategy by the combination of solid/solution-phase synthesis. Phakefustatin A () was identified as a RXRα modulator to inhibit cancer cell growth, and its pharmacophores could be Kyn and guanidine groups.
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| http://dx.doi.org/10.1021/acs.orglett.0c01586 | DOI Listing |
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Phakefustatins A-C: Kynurenine-Bearing Cycloheptapeptides as RXRα Modulators from the Marine Sponge .
Org Lett
September 2020
Research Center for Marine Drugs, State Key Laboratory of Oncogene and Related Genes, Department of Pharmacy, Ren Ji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, China.
Article Synopsis
- A neutral-loss scanning mass method helped identify new kynurenine-containing cycloheptapeptides, named phakefustatins A-C, from a marine sponge.
- Their structures were determined using spectroscopic analysis and advanced techniques like Marfey's method.
- Phakefustatin A was found to act as an RXRα modulator, potentially inhibiting cancer cell growth, with key pharmacophore groups being kynurenine and guanidine.
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