Masuda, Yuichi published the artcileSystematic Analysis of the Relationship among 3D Structure, Bioactivity, and Membrane Permeability of PF1171F, a Cyclic Hexapeptide with Paralyzing Effects on Silkworms, SDS of cas: 77128-73-5, the publication is Journal of Organic Chemistry (2017), 82(21), 11447-11463, database is CAplus and MEDLINE.
PF1171 hexapeptides, a family of cyclic hexapeptides produced by fungi, exhibit paralyzing effects on the larvae of silkworms via oral administration. To elucidate the structural features of PF1171 hexapeptides that are crucial for bioactivity, the relationship among 3D structure, bioactivity, and membrane permeability of PF1171F (the peptide with the highest bioavailability) was systematically analyzed through the synthesis of 22 analogs. The PF1171F analogs were prepared by the solid-phase synthesis of a linear precursor and subsequent solution-phase macrolactamization. Anal. by NMR spectroscopy and mol. modeling indicated that the major 3D conformations of PF1171F in various solvents resemble its x-ray crystal structure. The analogs with this conformation tend to exhibit potent paralysis against silkworms, indicating the significance of the conformation in the paralysis. The biol. activity was dependent on the mode of administration, varying between hemolymph injection and oral administration. Parallel artificial membrane permeability assay (PAMPA) of the analogs revealed a correlation between membrane permeabilities and paralytic activity by hemolymph injection, indicating that the target mol. of PF1171F is present inside the cell membrane.
Journal of Organic Chemistry published new progress about 77128-73-5. 77128-73-5 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, and the molecular formula is C25H23NO4, SDS of cas: 77128-73-5.
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https://en.wikipedia.org/wiki/Ether,
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