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Furthermore, clinical studies aimed at raising HDL-C levels through niacin and CETP inhibitors have failed to reduce risk of cardiovascular events and have been stopped prematurely due to lack of efficacy or increased number of events

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The constrained conformation additionally positions the pharmacophore residues (His, D-Phe, Arg, Trp) in an optimal spatial arrangement for simultaneous contact with the MC receptor binding pocket, which is why cyclic melanocortin analogs consistently demonstrate 10-100 fold greater potency than their linear counterparts in cAMP accumulation assays

10.3171/2019.11.SPINE19586 J

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