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Medicinal chemistry small-molecule modulator

The discovery of the first nonpetide CCK antagonist, the natural product asperlicin, in 1985 (495) shifted the medicinal chemistry focus from peptides to small molecule antagonists (496,497).CCK-B receptors are the dominant isoform in the brain, and antagonists at this subtype are potential anxiolytics. Many CCK-B antagonists also modulate gastric acid secretion through peripheral CCK-B (gastrin) receptors. [Pg.573]

Taylor, C.M., Barda, Y., Kisseley O.G., and Marshall, G.R. (2008) Modulating G-protein coupled receptor/G-protein signal transduction by small molecules suggested by virtual screening. Journal of Medicinal Chemistry, 51 (17), 5297-5303. [Pg.405]

Thiele, S., Malmgaard-Clausen, M., Engel-Andreasen, J., Steen, A., Rummel, P. C., Nielsen, M. C., et al. (2012). Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors. Journal of Medicinal Chemistry, 55, 8164-8177. [Pg.186]


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Medicinal chemistry

Small molecule modulators

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