Section 12
Chapter 11,934

Design and synthesis of photoaffinity-labeling ligands of the L-prolyl-L-leucylglycinamide binding site involved in the allosteric modulation of the dopamine receptor

Fisher, A.; Mann, A.; Verma, V.; Thomas, N.; Mishra, R.K.; Johnson, R.L.

Journal of Medicinal Chemistry 49(1): 307-317


ISSN/ISBN: 0022-2623
PMID: 16392815
DOI: 10.1021/jm050644n
Accession: 011933487

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Pro-Leu-Gly-NH2 (PLG), in addition to its endocrine effects, possesses the ability to modulate dopamine D-2 receptors within the central nervous system. However, the precise binding site of PLG is unknown. Potential photoaffinity-labeling ligands of the PLG binding site were designed as tools to be used in the identification of the macromolecule that possesses this binding site. Six different photoaffinity-labeling ligands were designed and synthesized on the basis of the gamma-lactam PLG peptidomimetic 1. The 4-azidobenzoyl and 4-azido-2-hydroxybenzoyl photoaffinity-labeling moieties were placed at opposite ends of PLG peptidomimetic I to generate a series of ligands that potentially could be used to map the PLG binding site.

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