title: Affinity probes for the avermectin binding proteins.
abstract: The design and synthesis of a series of avermectin affinity probes used in the identification and purification of the avermectin binding proteins is described. These modified avermectins fall into two design classes: ligands to covalently modify specific avermectin binding proteins [an 125I-labeled aryl azide photoprobe (15) and a tritiated aziridine analog (6)] and ligands for affinity chromatography applications [three biotinylated compounds (10, 12, and 13) and one resin-bound derivative (9)]. The binding affinities of these compounds for the Caenorhabditis elegans avermectin binding protein is presented as well as their biological activities against C. elegans and Artemia salina.
authors.affiliation: Department of Basic Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065-0900.
authors.forename: P T
authors.initials: PT
authors.lastname: Meinke
authors.forename: S P
authors.initials: SP
authors.lastname: Rohrer
authors.forename: E C
authors.initials: EC
authors.lastname: Hayes
authors.forename: J M
authors.initials: JM
authors.lastname: Schaeffer
authors.forename: M H
authors.initials: MH
authors.lastname: Fisher
authors.forename: H
authors.initials: H
authors.lastname: Mrozik
mesh_terms: D000345:Affinity Labels / Q000138:chemical synthesis* / Q000378:metabolism; D000818:Animals; D000871:Anthelmintics / Q000378:metabolism*; D001156:Artemia; D017173:Caenorhabditis elegans / Q000378:metabolism; D007559:Ivermectin / Q000031:analogs & derivatives* / Q000378:metabolism; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D011955:Receptors, Drug / Q000378:metabolism*
chemical_list: D000345:Affinity Labels; D000871:Anthelmintics; D008024:Ligands; D011955:Receptors, Drug; D007559:Ivermectin; C019264:avermectin