Pharmacia & Upjohn Company

The Upjohn Co.

Timothy G Geary

David E Lowery

Teresa M Kubiak

Martha J Larsen

Jerry W Bowman

Ronald D Klein

Alan R Friedman

The invention provides neuropeptide ligands, G protein-coupled receptors and methods of screening for modulators of receptor activity. Identified modulators, including neuropeptide ligand mimetics, are useful as biostatic and biocidal agents of varying scope, ranging from lethal activity restricted to particular invertebrate parasites to broad spectrum invertebrate parasiticides active on a wide range of invertebrates, including helminths and insects.

G protein-coupled receptor-like receptors and modulators thereof

The present invention provides a novel radioactive neuropeptide represented by the formula Lys-His-Glu-Tyr.sup.--I -Leu-Arg-Phe-amide. The invention also provides a method for detecting anthelmintic activity of a compound using the novel neuropeptide of the present invention in a receptor binding assay. The novel radioactive neuropeptide has potent bioactivity in Ascaris suum neuromuscular strips, and therefore is particularly useful for high volume screening for potential anthelmintic compounds.

Method for discovering novel anthelmintic compounds

A method for identifying compounds useful as antiparasitic drugs is disclosed. Deficient microorganisms are complemented with homologous metabolic enzyme genes. The metabolic enzyme is the drug target. In addition, recombinant DNA molecules comprising helminthic PFK and PEPCK genes are disclosed.

Method of indentifying compounds useful as antiparasitic drugs

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Kalamazoo, MI, United States of America

Timothy G Geary