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
David E. Lowery - Portage MI, US Timothy G. Geary - Kalamazoo MI, US Teresa M. Kubiak - Richland MI, US Martha J. Larsen - Kalamazoo MI, US
Assignee:
Pharmacia & Upjohn Company - Kalamazoo MI
International Classification:
C12N 15/12
US Classification:
536 235, 435 721, 435 691, 4352523, 4353201
Abstract:
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.
An anthelmintic composition comprising: (a) one or more active ingredients which is a member from the family of macrocyclic lactones; and (b) one or more active ingredients which is a member from the family of spirodioxepinoindoles is provided. The composition is used to treat or prevent parasitic diseases.
Timothy Geary - Kalamazoo MI, US Margaret Favreau - Richland MI, US
Assignee:
Pharmacia and UpJohn Company
International Classification:
C12Q001/18
US Classification:
435/032000
Abstract:
This invention describes novel methods for the identification of compounds useful as inhibitors of enzymes. The methods involve obtaining a target gene-complemented microorganism which is dependent on the expression of the target gene for survival in test conditions. By measuring the viability of the complemented microorganism after exposure to a compound, compounds that inhibit growth in test conditions are identified. These compounds that inhibit growth are further tested in conditions where the expression of the target gene is not required for growth in order to identify compounds that specifically inhibit the target gene but do not effect the viability of the host.
Method For Discovering Novel Anthelmintic Compounds
Timothy G. Geary - Kalamazoo MI Jerry W. Bowman - Lawton MI Alan R. Friedman - Portage MI
Assignee:
Pharmacia & Upjohn Company - Kalamazoo MI
International Classification:
A61K 3808
US Classification:
530329
Abstract:
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 Of Indentifying Compounds Useful As Antiparasitic Drugs
Ronald D. Klein - Schoolcraft MI Timothy G. Geary - Kalamazoo MI
Assignee:
The Upjohn Company - Kalamazoo MI
International Classification:
C12Q 102 C12Q 168 C12N 120 C07H 1512
US Classification:
435 29
Abstract:
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.