Merck + Co., Inc.

Other

Douglas J MacNeil

Lihu Yang

Akio Kanatani

Takehiro Fukami

Ying-Duo Gao

Masaki Ihara

Yasuyuki Ishii

Takahiro Fukuroda

Margaret A Cascieri

David H Weinberg

Nancy R Morin

Leonardus H T Van Der Ploeg

Catherine D Strader

Carina P Tan

Andrew D Howard

Roy G Smith

David L Linemeyer

Tanya MacNeil

Lin-Lin Shiao

Arthur A Patchett

Scott D Feighner

John G Menke

Stanley L Streicher

Philip S Paress

Karen Kulju McKee

Sheng-Shung Pong

Carolyn L Ruby

Euan MacIntyre

Keith M Gewain

The motilin receptor has been isolated and cloned, and nucleic acid sequences are given. Two spice variants have been identified. Also, assays for motilin receptor ligands are given. The identification of the cloned motilin receptor may be used to screen and identify compounds which bind to the receptor for use in a variety of gastric conditions, including gastric motility disorders.

Cloning and identification of the motilin receptor

The present invention relates to rhesus monkey DNA molecules encoding the melanocortin-4 receptor protein, recombinant vectors comprising DNA molecules encoding rhesus MC-4R, recombinant host cells which contain a recombinant vectors encoding rhesus MC-4R, the rhesus MC-4R protein encoded by the DNA molecule, and methods of identifying selective agonists and antagonists of rhesus MC-4R.

DNA molecules encoding the melanocortin 4 receptor protein from rhesus monkey

The present invention relates to DNA molecules encoding splice variants of the melanocortin-1 receptor (MC-R1) protein belonging to the rhodopsin sub-family of G-protein coupled receptors, recombinant vectors comprising DNA molecules encoding MC-R1B protein, recombinant host cells which contain a recombinant vector encoding MC-R1B, the human MC-R1B protein encoded by the DNA molecule, and methods of identifying selective agonists and antagonists of MC-R1B proteins disclosed throughout this specification.

DNA molecules encoding splice variants of the human melanocortin 1 receptor protein

Spiro-indolines as Y5 receptor antagonists

NPY Y5 receptor antagonists

Compounds of general structural formula I such as that shown in structural formula II

Compounds of the general structural formula I

Modified human neuropeptide Y1 Receptors

Neuropeptide Y receptor

The combination of a metabolic rate modifying agent (e.g., a .beta..sub.3 adrenergic receptor agonist) and a feeding behavior modifying agent (e.g., a NPY5 antagonist) is useful in the treatment of obesity and diabetes, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients. Methods of treating obesity and diabetes are also described.

Combination therapy for the treatment of diabetes and obesity

A novel mammalian neuropeptide Y receptor and method of making the receptor are provided. The invention includes DNA encoding the receptor, the receptor, assays employing the receptor, cells expressing the receptor, antibodies which bind specifically to the receptor, RNA encoded by the DNA sequence or its complementary sequence, and single-stranded DNA with a sequence complementary to the RNA which encodes the receptor. The receptor and assays employing the receptor are useful for identifying compounds which bind to the receptor, including specific modulators of the receptor. Such compounds are useful for treating a variety of disease conditions, including obesity, diabetes, anxiety, hypertension, cocaine withdrawal, congestive heart failure, memory enhancement, cardiac and cerebral vasospasm, pheochromocytoma and ganglioneuroblastoma, and Huntington's, Alzheimer's and Parkinson's diseases.

Avermectin compounds are glycosylated at the 4',13- Or 14a-positions by adding the avermectin compounds to the fermentation medium of a novel strain of Streptomyces avermitilis. The 13-hydroxy and 14a-hydroxy methyl groups of the avermectin compound are glycosylated with a glycosyl moiety, specifically an oleandrose group. The new strain offers the added advantage of not producing any C5-O-methylation products. The compounds are potent anthelmintic and antiparasite agents, and compositions for such uses are also disclosed.

Strain of streptomyces avermitilis capable of glycosylating avermectin

There are disclosed plasmids containing DNA isolated from Streptomyces avermitilis, the microorganism which is used to prepare avermectin compounds, identified as pAT1, pVE650 pVE855, pVE859, pVE1446, pVE923, and pVE924 which contain the genetic information for the biosynthesis of the avermectins. Methods for the isolation of such plasmid and for the manipulation of the plasmids to alter the formation of the avermectin compound are also disclosed.

Cloning genes from Streptomyces avermitilis for avermectin biosynthesis

There is disclosed a process for the incorporation of DNA into a microorganism that, because of natural restrictions in the organism, normally would prevent or limit the incorporation of the DNA. The process involves the selection of an intermediate host organism that has no restrictions to the incorporation of DNA. The DNA is then transferred into the intermediate host which is readily accomplished because there are no restrictions. The DNA is then isolated from the intermediate host and transferred into the target organism. Using this process the natural restrictions of the host organism are circumvented and DNA is transferred from a source organism to a target organism that normally would not be possible. In this manner desirable characteristics from the source organism can be imparted into the target organism.

Process for the incorporation of DNA molecules into microorganisms with

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Westfield, NJ, United States of America

Douglas J MacNeil