Andrew D. Howard - Park Ridge NJ Margaret A. Cascieri - East Windsor NJ Roy G. Smith - Houston TX Kathleen A. Sullivan - Springfield NJ Carina Tan - Metuchen NJ Leonardus H. T. Van Der Ploeg - Scotch Plains NJ Kevin R. Lynch - Charlottesville VA
Assignee:
Merck Co., Inc. - Rahway NJ
International Classification:
C12N 1512
US Classification:
435 691, 4353201, 435325, 536 235
Abstract:
A new galanin receptor, GALR3, is described. Also provided are nucleic acids encoding same and various assays to identify ligands particular to said receptor. Ligands so identified are useful for the treatment of obesity, treatment of pain, and treatment of cognitive disorders.
Cell Fusion Assays Using Fluorescence Resonance Energy Transfer
Kathleen A. Sullivan - Springfield NJ, US Diana Benincasa - Elizabeth NJ, US Margaret A. Cascieri - East Windsor NJ, US Lyndon J. Mitnaul - Piscataway NJ, US Lin-Lin Shiao - Westfield NJ, US Michael R. Tota - Middletown NJ, US
Methods of identifying inhibitors of the fusion of two types of cells, particularly when fusion is mediated by the interaction of a viral protein and such cellular proteins as CD4 and chemokine receptors, are disclosed. The methods are suitable for identifying substances that are useful for the treatment and prevention of viral diseases. Particularly preferred methods are useful for the identification of inhibitors of HIV-1 infection.
Galanin Receptor Galr3 And Nucleotides Encoding Same
Andrew Howard - Park Ridge NJ, US Margaret Cascieri - East Windsor NJ, US Roy Smith - Houston TX, US Kathleen Sullivan - Springfield NJ, US Carina Tan - Metuchen NJ, US Leonardus Van Der Ploeg - Scotch Plains NJ, US Kevin Lynch - Charlottesville VA, US
A new galanin receptor, GALR3, is described. Also provided are nucleic acids encoding same and various assays to identify ligands particular to said receptor. Ligands so identified are useful for the treatment of obesity, treatment of pain, and treatment of cognitive disorders.
Human Insulin-Like Growth Factor Analoges With Reduced Binding To Serum Carrier Proteins And Their Production In Yeast
Joy D. Applebaum - North Brunswick NJ Marvin L. Bayne - Westfield NJ Margaret A. Cascieri - East Windsor NJ
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
A61K 3726 C07K 710 C07K 740
US Classification:
514 3
Abstract:
A synthetic gene encoding a 71-amino acid analog of human insulin-like grouwth factor (hIGF-I) has been constructed and expressed in the yeast, Saccharomyces cerevisiae. The protein analog, IGF132, contains the first 17 amino acids of the B chain of human insulin in place of the first 16 amino acids of hIGF-I. The purified hybrid protein has high affinity for the type I IGF recepto (12 nM) yet has drastically reduced affinity for human serum carrier proteins (>1000 nM). This analog is 5 to 10 times more active than normal hIGF-I in stimulating DNA synthesis in 3T3 cells and is a more active growth factor in vivo due to its reduced affinity for serum carrier proteins. Other proteins with similar properties have also been constructed. The protein analogs thus have a variety of utilities such as in promoting lactation in animals; promoting growth and feed efficiency in animals; improving carcass quality by increasing lean and decreasing fat; promoting wound healing in animals, including humans; promoting glucose utilization in skeletal muscle, and stimulating erythropoiesis, the production of red blood cells.
Margaret A. Cascieri - East Windsor NJ Douglas John MacNeil - Westfield NJ Catherine D. Strader - Verona NJ
Assignee:
Merck & Co., Inc - Rayway NJ
International Classification:
C07K 14705 C07H 2104 C12P 1511
US Classification:
530350
Abstract:
Modified neuropeptide Y receptors having deletions, replacements or additions in the third intracellular domain are identified and methods of making the modified receptors are provided. The invention includes the modified receptors, assays employing the modified receptors, cells expressing the modified receptors, compounds identified through the use of the modified receptors, including modulators of the receptors, and the use of the compounds to treat 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.
Margaret A. Cascieri - East Windsor NJ Douglas J. MacNeil - Westfield NJ Lin-Lin Shiao - Avenel NJ David H. Weinberg - Westfield NJ Carina P. Tan - Metuchen NJ David L. Linemeyer - Westfield NJ Catherine D. Strader - Verona NJ
Assignee:
Merck & Co., Ltd. - Rahway NJ
International Classification:
C12Q 168 C12Q 102 C12N 1585 C12N 510
US Classification:
435 6
Abstract:
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.
Combination Therapy For The Treatment Of Diabetes And Obesity
Roy G. Smith - Westfield NJ Margaret A. Cascieri - East Windsor NJ Euan MacIntyre - Scotch Plains NJ Douglas J. MacNeil - Westfield NJ John G. Menke - Morganville NJ
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
A61K 3800 A61K 3124 C07K 500 C07K 1600
US Classification:
514 12
Abstract:
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.
Margaret A. Cascieri - East Windsor NJ Gary A. Chicchi - East Brunswick NJ Michael P. Graziano - Scotch Plains NJ Patricia J. Hey - Fanwood NJ
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
C12N 1510 C12N 510 C07K 14705
US Classification:
536 231
Abstract:
A synthetic human glucagon (hGlu) binding protein designated hGlu. DELTA. 252-259 binding protein is cloned, expressed and used in an in vitro assay to screen for compounds that bind to the synthetic binding protein, including compounds that specifically stimulate or inhibit the binding of glucagon to the synthetic receptor. The invention includes the assay, the synthetic binding protein used in the assay, DNA encoding the synthetic binding protein, cells expressing the synthetic binding protein, and compounds identified through the use of the synthetic binding protein.
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