Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.

PubWeight™: 0.88‹?›

🔗 View Article (PMC 27982)

Published in Proc Natl Acad Sci U S A on September 01, 1998

Authors

L Yang1, S C Berk, S P Rohrer, R T Mosley, L Guo, D J Underwood, B H Arison, E T Birzin, E C Hayes, S W Mitra, R M Parmar, K Cheng, T J Wu, B S Butler, F Foor, A Pasternak, Y Pan, M Silva, R M Freidinger, R G Smith, K Chapman, J M Schaeffer, A A Patchett

Author Affiliations

1: Department of Medicinal Chemistry, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USA.

Articles cited by this

Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol (1973) 47.81

Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. J Med Chem (1988) 3.04

Somatostatin. N Engl J Med (1983) 2.68

Somatostatin (second of two parts). N Engl J Med (1983) 2.35

The role of somatostatin and its analogs in the diagnosis and treatment of tumors. Endocr Rev (1991) 2.20

Essential role of growth hormone in ischemia-induced retinal neovascularization. Science (1997) 2.11

Cloning and functional characterization of a family of human and mouse somatostatin receptors expressed in brain, gastrointestinal tract, and kidney. Proc Natl Acad Sci U S A (1992) 2.07

N-terminally extended somatostatin: the primary structure of somatostatin-28. FEBS Lett (1980) 2.04

Molecular biology of somatostatin receptors. Endocr Rev (1995) 1.63

Isolation and structure of pro-somatostatin: a putative somatostatin precursor from pig hypothalamus. Proc Natl Acad Sci U S A (1980) 1.54

Cloning of a novel somatostatin receptor, SSTR3, coupled to adenylylcyclase. J Biol Chem (1992) 1.34

Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue. Proc Natl Acad Sci U S A (1995) 1.32

Molecular cloning and expression of a pituitary somatostatin receptor with preferential affinity for somatostatin-28. Mol Pharmacol (1992) 1.27

Somatostatin in the central nervous system: physiology and pathological modifications. Prog Neurobiol (1986) 1.24

Selective effects of somatostatin-14, -25 and -28 on in vitro insulin and glucagon secretion. Nature (1981) 1.23

All five cloned human somatostatin receptors (hSSTR1-5) are functionally coupled to adenylyl cyclase. Biochem Biophys Res Commun (1994) 1.22

The role of somatostatin in the regulation of anterior pituitary hormone secretion and the use of its analogs in the treatment of human pituitary tumors. Endocr Rev (1988) 1.21

Molecular cloning and functional expression of a brain-specific somatostatin receptor. Proc Natl Acad Sci U S A (1992) 1.19

Advances in the use of somatostatins in the management of endocrine tumors. Curr Opin Oncol (1996) 1.09

Molecular pharmacology of somatostatin receptor subtypes. J Endocrinol Invest (1997) 1.08

Somatostatin analogs for diagnosis and treatment of cancer. Pharmacol Ther (1993) 1.08

Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation. J Clin Invest (1997) 1.06

Flexibases: a way to enhance the use of molecular docking methods. J Comput Aided Mol Des (1994) 1.00

Characterization of cloned somatostatin receptors SSTR4 and SSTR5. Mol Pharmacol (1993) 0.97

Effects of somatostatin-14 and somatostatin-28 on bombesin-stimulated release of gastrin, insulin, and glucagon in the dog. Endocrinology (1981) 0.92

Physiological role of somatostatin in the digestive tract: gastric acid secretion, intestinal absorption, and motility. Scand J Gastroenterol Suppl (1986) 0.88

Specific inhibition of rat pancreatic insulin or glucagon release by receptor-selective somatostatin analogs. Biochem Biophys Res Commun (1994) 0.87

Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists. J Med Chem (1998) 0.85

Cell specific expression of the sst2A and sst5 somatostatin receptors in the rat anterior pituitary. Endocrinology (1998) 0.85

Immunohistochemical localization of somatostatin receptor SST2A in the rat pancreas. Endocrinology (1997) 0.85

Method for identifying ligands that bind to cloned G(s)- or G(i)-coupled receptors. Mol Cell Neurosci (1991) 0.84

Somatostatin receptors. Crit Rev Neurobiol (1992) 0.82

Cyclic hexapeptides related to somatostatin. Conformational analysis employing 1H-NMR and molecular dynamics. Int J Pept Protein Res (1990) 0.80

Structure and function of somatostatin receptors in growth hormone control. J Endocrinol (1997) 0.77

Three-dimensional quantitative structure-activity relationships of somatostatin analogues. 1. Comparative molecular field analysis of growth hormone release-inhibiting potencies. J Med Chem (1995) 0.77

The new pharmacology of somatostatin and its multiple receptors. J Pediatr Endocrinol (1994) 0.77

Articles by these authors

Defective LPS signaling in C3H/HeJ and C57BL/10ScCr mice: mutations in Tlr4 gene. Science (1998) 37.15

The role of attention in the treatment of attention-maintained self-injurious behavior: noncontingent reinforcement and differential reinforcement of other behavior. J Appl Behav Anal (1993) 9.17

A detailed model of reverse transcription and tests of crucial aspects. Cell (1979) 8.93

The functions of self-injurious behavior: an experimental-epidemiological analysis. J Appl Behav Anal (1994) 8.16

The human gene for vascular endothelial growth factor. Multiple protein forms are encoded through alternative exon splicing. J Biol Chem (1991) 7.22

Biochemical parameters of glutamine synthetase from Klebsiella aerogenes. J Bacteriol (1977) 6.99

Structure of a cloned circular Moloney murine leukemia virus DNA molecule containing an inverted segment: implications for retrovirus integration. Proc Natl Acad Sci U S A (1980) 6.73

A receptor in pituitary and hypothalamus that functions in growth hormone release. Science (1996) 5.45

PmrA-PmrB-regulated genes necessary for 4-aminoarabinose lipid A modification and polymyxin resistance. Mol Microbiol (1998) 5.01

Association of diabetes mellitus and chronic hepatitis C virus infection. Hepatology (1999) 4.59

Molecular characterization of receptor binding proteins and immunogens of virulent Treponema pallidum. J Exp Med (1980) 4.19

Minocycline inhibits caspase-1 and caspase-3 expression and delays mortality in a transgenic mouse model of Huntington disease. Nat Med (2000) 4.18

Specific lipopolysaccharide found in cystic fibrosis airway Pseudomonas aeruginosa. Science (1999) 3.98

The Saccharomyces cerevisiae FKS1 (ETG1) gene encodes an integral membrane protein which is a subunit of 1,3-beta-D-glucan synthase. Proc Natl Acad Sci U S A (1994) 3.90

Follow-up study of two hundred admissions to a residential home. Age Ageing (1976) 3.81

Regulation of synthesis of glutamine synthetase by adenylylated glutamine synthetase. Proc Natl Acad Sci U S A (1975) 3.56

Orexigenic action of peripheral ghrelin is mediated by neuropeptide Y and agouti-related protein. Endocrinology (2004) 3.54

A purely geometric module in the rat's spatial representation. Cognition (1986) 3.54

Protein sigma 1 is the reovirus cell attachment protein. Virology (1981) 3.48

Antibacterial agents that inhibit lipid A biosynthesis. Science (1996) 3.38

Differential expression and function of two homologous subunits of yeast 1,3-beta-D-glucan synthase. Mol Cell Biol (1995) 3.27

DNA-dependent DNA polymerases I and II from normal human-blood lymphocytes. Proc Natl Acad Sci U S A (1972) 3.27

Distribution of mRNA encoding the growth hormone secretagogue receptor in brain and peripheral tissues. Brain Res Mol Brain Res (1997) 3.21

Mutations that alter the ability of the Escherichia coli cyclic AMP receptor protein to activate transcription. Nucleic Acids Res (1990) 3.08

Regulation of glutamine synthetase formation in Escherichia coli: characterization of mutants lacking the uridylyltransferase. J Bacteriol (1978) 3.07

Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. J Med Chem (1988) 3.04

A new class of angiotensin-converting enzyme inhibitors. Nature (1980) 3.03

Projections of the medial and lateral prefrontal cortices to the amygdala: a Phaseolus vulgaris leucoagglutinin study in the rat. Neuroscience (1996) 3.01

Columns for visual features of objects in monkey inferotemporal cortex. Nature (1992) 2.93

Cloning of an avermectin-sensitive glutamate-gated chloride channel from Caenorhabditis elegans. Nature (1994) 2.92

Nature of phosphorus limitation in the ultraoligotrophic eastern Mediterranean. Science (2005) 2.79

Elevated expression of axin2 and hnkd mRNA provides evidence that Wnt/beta -catenin signaling is activated in human colon tumors. Proc Natl Acad Sci U S A (2001) 2.77

cisRED: a database system for genome-scale computational discovery of regulatory elements. Nucleic Acids Res (2006) 2.75

Regulation of vascular endothelial growth factor-dependent retinal neovascularization by insulin-like growth factor-1 receptor. Nat Med (1999) 2.74

Initial characterization of monoclonal antibodies against human monocytes. Proc Natl Acad Sci U S A (1980) 2.61

A new nomenclature for IL-1-family genes. Trends Immunol (2001) 2.57

Analysis of the reinforcement and extinction components in DRO contingencies with self-injury. J Appl Behav Anal (1993) 2.56

Viral and cellular DNA polymerase: comparison of activities with synthetic and natural RNA templates. Science (1972) 2.53

Extinction of self-injurious escape behavior with and without instructional fading. J Appl Behav Anal (1993) 2.52

An analysis of reinforcer substitutability using object manipulation and self-injury as competing responses. J Appl Behav Anal (1997) 2.47

Genetic and physical mapping of the Lps locus: identification of the toll-4 receptor as a candidate gene in the critical region. Blood Cells Mol Dis (1998) 2.46

Translocation of SAPK/JNK to mitochondria and interaction with Bcl-x(L) in response to DNA damage. J Biol Chem (2000) 2.44

Relationship between regional cardiac hyperinnervation and ventricular arrhythmia. Circulation (2000) 2.44

Momentum and extinction effects on self-injurious escape behavior and noncompliance. J Appl Behav Anal (1994) 2.41

Synthesis of a 600-nucleotide-long plus-strand DNA by virions of Moloney murine leukemia virus. Proc Natl Acad Sci U S A (1979) 2.39

Isolation and tissue distribution of type-C virus and viral components from a gibbon ape (Hylobates lar) with lymphocytic leukemia. Virology (1978) 2.37

Characterization of anti-reovirus immunoglobulins secreted by cloned hybridoma cell lines. Virology (1981) 2.36

Detection of retroviral antibodies in primary biliary cirrhosis and other idiopathic biliary disorders. Lancet (1998) 2.31

Receptors for polytropic and xenotropic mouse leukaemia viruses encoded by a single gene at Rmc1. Nat Genet (1999) 2.28

Organization of minicircle genes for guide RNAs in Trypanosoma brucei. Cell (1990) 2.28

Determination of Indole-3-acetic Acid in Douglas Fir Using a Deuterated Analog and Selected Ion Monitoring: Comparison of Microquantities in Seedling and Adult Tree. Plant Physiol (1978) 2.26

Antimicrobial substance from a human Lactobacillus strain. Antimicrob Agents Chemother (1987) 2.25

Purification of complexes of nuclear oncogene p53 with rat and Escherichia coli heat shock proteins: in vitro dissociation of hsc70 and dnaK from murine p53 by ATP. Mol Cell Biol (1988) 2.25

Sustained atrial tachycardia in adult patients. Electrophysiological characteristics, pharmacological response, possible mechanisms, and effects of radiofrequency ablation. Circulation (1994) 2.24

Discovery of a small molecule insulin mimetic with antidiabetic activity in mice. Science (1999) 2.21

Gentamicin resistance in Staphylococcus aureus. Lancet (1976) 2.18

An analysis of the reinforcing properties of hand mouthing. J Appl Behav Anal (1995) 2.18

Prolonged and effective blockade of tumor necrosis factor activity through adenovirus-mediated gene transfer. Proc Natl Acad Sci U S A (1994) 2.18

Targeted deletion of the Vgf gene indicates that the encoded secretory peptide precursor plays a novel role in the regulation of energy balance. Neuron (1999) 2.15

Rho3 of Saccharomyces cerevisiae, which regulates the actin cytoskeleton and exocytosis, is a GTPase which interacts with Myo2 and Exo70. Mol Cell Biol (1999) 2.15

HIV-1 protease specificity of peptide cleavage is sufficient for processing of gag and pol polyproteins. Biochem Biophys Res Commun (1988) 2.14

Essential role of growth hormone in ischemia-induced retinal neovascularization. Science (1997) 2.11

Activation of PPARdelta alters lipid metabolism in db/db mice. FEBS Lett (2000) 2.10

Gelsolin deficiency blocks podosome assembly and produces increased bone mass and strength. J Cell Biol (2000) 2.07

Reemergence and extinction of self-injurious escape behavior during stimulus (instructional) fading. J Appl Behav Anal (1994) 2.05

Synthesis of murine leukemia virus plus strong stop DNA initiates at a unique site. J Biol Chem (1982) 2.03

Can age and sex explain the variation in COPD rates across large urban cities? A population study in Canada. Int J Tuberc Lung Dis (2011) 2.01

The CALM1 core promoter polymorphism is not associated with hip osteoarthritis in a United Kingdom Caucasian population. Osteoarthritis Cartilage (2005) 1.99

The pterin component of the molybdenum cofactor. Structural characterization of two fluorescent derivatives. J Biol Chem (1984) 1.99

The interaction of a series of hybridoma IgGs with reovirus particles. Demonstration that the core protein lambda 2 is exposed on the particle surface. Virology (1981) 1.98

Regulation of Carbon Partitioning to Respiration during Dark Ammonium Assimilation by the Green Alga Selenastrum minutum. Plant Physiol (1990) 1.98

Regulation of the synthesis of glutamine synthetase by the PII protein in Klebsiella aerogenes. Proc Natl Acad Sci U S A (1980) 1.97

Regulation of expression of IL-4 alleles: analysis using a chimeric GFP/IL-4 gene. Immunity (2001) 1.97

GP73, a novel Golgi-localized protein upregulated by viral infection. Gene (2000) 1.96

Orphan G-protein-coupled receptors and natural ligand discovery. Trends Pharmacol Sci (2001) 1.94

Stat6 is necessary and sufficient for IL-4's role in Th2 differentiation and cell expansion. J Immunol (2001) 1.93

Biochemical characterization of the protein tyrosine kinase homology domain of the ErbB3 (HER3) receptor protein. Biochem J (1997) 1.91

Vascular endothelial growth factor: a new member of the platelet-derived growth factor gene family. Biochem Biophys Res Commun (1989) 1.91

Timing light and tone signals in pigeons. J Exp Psychol Anim Behav Process (1989) 1.90

Selective inhibitors of biosynthesis of aminergic neurotransmitters. Nature (1978) 1.88

Effects of exposure to mercury in the manufacture of chlorine. Am Ind Hyg Assoc J (1971) 1.88

Phosphonomycin: structure and synthesis. Science (1969) 1.87

Outcome of pediatric thromboembolic disease: a report from the Canadian Childhood Thrombophilia Registry. Pediatr Res (2000) 1.86

Single amino-acid changes that confer constitutive activation of mTOR are discovered in human cancer. Oncogene (2010) 1.85

Within-session patterns of self-injury as indicators of behavioral function. Res Dev Disabil (1994) 1.84

Role of papillary muscle in the generation and maintenance of reentry during ventricular tachycardia and fibrillation in isolated swine right ventricle. Circulation (1999) 1.83

Glutamine synthetase of Klebsiella aerogenes: properties of glnD mutants lacking uridylyltransferase. J Bacteriol (1978) 1.83

Molecular cloning and partial sequencing of hepatitis A viral cDNA. J Virol (1985) 1.82

A novel mechanism for the insulin-like effect of vanadate on glycogen synthase in rat adipocytes. J Biol Chem (1984) 1.79

Current research on the influence of establishing operations on behavior in applied settings. J Appl Behav Anal (2000) 1.79

A blood test for multiple sclerosis based on the adherence of lymphocytes to measles-infected cells. N Engl J Med (1976) 1.78

Internal lysine palmitoylation in adenylate cyclase toxin from Bordetella pertussis. Science (1994) 1.78

Assembly of microtubules at the tip of growing axons. Nature (1986) 1.77

A secreted Salmonella protein induces a proinflammatory response in epithelial cells, which promotes neutrophil migration. Proc Natl Acad Sci U S A (2000) 1.76

Vein of marshall cannulation for the analysis of electrical activity in patients with focal atrial fibrillation. Circulation (2000) 1.76

Natural history of Streptococcus sanguinis in the oral cavity of infants: evidence for a discrete window of infectivity. Infect Immun (2000) 1.75