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Response of melanocortin–4 receptor–deficient mice to anorectic and orexigenic peptides
Mutations reducing the functional activity of leptin, the leptin receptor, α–melanocyte stimulating hormone (α–MSH) and the melanocortin–4 receptor (Mc4r) all lead to obesity in mammals. Moreover,Expand
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Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
Human immunodeficiency virus type-1 (HIV-1) integrase is one of the three virally encoded enzymes required for replication and therefore a rational target for chemotherapeutic intervention in theExpand
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Neurokinin B is a preferred agonist for a neuronal substance P receptor and its action is antagonized by enkephalin.
Receptor specificity of the substance P-related peptides neurokinin A and neurokinin B was studied in the isolated guinea pig ileum. Substance P and the recently discovered neurokinins elicitExpand
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Efficient and regulated erythropoietin production by naked DNA injection and muscle electroporation.
We show that an electric treatment in the form of high-frequency, low-voltage electric pulses can increase more than 100-fold the production and secretion of a recombinant protein from mouse skeletalExpand
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Highly selective agonists for substance P receptor subtypes.
The existence of a third tachykinin receptor (SP‐N) in the mammalian nervous system was demonstrated by development of highly selective agonists. Systematic N‐methylation of individual peptide bondsExpand
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Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel
5-Aryl-2-(trifluoroacetyl)thiophenes were identified as a new series of class II HDAC inhibitors (HDACi). Further development of this new series led to compounds such as 6h, a potent inhibitor ofExpand
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4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.
The dihydroxypyrimidine carboxamide 4a was discovered as a potent and selective HIV integrase strand transfer inhibitor. The optimization of physicochemical properties, pharmacokinetic profiles, andExpand
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Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.
Human immunodeficiency virus type-1 (HIV-1) integrase, one of the three constitutive viral enzymes required for replication, is a rational target for chemotherapeutic intervention in the treatment ofExpand
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Phosphoramidate prodrugs of 2'-C-methylcytidine for therapy of hepatitis C virus infection.
The application of a phosphoramidate prodrug approach to 2'-C-methylcytidine (NM107), the first nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase, is reported. 2'-C-Methylcytidine,Expand
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PEGylation of Neuromedin U yields a promising candidate for the treatment of obesity and diabetes.
Neuromedin U (NMU) is an endogenous peptide, whose role in the regulation of feeding and energy homeostasis is well documented. Two NMU receptors have been identified: NMUR1, expressed primarily inExpand
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