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Viral RNA annealing activities of human immunodeficiency virus type 1 nucleocapsid protein require only peptide domains outside the zinc fingers.
TLDR
It is shown here that synthetic NCp7 with or without the two zinc fingers has the RNA annealing activities of NCp15, and could be used as a model for the design of antiviral agents. Expand
Inhibiting the breakdown of endogenous opioids and cannabinoids to alleviate pain
TLDR
The effects of Dual enkephalinase inhibitors and FAAH inhibitors are compared and the progress in their rational design is described, to consider the challenges in their clinical development and opportunities for combination therapies. Expand
Identification of metabolic pathways of brain angiotensin II and III using specific aminopeptidase inhibitors: predominant role of angiotensin III in the control of vasopressin release.
TLDR
Ang III behaves as one of the main effector peptides of the brain renin-angiotensin system in the control of vasopressin release, demonstrating for the first time that APA and APN are involved in vivo in the metabolism of brain Ang II and Ang III. Expand
Brain renin-angiotensin system blockade by systemically active aminopeptidase A inhibitors: a potential treatment of salt-dependent hypertension.
TLDR
It is reported that brain AngIII exerts a tonic stimulatory effect on blood pressure in a model of salt-dependent hypertension, the DOCA-salt rat, characterized by a depressed systemic but a hyperactive brain RAS, and suggested that RB150, a potent systemically active APA inhibitor, could be the prototype of a new class of antihypertensive agents for the treatment of certain forms of hypertension. Expand
The enkephalinase inhibitor thiorphan shows antinociceptive activity in mice
TLDR
Thiorphan is reported here that this compound, thiorphan [(DL-3-mercapto-2-benzylpropanoyl)-glycine; patent no. 8008601] protects the enkephalins from the action of enkephalinase in vitro in nanomolar concentration and in vivo after either intracerebroventricular or systemic administration. Expand
Angiotensin III: a central regulator of vasopressin release and blood pressure
TLDR
New insights are summarized into the predominant role of brain AngIII in the control of vasopressin release and blood pressure and the fact that brain aminopeptidase A, the enzyme forming central AngIII, could constitute a putative central therapeutic target for the treatment of hypertension is underlined. Expand
Conformational behaviour of the active and inactive forms of the nucleocapsid NCp7 of HIV-1 studied by 1H NMR.
TLDR
The results suggest that the spatial proximity of the zinc fingers induced by the peptide linker, plays a critical role in encapsidation of genomic RNA and morphogenesis of HIV-1 infectious particles. Expand
Autoradiographic comparison of the distribution of the neutral endopeptidase "enkephalinase" and of mu and delta opioid receptors in rat brain.
TLDR
High levels of enkephalinase and mu opioid binding sites were present at the level of the periaqueductal gray matter and in the substantia gelatinosa of the spinal cord, regions where only sparse delta opioid receptors could be detected. Expand
Aminopeptidase A inhibitors as potential central antihypertensive agents.
TLDR
In rats, ICV injection of the selective APA inhibitor EC33 blocked the pressor response of exogenous AngII, suggesting that the conversion of AngII to Ang III is required to increase blood pressure (BP), and demonstrates that AngIII is a major effector peptide of the brain RAS, exerting tonic stimulatory control over BP. Expand
Expression of neutral endopeptidase (enkephalinase) in heterologous COS-1 cells. Characterization of the recombinant enzyme and evidence for a glutamic acid residue at the active site.
TLDR
An expression vector is constructed in which the rabbit kidney cDNA encoding the entire neutral endopeptidase sequence is introduced downstream from the SV40 virus early promotor, which identifies Glu-584 as one of the important residues responsible for the catalytic activity of the enzyme. Expand
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