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ionophore br Acknowledgments We would like to acknowledge Je
2021-11-06
Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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Some previous findings indicate that GALP has an
2021-11-06
Some previous findings indicate that GALP has an influence on AVP and OT secretion from the posterior pituitary gland. Cunningham et al. (2004) noted that the expression of GALP mRNA was increased in the neurohypophysis of lactating rats compared to non-lactating rats, whereas GALP mRNA expression i
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Somatostatin analogues are among the first peptide based dru
2021-11-06
Somatostatin analogues are among the first peptide-based drugs used in cancer imaging and therapy (for review see Reubi, 2003). Treatment of tumors by the use of peptide analogues labeled with cytotoxic agents acting via specific receptors is also under investigation for neuropeptide Y (Koglin and B
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Having shown that some of
2021-11-06
Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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During the activation of the coagulation cascade factor
2021-11-06
During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium ST 2825 on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit platele
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herpes simplex virus The site of paracetamol action
2021-11-06
The site of paracetamol action remains controversial. Some publications are in favor of a central action (Barrière et al., 2013, Dogrul et al., 2012, Mallet et al., 2010, Pickering et al., 2006), while others report a peripheral action (Dani et al., 2007, Ferreira et al., 1978). FAAH is a ubiquitous
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The effect of combined A and PD treatment on the
2021-11-06
The effect of combined A-192621 and PD 155080 treatment on the dna synthesis during endotoxin infusion is quite different compared to either drug used alone (Wanecek et al., 1999). After administration of both antagonists in combination, cardiac index increased to baseline values within 30 min, and
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The GPR receptor is also emerging as an
2021-11-05
The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also
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The pharmacokinetics of was obtained
2021-11-05
The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indicat
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Acknowledgments We would like to thank Dr Greg Morriello Mr
2021-11-05
Acknowledgments We would like to thank Dr. Greg Morriello, Mr. Lehua Chang, Mr. Chris Moyes and Mr. Nam Fung Kar for intermediate 3 syntheses. Cheng Zhu would like to thank Dr. Milana Maletic, Mr. Kake Zhao and Mrs. Wanying Sun for helpful discussions. Introduction Glucagon-like peptide-1 (GLP-
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Introduction CD T cell recovery after initiation of combinat
2021-11-05
Introduction CD4+ T cell recovery after initiation of combination antiretroviral therapy (cART) is essential for restoring immune function in HIV-positive individuals [1]. However, CD4 recovery is variable and is affected by factors such as biological sex [2], [3], race [4], BMI [5], geographic reg
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Foreign polypeptide antigens can be incorporated into
2021-11-05
Foreign polypeptide antigens can be incorporated into VLPs to create “chimeric” structures, either as fusions to either end of the VLP capsid (coat) protein (CP) or as additions to well-presented loops [18]. This kind of direct fusion to the coat is usually good for small peptides, however, larger p
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The precise mechanisms of action of PBA are as yet
2021-11-05
The precise mechanisms of action of 4-PBA are as yet ambiguous. Its capacity as a chemical chaperone has been thoroughly documented for the ABC transporter family in particular (Prulière-Escabasse et al., 2007; Iram and Cole, 2014; Gordo-Gilart et al., 2016; Pomozi et al., 2017). 4-PBA has been clas
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Here we reported series of carbohydrate modified compounds c
2021-11-05
Here, we reported series of carbohydrate-modified compounds containing a dibromo substituted benzene ring which was derived from the red alga (). The conformation flexibility of 2-NBDG and their polyol structures give them many unique biological properties as we have described earlier. More intere
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br Ghrelin interactions with the opioid system The endogenou
2021-11-05
Ghrelin interactions with the opioid system The endogenous opioid system is an important regulator of appetite and metabolism (Bodnar, 2017, Nogueiras et al., 2012). In fact, several pharmacological studies have demonstrated that agonists of the three opioid receptors (mu, kappa, and delta) incre
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