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Compounds were profiled for their inhibitory activity agains
2024-04-01

Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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GSK503 These results from the present study are summarized i
2024-04-01

These results from the present study are summarized in Table 1. Eight drugs (doxorubicin, epirubicin, daunorubicin, idarubicin, irinotecan, imatinib, sunitinib and gefitinib) inhibited 5-HT-induced 5-HT3A and 5-HT3AB currents; three (irinotecan, topotecan and mitoxantrone) showed different responses
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Skeletal pain associated with bone fracture is another
2024-04-01

Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model
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The ambiguity surrounding the role played by the
2024-04-01

The ambiguity surrounding the role played by the 15-LOXs in malignant biological processes stems also from the limitations of current animal models, and especially the usage of its 12/15-LOX murine homolog, which can also catalyze the production of 12-HETE. Indeed, the proinflammatory effect of 12-H
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Several alterations have been or can be
2024-04-01

Several alterations have been or can be associated to the decreased tolerance of steatotic liver to I/R injury. Previous studies demonstrated that upregulation of the mitochondrial uncoupling protein-2 (UP2) is strictly related to the increase of I/R injury in steatotic liver [4]. UPR induction is c
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ASK has been identified as
2024-04-01

ASK2 has been identified as an ASK1 binding protein (Wang et al., 1998). ASK1 supports the stability and active configuration of ASK2 in the heteromeric complex, while ASK2 has been found to activate ASK1 by direct phosphorylation (Takeda et al., 2007). Unlike ASK1, which is ubiquitously expressed i
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The most likely explanation for the species differences in
2024-04-01

The most likely explanation for the species differences in aromatase distribution and the unique SGC707 distribution in humans is the unique location, size and highly elaborate organization of the human aromatase gene (e.g. Bulun et al., 2003). The human Cyp19 is a large gene located on chromosome 1
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AP was originally described as a heterodimer
2024-03-30

AP-1 was originally described as a heterodimer of the bZIP proteins c-Jun and c-Fos. The experiments described here showed that stimulation of TRPV1 channels induced the expression of both of these classical constituents of AP-1. The essential role of both proteins was analyzed in a series of experi
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Topotecan HCl A Belgian review on perioperative management
2024-03-30

A Belgian review [9] (2011) on perioperative management of drugs recommends not using ACEI/ARBs due to the same reason. Another 2014 French [10] publication on the management of antihypertensive drugs in the perioperative period suggests withholding this medication before surgery even though they a
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br Introduction Androgens have been shown to regulate severa
2024-03-30

Introduction Androgens have been shown to regulate several neural functions ranging from reproduction to mood and cognitive abilities. This property starts as early as the perinatal period, which is characterized by prenatal and postnatal surges of gonadal testosterone, and continues through pube
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Cell surface metalloproteases coordinate signaling
2024-03-30

Cell surface metalloproteases coordinate signaling during development, tissue homeostasis, and disease. A disintegrin and metalloprotease 17 (ADAM17) is a well-characterized member among ADAM family, which mediates the cleavage of various cell surface proteins (Black, 2002, Black et al., 1997, Dello
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Leupeptin Glu Gln Asp and Asn the main amino acids presented
2024-03-30

Glu, Gln, Asp, and Asn, the main Leupeptin presented in the present study, are involved in nitrogen assimilation and transport processes within the plants. Furthermore, they are used to build up reserves during periods of nitrogen availability for subsequent use in growth, defense, and reproductive
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The finding that OCT is expressed in the nucleus accumbens
2024-03-30

The finding that OCT3 is expressed in the nucleus accumbens (Gasser et al., 2009) suggests that inhibition of this transporter may underlie previously described effects of glucocorticoids on extracellular DA concentrations and indicates that DA clearance in this region is not mediated exclusively by
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br Experimental procedures br Results br Discussion br Ackno
2024-03-30

Experimental procedures Results Discussion Acknowledgments Introduction β-Adrenergic receptors (β-ARs) belong to the superfamily of membrane proteins termed G protein-coupled receptors. β-ARs are distributed in the effector K-115 of most of the sympathetic nerve fibers, and the recept
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NLX a k a F
2024-03-30

NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in 7ACC2 to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it has sho
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