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aminoisobutyric acid BAIBA is a
2019-12-16

β-aminoisobutyric EI1 (BAIBA) is a natural catabolite of the branched-chain amino acid thymine. BAIBA was recently found to reduce inflammation in skeletal muscle via the AMP-activated protein kinase (AMPK)-peroxisome proliferator-activated receptor (PPAR)δ signaling pathway. BAIBA reportedly enhan
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Here we explored the relative contribution of D like and
2019-12-16

Here we explored the relative contribution of D1-like and D2-like receptor subtypes in the control of glutamate release, as well as their pharmacological properties and their interactions modulating the release. The pharmacological parameters (EC50 and Emax) of dopamine for the different types of re
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br Introduction The allergic response is a complex process i
2019-12-16

Introduction The allergic response is a complex process involving the interaction of several mediators; among these, cysteinyl leukotrienes (CysLTs) represent one of the most important actors in the pathogenesis of airway allergic diseases such as allergic rhinitis and asthma [1]. Pharmacological
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In this review we first introduce the in vivo metabolism
2019-12-16

In this review, we first introduce the in vivo metabolism profile of VD3, and the mediation of Cyp3a gene transcription by PXR and CAR in humans, mice and rats. We then focus on the species-specific VDR-dependent regulation of human (CYP3A4, CYP3A5 and CYP3A7), mouse (mainly CYP3A11 and CYP3A13), an
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Prostaglandins PGs are lipid mediators that
2019-12-16

Prostaglandins (PGs) are lipid mediators that exhibit a variety of physiological properties by interacting specific G protein-coupled receptors (GPCRs) [10]. PGD2 is synthesized from PGH2 through two distinct PGD synthases; lipocalin-type PGD synthase (L-PGDS) and hematopoietic PGD synthase (H-PGDS)
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It is well known that the tumor suppressor p plays
2019-12-16

It is well known that the tumor suppressor p53 plays an important role in regulating the phospholipase inhibitor and cellular senescence [43,46,48]. For example, FOXO4 could interact with P53, which selectively induced apoptosis in senescent cells [48]. In addition, loss of MECP2 was found to lead
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Terazosin br Effects of estrogen on
2019-12-16

Effects of estrogen on vascular function Atherosclerosis is a chronic inflammatory condition of the vascular wall (Figure 1) that can be converted to an acute clinical event by the induction of plaque rupture or erosion, leading to thrombosis [58]. This perpetuating process is characterized by ph
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Although the presence of calcium in RHA
2019-12-16

Although the presence of calcium in RHA-P active site is confirmed by the homology modeling, some additional observations can be made following the metal depletion and reconstitution experiments performed on RHA-Phis. EDTA-treated RHA-Phis recovers its activity in the presence of divalent cations su
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Dasatinib Monohydrate Our previous high throughput screening
2019-12-16

Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based Dasatinib Monohydrate assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21
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br Early developments Historically the advent
2019-12-16

Early developments Historically, the advent of SMEPT can be traced to the 1980′s, where the first example of localized prodrug conversion was achieved using a judiciously placed enzyme – in order to achieve a localized feed of 5-fluorouracil (5-FU). Immobilization of E. coli-derived cytosine deam
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The discoidin domain receptors DDR and DDR are
2019-12-16

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases that are activated by different types of collagen (Shrivastava et al., 1997, Vogel et al., 1997). Both receptors interact with a number of fibrillar collagens, and DDR1, but not DDR2, is also activated by the network-formin
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Two parameters were extracted from these experiments to
2019-12-16

Two parameters were extracted from these experiments to compare the interactions of the three compounds with ct-DNA. The association constant K for the binding of the naphthalimide derivatives to ct-DNA was calculated by fitting the evolution of the fluorescence spectra with a 1:1 binding model usin
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In our recent study we established a procedure to examine
2019-12-16

In our recent study, we established a procedure to examine the chromatin binding of XRCC4 using a biochemical fractionation analysis using a detergent Nonidet P-40 [22]. In this study, we investigated the role of LIG4 and its subdomains in the recruitment of XRCC4/LIG4 complex to chromatin. Mater
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AAG has a broad substrate
2019-12-16

AAG has a broad substrate specificity and besides 3-methyladenine can excise other altered purine residues, such as the minor lesions hypoxanthine and 1, N6-ethenoadenine from DNA. AAG initially activates these neutral base lesions by protonation of the base to allow for general teniposide catalysi
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br Introduction The discoidin domain receptors DDRs DDR and
2019-12-16

Introduction The discoidin domain receptors (DDRs), DDR1 and DDR2, are unique among the receptor tyrosine kinases (RTKs) in being activated by interaction with the extracellular matrix [1], [2]. Binding to triple-helical collagen is mediated by the receptor extracellular domains that include an N
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