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The known crystal structures of class C GPCR
2024-02-22
The known crystal structures of class C GPCR VFTs do not include attached TM domains, therefore current conformational data may not accurately reflect the dynamics of extracellular domains in full-length receptors. Nevertheless, compelling mechanisms of signal transduction can still be postulated. S
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Most of lipid lowering agents
2024-02-22
Most of lipid-lowering agents have many therapeutic problems with severe side effects, while dietary fibers as lipid lowering therapy are safer. Chitosan (CS) is a dietary fiber biodegradable, biocompatible and has many health benefits including wound healing, antiinflammatory, anti-cancers, immune-
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Although the gene that encodes DHFR has been
2024-02-22
Although the gene that encodes DHFR has been strongly conserved during evolution, subtle differences in the active sites of bacterial, human and parasite Griseofulvin have been exploited to develop DHFR inhibitors specific to particular pathogens 1, 3. For example, pyrimethamine and cycloguanil bin
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It thus appeared reasonable that AR needed to be inhibited
2024-02-21
It thus appeared reasonable that AR needed to be inhibited and great experimental efforts began which are still on-going [6]. Indeed, hundreds of ARIs have been characterized but no significant drug development has followed. The case of Sorbinil, which did not pass clinical trials is emblematic [7]
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ALDHs also act as opposite roles in the initiation and
2024-02-21
ALDHs also act as opposite roles in the initiation and development of carcinoma. For example, ALDH2, as a key enzyme which oxidises acetaldehyde, participates in alcohol metabolism and is associated with alcohol-mediated carcinogenesis [37]. It has been reported that up to 8% of the world's populati
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The present study determined the effect of DCA on VSMC
2024-02-21
The present study determined the effect of DCA on VSMC calcification in vitro and in atherosclerotic ApoE-/- mice in vivo. We found that SRT2104 non-toxic concentrations of DCA, did not affect VSMC viability, induced calcification of VSMC in culture and increased atherosclerotic vascular calcificat
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An alternative to the agonist
2024-02-21
An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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br Co http www apexbt com media
2024-02-21
Conclusions This paper is the first meta-analysis about the association between SRD5A2 V89L polymorphism and hypospadias risk. The results of this meta-analysis have revealed that V89L polymorphism definitely increases the risk of hypospadias, and the C allele is a genetic risk factor for hypospa
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The altered frequency of CD T cells in LO
2024-02-21
The altered frequency of CD4+ T cddo in 5-LO−/− mice led us to hypothesize that these leukocytes could be exerting a primary control of the inflammatory response. In fact, the lack of 5-LO resulted in the accumulation of CD4+CD25+ cells expressing Treg markers. It is plausible to speculate that 5-L
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In addition to the data provided by the
2024-02-21
In addition to the data provided by the Ki16425 treatment in the K/BxN arthritis model, new findings from the study of two new LPA receptor antagonists confirm the involvement of the LPA pathway in the pathogenesis of experimental arthritis. In the study by Miyabe et al., the authors reported the tr
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Chronic inflammation is associated with
2024-02-21
Chronic inflammation is associated with both initiation and progression of many neoplastic conditions [149], and ATX may be a player in the process. ATX/LPA signaling is positively correlated with the invasive and metastatic potential of several cancers including melanoma, breast cancer, ovarian can
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Our current knowledge on autophagy
2024-02-21
Our current knowledge on autophagy broadly differentiates it into three types: macroautophagy, microautophagy, and chaperone-mediated autophagy. Macroautophagy mainly involves the sequestration of cytoplasmic contents in a double-walled membrane followed by the fusion with the lysosomes. The lysosom
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Although the LB domains of
2024-02-21
Although the LB2 domains of mGlu receptors have not been shown to form an extensive interface during activation, they do draw closer to each other, as demonstrated in crystal structures (Kunishima et al., 2000, Muto et al., 2007, Tsuchiya et al., 2002) and by FRET analysis (Doumazane et al., 2013, V
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br Materials and methods br Results br Discussion In this
2024-02-21
Materials and methods Results Discussion In this study, we administrated BDE-153 to newborn rat pups at PND 10 and cultured primary neurons, measured neuronal apoptosis and LDH activity in vivo and in vitro, then explored the possible predominant pathway underlying the neuronal apoptosis by
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The functional similarity between GPR and APLNR ie
2024-02-21
The functional similarity between GPR25 and APLNR, ie both can be activated by Apelin and Apela and are coupled to Gi-cAMP signaling pathway (Fig. 2, Fig. 3, Fig. 4), strongly suggests that GPR25 signaling may play important physiological and pathological roles in vertebrates more or less similar to
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