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Based on pharmacophore modeling a good HDAC inhibitor has at
2021-09-06

Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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Several studies have found that GPR possesses a
2021-09-06

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Febuxostat expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Ri
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Fmoc-Cys(Trt)-ol receptor GPR and TRPV co localized in small
2021-09-06

GPR35 and TRPV1 co-localized in small- and medium-diameter DRG neurons. Nociceptive (Aδ- and C-fiber) neurons expressing TRPV1 mediate hyperalgesia, neurogenic inflammation, and neuropathic pain [12]. The cAMP-protein kinase A (PKA) dependent modifications of TRPV1 currents have been demonstrated in
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Gap junctions mediate electrical coupling between cells
2021-09-03

Gap junctions mediate electrical coupling between cells by conducting direct ionic currents and thereby modulate their electrical activity (Hormuzdi et al., 2004). In the nervous system, electrical coupling organizes network activity by amplifying and synchronizing neuronal firing (Galarreta and Hes
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br Introduction As a fundamental metal dependent hydrolytic
2021-09-03

Introduction As a fundamental metal-dependent hydrolytic enzyme, inorganic pyrophosphatase (PPase) exhibits a specific catalytic ability, in which one molecule of inorganic pyrophosphate (PPi) can be transformed into two orthophosphate (Pi) ions [1,2]. The process of transformation is extremely e
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CC is a widespread disorder affecting up to
2021-09-03

CC is a widespread disorder affecting up to 20% of people worldwide, which also deteriorates the quality of life of patients and causes a substantial economic burden to society. There are 3 categories of CC: normal-transit constipation, slow-transit constipation and defecatory or rectal evacuation d
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Immunohistochemistry using anti FFAR antibodies
2021-09-03

Immunohistochemistry using anti-FFAR1 antibodies revealed immunoreactivity for FFAR1 in association with the cell membrane of the hepatocytes (Figure 2). However, the anti-FFAR2 antibody was not suitable for immunohistochemistry under the tested conditions (data not shown). Fatty liver is an import
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Factor Xa FXa has emerged
2021-09-03

Factor Xa (FXa) has emerged as a particularly promising target for the development of effective anticoagulant drugs because FXa acts at the convergence point of the extrinsic and intrinsic coagulation pathways. It efficiently catalyzes the conversion of prothrombin to thrombin with one molecule of F
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The synthesis route of strobol C started
2021-09-03

The synthesis route of strobol C started from kirenol, which was treated with phosphomolybdic dichloroacetate hydrate in acetone to afford isopropylidenkirenol () as illustrated in . Treatment of with acetic anhydride in a mixture of dry pyridine, gave fully protected intermediate in 84.5% yields
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The above inferences concluded that histidine is
2021-09-03

The above inferences concluded that histidine is enhancing the overall stability and rigidity of the protein which further might be restraining the protein during the transition from inactive to active state and vice-versa present in the SANT domain. Since the SANT domain binds with histone via elec
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Importantly the regulation of the Hippo pathway
2021-09-03

Importantly, the regulation of the Hippo pathway by metabolic networks, such as by glycolysis39, 40, hexosamine biosynthesis41, 42, and mevalonate synthesis43, 44, as well as by nutrient-sensing pathways including AMP-activated protein kinase (AMPK) 40, 45, 46 and mTOR 47, 48, 49, 50, was recently d
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BWX 46 synthesis Sequences of HKI and HKII from humans were
2021-09-03

Sequences of HKI and HKII from humans were compared to those of the Atlantic salmon to better understand the observation of HKI movement to the mitochondrial fraction in this study, as HKI in mammals is commonly assumed to be mostly passively regulated by product inhibition, with little evidence of
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br Funding This study was supported by grants in
2021-09-03

Funding This study was supported by grants-in-aid for scientific research from the Japan Society for Promotion of Science (grant 16K186462 to Dr. Tomizawa, grant 16K19989 to Dr. Kobayashi, and grant 16H05433 to Dr. Mitsudomi) and a research grant from Boehringer-Ingelheim (to T. Mitsudomi). Co
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Anti apoptotic Bcl proteins have become attractive
2021-09-03

Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients w
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Our data demonstrate that cobas HCV
2021-09-03

Our data demonstrate that cobas HCV’s performance characteristics meet these requirements, making the assay useful in the management of therapy for chronic hepatitis C. We documented that cobas HCV has the requisite LOD, measureable range (15 − 1.0E + 08 IU/mL) and precision allowing for baseline HC
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