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Sirolimus rapamycin and everolimus both of which are
2022-09-17

Sirolimus (rapamycin) and everolimus, both of which are mTOR inhibitors, are released by commonly used first- and second-generation DES. Considering the relatively high rates of the target vessel failure with currently available DES [12,14,16,45,46], there is a need for a novel drug strategy that pr
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In the FARM motifs of GGPPSs hydrophobic amino
2022-09-17

In the FARM motifs of GGPPSs, hydrophobic Pirfenidone are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta CA possesses GGPP synthase (GGP
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In humans mutations in KDM A KDM B and KDM
2022-09-17

In humans, mutations in KDM5A, KDM5B, and KDM5C are found in patients with ID, implicating KDM5-regulated transcription in the development or activity of neuronal tissues (Vallianatos and Iwase, 2015). KDM5D is Y-linked, and its role in cognition remains uncharacterized. Mutations in KDM5C are the m
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This crosstalk may be responsible for the beneficial
2022-09-17

This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on SNS-314 Mesylate pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of high-dose
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According to the experimental data HKI preferentially
2022-09-17

According to the experimental data, HKI preferentially binds to the mitochondrial inter-membrane contact sites formed by ANT and VDAC [[5], [6], [7],27], mainly via the VDAC1 isoform [7,8]. These electrogenic contact sites allow application of a part of IMP to MOM by transferring phosphoryl groups f
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Subcellular domains where Rac is active show limited Rho act
2022-09-16

Subcellular domains where Rac is active show limited Rho activity and vice versa (Fig. 4). This distinctive patterning in Rho activity is achieved via the downstream Rac effector Par6, an important part of the so-called Par polarity complex. In primary epithelium, the cytoskeleton and associated Rho
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br Results and discussion br Conclusions In
2022-09-16

Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10
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br Acknowledgments br Introduction Myelin one of
2022-09-16

Acknowledgments Introduction Myelin, one of the fundamental adaptations of vertebrates, is a multilamellar structure deriving from the spiral wrapping around the Adenosine-5'-diphosphate mg of the plasma membrane of myelin forming glia, oligodendrocytes in the central nervous system and Schwa
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The action of niacin in upregulating cAMP is
2022-09-16

The action of niacin in upregulating cAMP is most likely determined by the milieu of adenylyl cyclase isoforms expressed in macrophages that are responsive to GPR109A activation. Several adenylyl cyclase isoforms, namely AC2, AC4 and AC7, are responsive to the stimulatory action of Gβγ G-protein sub
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CF patients can suffer from a multitude of hepatobiliary pro
2022-09-16

CF patients can suffer from a multitude of hepatobiliary problems including gall stones, hepatitis, steatosis and cirrhosis. Hepatobiliary problems are common in pediatric CF patients with reported prevalence rates up to 25% [12,13]. Cystic fibrosis related liver disease (CFLD) was thought to develo
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br Acknowledgments This publication was supported by NORAD N
2022-09-16

Acknowledgments This publication was supported by NORAD (Norwegian Agency for Development Cooperation) under the NORHED-Program, agreement no. ETH-13/0024. MCM works at the MRC Integrative Epidemiology Unit which receives infrastructure funding from the UK Medical Research Council (MRC) (MC_UU_12
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br Acknowledgements This work was supported by
2022-09-16

Acknowledgements This work was supported by Slovak Academy of Sciences grants VEGA 2/0052/10 and 2/0045/10. Both clinical observations and preclinical studies suggest that hypofunction of -methyl--aspartate (NMDA) receptor is implicated in the pathophysiology of schizophrenia. Thus, therapeuti
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Polyunsaturated fatty acids PUFAs represent
2022-09-16

Polyunsaturated fatty acids (PUFAs) represent a class of lipids that contain two or more carbon double (unsaturated) bonds (CC) and classified as n-3, n-6 and n-9 fatty acids. PUFAs including n-3 such as docosahexaenoic Kif15-IN-2 sale (DHA), eicosapentaenoic acid (EPA) and n-6 such as arachidonic
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Heparin br Sodium glucose co transporter
2022-09-16

Sodium-glucose co-transporter-2 inhibitors (SGLT2i) are the latest class of non-insulin glucose-lowering agents that facilitate glycaemic control by inhibiting renal glucose reabsorption, thus promoting glycosuria. Canagliflozin, dapagliflozin, and empagliflozin are the three commonly used agents
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It is generally considered that elevated blood glucose due
2022-09-16

It is generally considered that elevated blood glucose due to insulin resistance is an important factor in islet compensation to high fat feeding [27]. However, we have shown recently that insulin resistance induced in mice by hydrocortisone injection provokes significant islet cpi 1 receptor in the
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