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Introduction Lipoxygenases LOXs are key enzymes that catalyz
2023-09-18
Introduction Lipoxygenases (LOXs) are key enzymes that catalyze the polyunsaturated fatty acids (PUFAs) such as arachidic neuropeptide receptors (AA), linoleic acid (LA) and others unsaturated fatty acids (Brash, 1999). LOXs are expressed in immune, neural, epithelial, tumor cells and other cells (
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Em um estudo com modelos de ratinhos triplamente mutados par
2023-09-18
Em 2011, um estudo com modelos de ratinhos triplamente mutados para heat shock protein inhibitors doença de Alzheimer expôs um grupo a anestesia geral com halotano ou isoflurano cinco horas por semana durante quatro semanas (a três diferentes idades: dois, quatro e seis meses) e um grupo sem exposiç
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There are two ways to transport
2023-09-18
There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty Beclomethasone dipropionate transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD
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HT modulates cortical and hippocampal pyramidal
2023-09-18
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal Genistein as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al., 20
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br Perspectives and challenges Previously the main focus of
2023-09-18
Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular
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Encouraged by this observation a systematic SAR study on
2023-09-18
Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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br Acknowledgements This work was supported by
2023-09-18
Acknowledgements This work was supported by Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), Fundação de Amparo à Pesquisa do Estado do Rio Grande do Sul (FAPERGS) FINEP research grant “Rede Instituto Brasil
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A high throughput small molecule ACK biochemical
2023-09-18
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found Esomeprazole Sodium mg to be both ATP-competitive and reversible. Early structure-activity relationship (SAR
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br AD and COX LOX pharmacology Early studies
2023-09-18
AD and COX/5-LOX pharmacology Early studies on the role of cyclooxygenases in AD were inspired by epidemiological data suggesting that COX inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs) could be beneficial in AD patients (Lucca et al., 1994, McGeer et al., 1990). This line of re
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Because of its role in
2023-09-18
Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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The molecular mechanisms involved in the pathogenesis
2023-09-18
The molecular mechanisms involved in the pathogenesis of cholestatic pruritus remain unknown [45], [46]. Indeed, there has been an enormous effort at understanding the etiology of PBC-related pruritus, including work at the cellular and molecular level, but such efforts have not been translated into
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br Transparency document br Acknowledgments This
2023-09-18
Transparency document Acknowledgments This work has been supported by the National Eye Institute (NIH) Grant 5R01EY023315-02 (MA). This study was also supported in part by National Center for Research Resources Grant S10RR027926 for the lipid analysis and by James and Jean Culver Vision Discov
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Epothilone D synthesis According to the present observations
2023-09-18
According to the present observations, the Ampkα1 isoform promotes AP-1 transcriptional activity and thereby fosters Epothilone D synthesis of AP-1 target genes in cardiomyocytes via activation of Pkcζ. The transcription factor AP-1 plays a decisive role during cardiac remodeling [24], [25], [26],
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It is worth noting that in S cerevisiae
2023-09-18
It is worth noting that in S. cerevisiae, the control of two cell-cycle checkpoints requiring Mcm1 involves two very different mechanisms. At the G1/S transition, Mcm1 transactivation activity is inhibited by Yox1 and Yhp1 repressors, whose expression is periodically regulated through the cell cycle
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In our study we provide evidence for
2023-09-16
In our study we provide evidence for the existence of an endosome-lysosomal pathway for the proteolytic degradation of AR triggered by its interaction with the ESCRT-I component TSG101. The following findings of this study support this notion: (1) We showed that TS101 interacts with endogenous or ec
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