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The current antifungal pipeline contains several categories
2024-01-18
The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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br Introduction Breast cancer is the second most
2024-01-18
Introduction Breast cancer is the second most lethal cancer among women, accounting for approximately 40,000 deaths in the United States in 2015 [1]. The prognosis of breast cancer has improved significantly with the identification of immunohistochemical subtypes that predict response to therapy
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br Results and discussion In order to investigate the assemb
2024-01-18
Results and discussion In order to investigate the assembly dynamics and aggregate structures of Aβ16-22, twelve molecular systems with the number of peptides varying from 1 to 12 were studied. In all simulations, the same peptide concentration (~15 mM) was maintained by adjusting the dimensions
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Our present result that week
2024-01-18
Our present result that ≤2-week-old 150ΔPKA mice express normal LTP that does not depend on CP-AMPARs also supports the collective findings of previous work showing that LTP mechanisms are remarkably adaptable in juvenile animals compared with adults. In particular, GluA1 knockout, S845A/S831A, and
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Pregnane X receptor PXR is a nuclear receptor that
2024-01-18
Pregnane X receptor (PXR) is a nuclear receptor that plays an important role in regulation of metabolism and disposition of structurally diverse xenobiotics as well as endogenous steroids and bile acids (Bertilsson et al., 1998, Kliewer et al., 1998, Lehmann et al., 1998). PXR regulates the metaboli
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br ABCA and cancer drug
2024-01-18
ABCA2 and cancer drug response Overall, the expression of ABC transporters has been linked with multidrug resistance phenotypes through the efflux of drugs via ATP-dependent transport. For example, 13 distinct transporters (ABCA2, ABCB1, ABCB4, ABCB11, ABCC1–6 ABCC10, ABCC11 and ABCG2) have been
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The most widely recognized effects of adenosine are operated
2024-01-18
The most widely recognized effects of adenosine are operated through inhibiting A1R, one of the most abundant G protein-coupled receptors in RQ-00203078 tissue [53]. A1R are located presynaptically, postsynaptically and nonsynaptically [54]. Effect of adenosine in neuronal circuits of adult mammals
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Adenosine A A agonists have been shown to
2024-01-18
Adenosine A2A agonists have been shown to significantly reduce albuminuria in diabetic mice as well as plasma creatinine [24]. Proteinuria was greater in diabetic A2A knock-out (KO) mice than diabetic wild type (WT) mice [24]. Consistent with these findings, our laboratory initially found that prote
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br Acknowledgements This work was supported by Conselho Naci
2024-01-18
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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br GMF Remodels Actin Networks at the Leading Edge
2024-01-18
GMF Remodels Actin Networks at the Leading Edge How are the conserved activities of GMF used in vivo to regulate branched Lenalidomide networks (e.g., at sites of endocytosis and at the leading edge) (Figure 2A,B)? In animal cells, the regulatory effects of GMF on actin networks appear to govern
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In pioneering work from Ikeda and colleagues showed that GMF
2024-01-18
In 2006, pioneering work from Ikeda and colleagues showed that GMF localizes to and regulates the Ginsenoside Rb1 receptor cytoskeleton (see Glossary), and noted its sequence similarity to ADF/cofilin[11]. In 2009, the structure of GMF [6] was solved, revealing it to be a bona fide member of the ac
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Toxicity is the main reason
2024-01-18
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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Composite soil samples were transported to the laboratory an
2024-01-18
Composite soil samples were transported to the laboratory and then dried, crushed and passed through a 2mm sieve was. Sample digestion and release of elements method Sposito was performed [15]. Accordingly, taking into account soil moisture to 2g soil samples 12.5ml of nitric acid was added 4M. Samp
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Pregnenolone Carbonitrile Nowadays more than kinases have be
2024-01-17
Nowadays, more than 500 kinases have been identified of human genome [2]. Imatinib (Gleevec) was the first tyrosine kinase inhibitor approved by the US Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia [3], and kinases have become an attractive target for the developme
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Here we report discovery of highly selective pan Aurora
2024-01-17
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Fucoidan bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To i
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