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Introduction Cyclin dependent kinases CDKs are a family of p
2020-04-15

Introduction Cyclin dependent kinases (CDKs) are a family of proline-directed serine/threonine kinases with roles in regulation of crucial cellular processes such as salubrinal receptor and transcription [1]. One of the unifying features of this family is its dependence on association with cyclins
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MRS 2578 australia br Introduction The ubiquitination statu
2020-04-15

Introduction The ubiquitination status of a target protein is achieved via a delicate balance between two opposing forces: ubiquitin E3 ligases and DUBs. It has been postulated that the majority of proteins in a cell are regulated and modified by ubiquitin at some point (Hershko and Ciechanover,
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Ligand binding RTK activation induces the endocytic internal
2020-04-15

Ligand binding (RTK activation) induces the endocytic internalization of RTKs, and this has been demonstrated for CSF-1R [15], [16], [17]. Endocytosed RTKs are targeted to the lysosome, which we and others have established to be dependent on ubiquitination via CBL-family and recognition by ESCRT com
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Two additional hydrogen bonds are
2020-04-15

Two additional hydrogen-bonds are formed by the -substituted methoxy-group with Ser and Asp. Ser exerts the role of a gate keeper in CK1: Entry of the ATP in the binding-site causes a conformational change into the closed form by Ser, which locks the binding-site and prevents ATP-diffusion out of th
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Compound was prepared from chloroindole by acylation to give
2020-04-15

Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole Cathepsin K Activity Fluorometric Assay Kit sale
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MPI-0479605 sale Our results demonstrate that pt PGE
2020-04-15

Our results demonstrate that 17-pt-PGE2 - in addition to its described effects on EP1 and EP3 receptors - also acts as an EP4 agonist and thereby enhances vascular barrier function. Materials and methods Results Discussion In this study we demonstrate that the purported EP1/EP3 receptor ag
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In addition to providing substantial
2020-04-15

In addition to providing substantial insight into substrate recognition, structural studies have revealed important details about mechanisms of glycosylation and HCF-1 cleavage [28,30,33]. Activation of the nucleotide-sugar is accomplished through interactions of the β-phosphate with the N-terminus
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br ET Antagonist for the Future Macitentan and Atresentan Ma
2020-04-15

ET Antagonist for the Future: Macitentan and Atresentan Macitentan is an insurmountable antagonist, resulting from structure-activity studies to improve the efficacy and tolerability of bosentan, and gained approval in the United States in 2013 for the treatment of PAH. Actelion describes the com
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br Acknowledgments br Introduction Hypertensive retinopathy
2020-04-15

Acknowledgments Introduction Hypertensive retinopathy is a disease of the retinal microvasculature associated with elevated blood pressure (Fraser-Bell et al., 2017). Narrowing of retinal arterioles occurs in the early stage of the disease, and with persistent hypertension further vascular pat
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In mammals NETs contain DNA and antimicrobial proteins compo
2020-04-15

In mammals, NETs contain DNA and antimicrobial proteins composed mainly of nuclear histones, granule-derived neutrophil elastase, myeloperoxidase, lactoferrin, pentraxin, and gelatinase among others [11], [46], [47], [48]. In fish, NETs-like structures have been observed, and DNA staining and immuno
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How does an increase in E
2020-04-14

How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini
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We initially identified four putative Egr
2020-04-14

We initially identified four putative Egr1 AZ191 synthesis (−39/−36, −105/−102, −107/−104, and −227/−224) on the DBH proximal promoter. The deletion and mutagenesis experiments indicate that the motif at −227/−224 is required for Egr1-elicited reduction in DBH promoter activity. It remains to be det
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EphB promotes tumor growth by stimulating angiogenesis throu
2020-04-14

EphB4 promotes tumor growth by stimulating angiogenesis through EphrinB2 [18]. However, the distinct and specifically involvement of L-Phenylephrine sale and veins in the tumor angiogenesis of all tumor grades is unclear. Our results indicate that the relation between EphrinB2 and EphB4 stained blo
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Compounds and possessed relatively low clogP values and tend
2020-04-14

Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.
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br Materials and Methods br Acknowledgements br
2020-04-14

Materials and Methods Acknowledgements Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the int
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