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As mentioned above variation of the A ring
2024-05-13
As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to Clindamycin Phosphate synthesis (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide ()
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In this study significant reduction
2024-05-13
In this study, significant reduction in the HCO3− content in sham-operated and testosterone-treated rats following bafilomycin A1 administration suggested that V-ATPase could be involved in mediating the decrease in vas deferens fluid HCO3− content, most probably due to the increase in H+ secretion
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Introduction Cytochrome P CYP aromatase catalyzes the
2024-05-11
Introduction Cytochrome P450 19 (CYP19; aromatase) catalyzes the conversion of androgens to estrogens in a three-reaction sequence, where each step depends on NADPH and O2 [[1], [2], [3]]. The first two steps are accepted to be hydroxylations of the steroid C19 methyl group, whereas the final step
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NO is an important mediator
2024-05-11
NO is an important mediator for maintaining bone integrity since it plays a role in the bone remodeling process. It was shown that mechanical strain and shear stress induce NO synthesis in osteoblasts and osteocytes (van't Hof & Stuart, 2001). It was reported that mechanical loading influences its a
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Echinocandin resistance is systematically associated with po
2024-05-11
Echinocandin resistance is systematically associated with point mutations in either FSK1 or FSK2 genes [7], [104]. These mutations are located in two different not spot regions of these genes named HS1 and HS2. Hot spot mutations have been reported in C. albicans, C. glabrata, C. tropicalis, C. krus
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Sorafenib was the first small RTK inhibitor drug to
2024-05-11
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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In addition to differential expression
2024-05-11
In addition to differential expression of AR protein primarily in surgical specimens, genetic alterations involving the AR gene have been documented in human abnormal lipid metabolism cancer. Loss of heterozygosity at the AR locus was identified in all 3 informative cases of muscle-invasive bladder
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br Pathophysiology of Alzheimer disease
2024-05-11
Pathophysiology of Alzheimer disease Alzheimer disease is characterized by severe neurodegeneration, neuroinflammation, and progressive loss of cognitive abilities. The diagnostic criteria for dementia released by the National Institute on Aging-Alzheimer's Association define dementia as the deve
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br Materials and method br Result and
2024-05-11
Materials and method Result and discussion Conclusion Acknowledgments This work is partly supported by the University Research Committee (URC) of the Senate of The Federal University of Technology, Akure. The authors thanked IFS for the funds (F/4449 1F and F/4449-2F) used to purchase th
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According to their structures and substrate specificity MMPs
2024-05-11
According to their structures and substrate specificity, MMPs are divided into five major groups: collagenases (e.g., MMP1), gelatinases (e.g., MMP2, MMP9), stromelysins (e.g., MMP3, MMP10), matrilysins (e.g., MMP7), and membrane-type MMPs [7]. Among them, MMP1 is a major collagenase that degrades t
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In an AP scenario several inflammatory mediators are produce
2024-05-10
In an AP scenario, several inflammatory mediators are produced locally to orchestrate an immune response. Eicosanoids are among those molecules and represent a class of lipid mediators synthesized from arachidonic pak1 through the action of cyclooxygenases or lipoxygenases to generate prostaglandins
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Consistent with the observation that mutations in the redox
2024-05-10
Consistent with the observation that mutations in the redox-partner binding site of P450c17 that reverse charge from basic to acidic (R347H, R358Q) cause 17,20-lyase deficiency (Geller et al, 1997, Geller et al, 1999), at least one POR mutation that changes a residue in the FMN domain from neutral t
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Starting with commercially available or nitropyrazole carbox
2024-05-10
Starting with commercially available 4- or 5-nitropyrazole-3-carboxylic acid, anilides containing nitro, amino or methylsulfonamido were synthesized. Here, manipulation of the substituents on the pyrazole ring was conducted after the anilide formation (). The pkd kinase of the nitro group was perfor
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br Acknowledgements M M M is the William Dow Lovett
2024-05-10
Acknowledgements M.M.M. is the William Dow Lovett Professor of Neurology and is supported by grants from the Michael J. Fox Foundation for Parkinson's Research, the American Parkinson Disease Association, the New Jersey Health Foundation/Nicholson Foundation, and by the National Institutes of Hea
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br Apelin Discovered in apelin was initially
2024-05-10
Apelin Discovered in 1998, apelin was initially identified as the sole endogenous ligand for the APJ receptor (Tatemoto et al., 1998). Apelin-77 (pre-pro-apelin) is the precursor for various pharmacologically active apelin isoforms (e.g. apelin-12, -13, -17 and 36), and it shares 75–95% sequence
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