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br Rationale and Conventional Use of Alkylating
2021-08-05
Rationale and Conventional Use of Alkylating Agents and Platinum Derivatives in Clinical Practice After the attack on Bari Harbor in 1943 revealed the effects of mustard gas on bone marrow depletion and the first therapeutic outcomes in lymphoma, alkylating agents gradually became a gold standard
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A novel series of DHODH
2021-08-05
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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br Conflict of interest br Acknowledgments We
2021-08-04
Conflict of interest Acknowledgments We thank Jianru Zuo (Institute of Genetics and Developmental Biology, Chinese Academy of Sciences, Beijing, China) for providing fbr11-1 seeds. We are grateful to Carol MacKintosh and the DSTT at the University of Dundee (UK) for anti-RD21 antibodies. This
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Because aspirin and ibuprofen are
2021-08-04
Because aspirin and ibuprofen are NSAIDs, both cause a variety of adverse effects, including stomach ulcers, stomach bleeding, coagulation disorders, Sotalol and cerebral microbleeds [13]. Moreover, both cause liver damage [10]. Laster [14] reported a patient with pericarditis treated with aspirin
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We also identified a role for the
2021-08-04
We also identified a role for the transcription factor p53 in the regulation of the Crm1 promoter. p53 can activate or repress the transcription of target genes. While activation generally occurs through binding of p53 to its consensus binding site in the promoter region of target genes, for example
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Nodinitib-1 br Results br Discussion Drug resistance poses
2021-08-04
Results Discussion Drug resistance poses the greatest hurdle of achieving high efficacy with AADs in cancer patients. AAD-treated cancer patients often encounter intrinsic and evasive drug resistance that diminishes the therapeutic efficacy to only minor survival benefits in most cancer types.
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Phenylbenzofurans are a very important molecule skeleton
2021-08-04
Phenylbenzofurans are a very important molecule skeleton due to their synthetic versatility and their proved pharmacological properties [2]. They are synthetic compounds in which an additional phenyl ring is present in any position of the benzofuran nucleus. This could be easily obtained possible by
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Tibolone is also efficacious on bone in
2021-08-04
Tibolone is also efficacious on bone in elderly women and induces a clear reduction in bone turnover markers [50], [51]. Rymer et al. showed that, after 10 years of treatment with tibolone, the difference in bone mineral density compared with a placebo group was more than 12% for both lumbar spine a
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In SLO permeabilized human sperm the AR elicited by
2021-08-04
In SLO-permeabilized human sperm, the AR elicited by calcium, persistently active Arf6 [41] and Rab3A, 8-pCPT-2′-O-Me-cAMP [8], diacylglycerol and a non-hydrolyzable analog [35], is sensitive to the PLC blocker U73122. Furthermore, 8-pCPT-2′-O-Me-cAMP elicits a calcium signal in non-permeabilized sp
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Prostaglandin E receptor subtype EP is a transmembrane G cou
2021-08-04
Prostaglandin E receptor subtype 4 (EP4) is a transmembrane G-coupled protein receptor activated by prostaglandin E2 (PGE2). EP4 activation exerts anti-inflammatory effects in adipose tissue by dampening the levels of inflammatory chemokines [12]. In the mouse, EP4 deficiency aggravates fragmentatio
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The interface between the E ligase
2021-08-04
The interface between the E3 ligase and the E2 enzyme can vary, and ZNF451 and SP-RING ligases stabilize this interaction via noncovalent binding to a scaffold SUMO (SUMOB) on the backside of the E2 (Cappadocia et al., 2015; Eisenhardt et al., 2015; Streich & Lima, 2016). By contrast, RanBP2 does no
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read the article Acanthopanax senticosus Rupr Maxim Harms a
2021-08-03
Acanthopanax senticosus (Rupr. & Maxim.) Harms, a nontoxic herb belongs to the family of Araliaceae, which found in Northeast Asia. A. senticosus traditionally used as a tonic to treat rheumatism, diabetes, and hepatitis [7]. Previous phytochemical and biological investigations found its roots and s
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However there are still some issues that remain poorly
2021-08-03
However, there are still some issues that remain poorly understood. For instance, how TGF-β modulates DDR2 expression and whether Smads participate in the regulation. How does DDR2 regulate the expression of PTHrP via Runx2? Is there any other kinase downstream of DDR2 participating in PTHrP regulat
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van Linden et al developed a
2021-08-03
van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur
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MTT results show that both pancreatic cell lines were quite
2021-08-03
MTT results show that, both pancreatic cell lines were quite sensitive to camptothecin (CPT), a well known topoisomerase I poison. Interestingly, CPT does not show any selectivity over cancer cell lines probably due to the duplication times for cancerous (MIA PaCa-2) and immortalized healthy (HPDEC)
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