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Since artemisinin shows low solubility and
2023-02-06

Since artemisinin shows low solubility and poor oral bioavailability [8], [9], derivatizations of artemisinin were carried out and yielded different semisynthetic antimalarial drugs such as artemether and sodium artesunate. Artemether (decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano [4.3-
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Introduction Glaucoma consists of a group of
2023-02-06

Introduction Glaucoma consists of a group of eye diseases showing a broad spectrum of clinical presentation and unknown aetiologies, that lead to a permanent loss of visual function due to the death of retinal ganglion XMU-MP-1 and damage of the optical nerve. It is well accepted that a critical ri
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Our in vitro data show that CyaA does not
2023-02-06

Our in vitro data show that CyaA does not play a critical role in the bacterial adherence to mammalian cells. This observation is in contrast to previous studies that reported a role for CyaA in FHA-mediated adherence of B. pertussis bacteria to the respiratory epithelial MLN4924 [37,38]. This disc
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br Effective therapeutic window of AR actions on ROP Retinal
2023-02-06

Effective therapeutic window of AR actions on ROP Retinal vasculature undergoes critical developmental changes postnatally: from P7 onward the superficial encorafenib synthesis start sprouting vertically in retina to form first the deep then the intermediated vascular plexus in the retina of C57
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The introduction of a pyrazole moiety into
2023-02-01

The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,
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The resolution cocrystal structure of ACL in
2023-02-01

The 2.10Å resolution cocrystal structure of ACL in complex with citrate indicates that the carboxyl (COH) groups of citrate forms a network of H-bonds with hydrophilic residues surrounding the ACL citrate binding domain (CBD) (A). The - carboxyl group forms a salt bridge with the guanidine moiety of
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chenodeoxycholic acid br Ataxia telangiectasia and Rad
2023-02-01

Ataxia–telangiectasia and Rad3 related as a therapeutic target Several concerns revolving around functional inhibition of ATR have hindered the exploitation of ATR as therapeutic target in cancer therapy and delayed the development of specific ATR kinase inhibitors. It was anticipated that pharma
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The protective role of HMW
2023-02-01

The protective role of HMW-HA in inflammatory diseases and pulmonary damage led us to investigate whether PM2.5-induced ALI could be attenuated by HMW-HA and the underlying mechanisms. In this study, we used a rat model to evaluate the effect of HMW-HA on pulmonary histology, lung inflammation, oxid
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Bioavailability has been defined as the amount
2023-02-01

Bioavailability has been defined as the amount of a drug given by any route, other than intravenously, that reaches general circulation and is available at the site of action [86]. The low bioavailability observed with the initial intravaginal devices (16%) was attributed to the melting point of the
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It was deduced empirically that the helix direction of the
2023-02-01

It was deduced empirically that the helix direction of the COOC torsion might relate to the sign of the peroxide Cotton effect. Huang reported ab initio calculation of the peroxide bond using MRDCI method and DZP basis set, but only the fragment CH3OOCH3 instead of full molecule was studied [19]. Si
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ganciclovir br Materials and methods br Results br Discussio
2023-02-01

Materials and methods Results Discussion We demonstrate reduced angiogenic activity in NDRG1 overexpressing malignant glioma leading to reduced glioma growth. This antiangiogenic phenotype is paralleled by a significant upregulation of the antiangiogenic gene TNFSF15. TNFSF15 upregulation i
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Earlier studies with SERMs identified that
2023-02-01

Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes
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Although AMPK is a negative regulator
2023-02-01

Although AMPK is a negative regulator of bioenergetic reprogramming in cancer cells, little is known about the role of AMPK in immunometabolism in sepsis. Our current study indicates that AMPKα dysfunction enhances PKM2-dependent aerobic glycolysis, which results in HMGB1 release in macrophages and
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In this report we introduce a new method for identifying
2023-02-01

In this report, we introduce a new method for identifying aminopeptidases. Because single substrates can be insufficient for enzyme identification, we used an entire library of substrates to obtain more information about enzyme activity and to directly detect aminopeptidases. Moreover, substrates ca
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br Introduction Alcohol i e
2023-02-01

Introduction Alcohol, i.e., ethanol, is absorbed into the blood from the stomach to the small intestine, then distributed throughout the body. The metabolism of alcohol converting to acetic perhexiline basically involves two enzymes; alcohol dehydrogenase converting ethanol to acetaldehyde and a
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