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As expected the nortestosterone derived progestins
2020-09-24
As expected, the 19-nortestosterone-derived progestins tested were moderate agonists of hAR (C), with EC50s ranging from 2 to 10nM, however all were less potent than the endogenous ligand DHT by at least a factor of 6, with relative potencies ranging from 0.0301 to 0.164. This is in agreement with p
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If the effects described here
2020-09-23
If the effects described here are present in catalysis, their empirical confirmation poses many challenges. Cat state correlations are fragile outside an environment especially suited for their preservation. As present day observational techniques whether in vivo or in vitro were not designed bearin
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Just as Dorin et al and Nguyen et al write
2020-09-23
Just as Dorin et al. [2] and Nguyen et al. [3] write in regard to their models, our static model can be used to estimate the affinities of lysophospholipid receptor to albumin and CBG. Dorin et al. [2] estimates the K, but not K, since they find that their model is not particular sensitive towards
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Overall the evidence and the
2020-09-23
Overall, the evidence and the results from in vivo studies clearly indicate that cyclosporine biotransformation can be induced by dasatinib co-administration through induction of CYP3A expression. However, further studies are needed to explore the role of P-gp modulation in DDIs. Conclusion In v
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br Materials and methods br Results
2020-09-23
Materials and methods Results Discussion Oxidative stress is a disturbance in the balance of pro- and antioxidant species, resulting in oxidative damage to membrane proteins, lipids, and DNA. Oxidative stress is a predisposing factor for the progression of metabolic diseases and liver injur
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The question arises as to how
2020-09-23
The question arises as to how the massive conformational changes determining whether APC/CCDC20–MCC is inhibited or able to catalyze MCC ubiquitylation are naturally controlled? This transition likely involves APC/C regions near the subunit APC15, because reducing cellular APC15 levels stabilizes MC
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Pyruvate dehydrogenase multienzyme complex PDHc
2020-09-23
Pyruvate dehydrogenase multienzyme complex (PDHc) catalyzes the oxidative decarboxylation of pyruvate, and subsequently acetylates coenzyme A (CoA) to acetyl-CoA during the tricarboxylic Tubastatin A HCl metabolic pathway using thiamine diphosphate (ThDP) and Mg2+ as cofactors. PDHc poses a key rol
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Protein deubiquitination is becoming increasingly instrument
2020-09-23
Protein deubiquitination is becoming increasingly instrumental in understanding the complexities of the Ub system. Adding to this complexity is the discovery of bacterial effectors with DUB activity that have structurally adapted themselves to interfere with the eukaryotic Ub system (Pruneda et al.,
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br Rationale and Conventional Use of
2020-09-22
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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Diacylglycerol kinase was one of
2020-09-22
Diacylglycerol kinase was one of the hits identified from the RNAi screen. Diacylglycerol kinases are conserved across a psoralen of species with more complex, multicellular organisms possessing several DGKs with differing protein domains, expression patterns and functions [61], [62], [63]. Some of
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A novel series of DHODH inhibitors was developed by
2020-09-22
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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Collagen X is a homotrimeric molecule
2020-09-22
Collagen X is a homotrimeric molecule of three α1(X) chains (Mr 59 kDa) comprising a 45 kDa triple-helical domain flanked by an N-terminal (NC2) and a larger C-terminal (NC1) non-collagenous domains (Shen, 2005). In the hypertrophic ECM, collagen X most likely forms an extended hexagonal network, as
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br Introduction Noncanonical nucleoside triphosphates NTPs s
2020-09-22
Introduction Noncanonical nucleoside triphosphates (NTPs; such as deoxyinosine triphosphate (dITP), deoxyxanthosine triphosphate (dXTP), 8-oxo-deoxyguanosine triphosphate, and 2-oxo-deoxyadenosine triphosphate are produced from oxidation, deamination, or other modifications of canonical nucleotid
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Introduction Quassinoids are natural products
2020-09-22
Introduction Quassinoids are natural products formed through the oxidative degradation of triterpene derivatives with anti-inflammatory, antimicrobial, antineoplastic, and antiplasmodial effects (Chakraborty and Pal, 2013; Houël et al., 2013). They are characteristic ingredients of the family Simar
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The mutation in Caucasian people of European heritage
2020-09-22
The Δ32 mutation in Caucasian people of European heritage is quite common but extremely rare in Asian and African countries (Huang et al., 1996). We recently reported the presence of this mutation from India (Husain et al., 1998a) and established the complete inheritance pattern (Husain et al., 1998
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