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Tetrazole is one of the most commonly used bioisosteres
2021-10-12

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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br Materials and methods br Chemical synthesis br
2021-10-11

Materials and methods Chemical synthesis Declaration of interest Acknowledgements This research was supported by a grant from the National Institute for General Medicine to K.W.M. (GM 58448) and by the Department of Anesthesia, Critical Care & Pain Medicine at Massachusetts General Hospi
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Dithiodipyridine also known as aldrithiol is
2021-10-11

2,2′-Dithiodipyridine , also known as aldrithiol, is a known zinc ejector, targeting for instance the zinc finger in nucleocapsid protein of human immunodeficiency Penciclovir Sodium mg type 1. inhibited G9a activity with IC = 0.65 µM and GLP with IC = 2.6 µM. We also tested disulfide cysteamine dih
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With the aim to identify potential novel
2021-10-11

With the aim to identify potential novel targets in CVD, we applied proteome analyses on vascular tissue of these frequently used mouse models of atherosclerotic disease in the presence and/or absence of diabetes. Potential targets for intervention identified with this approach were validated in hum
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However HDACi can also increase
2021-10-11

However, HDACi can also increase the acetylation of other transcription factors that regulate p65 transcriptional activity. The HDACi-induced activation of p65 can be negated by acetylated STAT1, which can specifically bind to p65 and inhibit its transcriptional activity 81, 82, 83. Interestingly, a
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Preliminary analyses of these identified
2021-10-11

Preliminary analyses of these identified two bands for MALDI-TOF/TOF have shown the presence of approximately 20 proteins, most of which have not yet been characterized. However, several proteins, such as cytochrome c oxidase [53], peroxiredoin II E [54] and alcohol dehydrogenase [55], have been ide
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The saturated carbocyclic derivatives pyrazoles M and M and
2021-10-11

The saturated carbocyclic derivatives, pyrazoles (2.5μM and 5.2μM) and (9.0μM and 2.5μM), provided little improvement in potency when compared to the linear alkyl derivatives, whereas the C5-phenyl derivative (0.31μM and 0.43μM) showed promise as a scaffold for further structural modifications. In
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As a part of our continuing
2021-10-11

As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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Introduction The West syndrome or epilepsy
2021-10-11

Introduction The West syndrome or epilepsy with epileptic spasms (ES) is an epileptic encephalopathy in early infancy with probable seizure-related developmental regression. According to the United Kingdom Infantile Spams Study (UKISS), common causes of infantile spasms include hypoxic-ischemic enc
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As we showed earlier a
2021-10-11

As we showed earlier [19], a 20- to 30-min incubation with 2mM t-BHP resulted in erythrocyte swelling, which was less in a Ca2+-containing medium. Given that this effect was abolished in the presence of the Gardos channel inhibitor CLT, as well as in media high in K+, we suggested the contribution f
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To effectively evaluate prospective mechanisms
2021-10-11

To effectively evaluate prospective mechanisms by which chronic HIV infection induces pulmonary fibrotic changes in humans, we confirmed that predisposition to fibrotic change in older individuals could be mimicked in a mouse model. Hydroxyproline is a nonessential amino LY335979 required for the s
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br Conclusion The wild study reports
2021-10-11

Conclusion The wild study reports seasonal variations in reproductive physiology, behavior and Panobinostat plasticity at different age stages in wild-caught Mongolian gerbils. The gerbils in breeding seasons have more mature sexual development, higher exploratory behavior, higher novelty prefere
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CaCl was from the Radiochemical Centre Amersham UK NaVO was
2021-10-11

45CaCl2 was from the Radiochemical Centre (Amersham, UK), NaVO3 was from Reachim (Moscow, Russia). Tetrodotoxin was purchased from Calbiochem, DTNB from Merck, Darmstadt, Germany. Nifedipine was synthesized in the Institute of Drug Research, Modra, Slovakia and was kindly provided by Dr. Zdeno Mahrl
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Naproxen Sodium br Materials and methods br Results br Discu
2021-10-09

Materials and methods Results Discussion G-quadruplex structures are extensively studied for its role in central dogma of molecular biology viz. replication problems leading to chromosomal translocations [20], [21], transcriptional inhibition [32] and alternative splicing and translational
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AD is a major neurological disorder
2021-10-09

AD is a major neurological disorder, usually effecting the elderly population, which is difficult to diagnose until symptoms begin to accumulate. As of 2013, approximately five million Americans were living with AD. The number with this disease is projected to be 16 million by 2050 (Hebert et al.,
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