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Various compounds have been designed to inhibit aldose
2023-11-16

Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic Raltegravir moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to be a p
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br Conflict of interest br Acknowledgement This study
2023-11-16

Conflict of interest Acknowledgement This study was supported by a grant from University Grants Commission - Basic Scientific Research (UGC-BSR), New Delhi, India (UGC-BSR No:F-7-115/2007). Introduction The G protein-coupled receptors activated by extracellular adenosine (Ado), called Aden
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where is the breaking force In the following
2023-11-16

where is the breaking force. In the following, the details of the simulation are presented and subsequently, the results are discussed. The initial atomic structure is extracted from the crystal structure of single AF (PDB identification 3G37) which consist 12 monomers. As aforementioned 4 monomer
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br Patients and methods The severity of disease documented
2023-11-16

Patients and methods The severity of disease documented at each outpatient visit was graded according to the modified Osserman classification: grade I, focal disease (e.g. restricted to ocular muscles); grade II, generalised disease that is mild (IIa) or moderate (IIb); grade III, severe generali
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br Methods br Transparency document br Introduction Epinephr
2023-11-16

Methods Transparency document Introduction Epinephrine (EP) is a critical hormone and catecholamine neurotransmitter in nervous system of mammals.1, 2, 3 It has been known to accelerate and regulate heartbeat, blood pressure, bronchodilation, mydriasis, blood sugar and lipolysis, and can he
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br Methods br Results and discussion br Conclusions br Ackno
2023-11-16

Methods Results and discussion Conclusions Acknowledgements The authors thank Dr. Francois Alhenc-Gelas (then INSERM U367, Paris, France), who kindly provided the plasmid for truncated soluble recombinant human ACE – WTΔ, Dr. Elena Arablinskaya (Institute of Phtiziopulmonology, Moscow, R
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In the nineties we knew that
2023-11-15

In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available
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Chlorogenic acid an abundant polyphenol found in coffee and
2023-11-15

Chlorogenic adenosine triphosphate synthesis (7), an abundant polyphenol found in coffee and the human diet, has various biological activities including antioxidant and anticancer effects [54]. Jiang et al. reported that compound 7 had a selective cytotoxic activity on human oral tumor cells (HSG,
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The putative residue apelin proprotein proapelin or apelin i
2023-11-15

The putative 55-residue apelin proprotein (proapelin or apelin-55) is processed from a 77-residue preproprotein through removal of a 22-residue signal peptide (Table 1). Apelin-55 is further processed into bioactive isoforms of 36, 17, or 13 residues, likely through protease-mediated mechanisms. To
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br Competing interests br Acknowledgments This research was
2023-11-15

Competing interests Acknowledgments This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science and ICT (NRF-2014R1A4A1071040). Introduction Mitochondria occupy an important position as mediators of
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br Conclusion We have identified
2023-11-15

Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina
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This chemistry paved way for multi gram synthesis of which
2023-11-15

This chemistry paved way for multi-gram synthesis of which was utilized for extensive piperazine benzamide SAR exploration. Depicted in , the two-step operation towards final targets involved standard amide coupling conditions with EDC or HATU followed by Boc deprotection under acidic conditions. S
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In particular we focused our attention
2023-11-15

In particular, we focused our attention on beta2 adrenergic receptors, since their commercial inhibitors are effective in lowering IOP, the primary indication of glaucoma. The hypotensive action of a commercial sequence of beta2 adrenergic receptor siRNA was tested in rabbits. The results confirmed
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Idoxuridine While A Rs communicate mainly with the D
2023-11-15

While A1Rs communicate mainly with the D1R subtype [36], A2AR and D2R interaction occurs mainly in basal ganglia. D2Rs colocalizes with A2ARs in this Idoxuridine area where they are preferentially localized postsynaptically in the soma and dendrites of GABAergic striatopallidal neurons [69]. This in
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br Introduction Fungi are an inexhaustible source
2023-11-14

Introduction Fungi are an inexhaustible source of natural products mainly due to their wide distribution in the nature, estimated to range from 1.5 to 5.1 million species in the world [1]. Secondary metabolites from fungi represent a substantial fraction of drugs and drug models in pharmaceutical
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