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The difficulty of characterizing nAChRs in
2024-02-26

The difficulty of characterizing nAChRs in the central nervous system is also exemplified by early observations that nicotine caused no detectable effect when applied on a brain slice and it is only with the focal and high time resolution of more recent experiments that the effects of nicotinic neur
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On another hand pyrazoles are widely found as
2024-02-26

On another hand, pyrazoles, are widely found as the core structure in a large variety of compounds of great biological and pharmaceutical value exhibiting anti-HCV [11], antitumor [12], cytotoxic[13], and antioxidant activities [14]. Finally, 1,2,3-triazoles have attracted the interest of medicinal
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Pyrimidine is the important pharmacology core in
2024-02-26

Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the Golgicide A synthesis
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Here we report discovery of highly selective pan
2024-02-26

Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of 6 his tag bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To
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br Materials and methods br Results br Discussion Human
2024-02-26

Materials and methods Results Discussion Human MutL-family complexes (MutLα: MLH1-PMS2, MutLβ:MLH1-PMS1, MutLγ:MLH1-MLH3) exhibit multiple molecular activities including DNA binding, DNA cleavage, ATP binding and hydrolysis [43]. In our recent study, we have uncovered an important function
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However most of these SBVS studies were focused on
2024-02-26

However, most of these SBVS studies were focused on the target(s) for which crystal structures were available or have a similar template in PDB for comparative modeling. Besides, these were limited to SBVS only which relies on the rigid binding pocket, therefore, it may result in high false positive
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Torin 2 br Concluding remarks br Conflict of interest br
2024-02-23

Concluding remarks Conflict of interest Acknowledgment This work was supported by the H.E.B. Endowed Chair in Marine Science (to P.T.) and University of Texas Marine Science Institute endowment-supported scholarships (to A.C). Introduction Disorders of sex development (DSD) are defined
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We have recently begun to demonstrate this concept by
2024-02-23

We have recently begun to demonstrate this concept by reporting a novel class of β-hairpin peptidomimetics, built on a piperidine-pyrrolidine semi-rigid β-turn inducer [12] and bearing two recognition pentapeptide sequences, designed on oligomeric and fibril structures of Aβ1-42 (compound 1, Fig. 1
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Introduction Alzheimer s disease AD is
2024-02-23

Introduction Alzheimer's disease (AD) is a complex neurological disorder characterized by a progressive dementia resulting from synapse failure (Selkoe, 2002, Tanzi, 2005). The amyloid hypothesis maintains that the pivotal event in AD is the production of amyloid-β (Aβ) peptides following the prote
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Sixth significant progress has been made during the last
2024-02-23

Sixth, significant progress has been made during the last few years regarding the molecular mechanisms underlying the activation of AMPK and this should aid to develop more potent and specific compounds. Information from crystallographic structures combined with computer-based drug design hold promi
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JP 1302 dihydrochloride This development notwithstanding the
2024-02-23

This development notwithstanding, the chemotherapeutic treatment for leukemia has stagnated over the last 40 years [35]. Main treatment options necessitate aggressive chemotherapy to target leukemic cells [36], [37], [38], [39]. Several limitations of current treatment options include the use of ant
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AR is an enzyme involved in conversion of glucose
2024-02-23

AR is an enzyme involved in conversion of glucose into sorbitol using NADPH as a cofactor [46]. This AR polyol pathway generates sorbitol accumulation and NADPH depletion. NADPH participates in detoxification via glutathione (GSH) reductase pathway [47]. Therefore, reduction of NADPH attenuates remo
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ezh2 pathway br Conclusion br Conflict of interest br
2024-02-23

Conclusion Conflict of interest Acknowledgements Introduction Human salivary aldehyde dehydrogenase (hsALDH) (E.C. 1.2.1.5) is the first line of defence against toxic aldehydes in the oral cavity. HsALDH is primarily a dimeric, class 3 ALDH (ALDH3A1) specific for aromatic and long/medium
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Introduction br This paper is a commentary on the history
2024-02-23

Introduction This paper is a commentary on the history of language among the Aché. What was language for the Aché prior to contact with Paraguayan society? How has the Aché language come to be endangered? Why is language such an important issue today? In exploring these questions I come to a slig
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Specifically equity injections in a multinational affiliate
2024-02-23

Specifically, equity injections in a multinational affiliate X located in an ACE country can be passed on as lending to another group member Y located in a different country with a high corporate income tax rate. For the group member Y, the interest on the loans is tax deductible, and at the same ti
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