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Aromatization of the pyrrole ring after anion capturing
2023-02-01
Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re
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Applications for protein switches are numerous In
2023-02-01
Applications for protein switches are numerous. In diagnostics, protein switches can detect analytes as components of inexpensive homogeneous assays that do not require specialized equipment or time-consuming incubation and washing steps characteristic of immunoassays [8]. Protein switches have also
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cdc42 Our research group has been
2023-02-01
Our research group has been involved by many years in the synthesis of new 2,3-benzodiazepin-4-ones (e.g. 1, Fig. 1) and in the characterization of their mechanism of action.15, 16, 17 Within the development of these compounds, we demonstrated that an improvement of AMPAR antagonism by 2,3-benzodiaz
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In order to postulate its
2023-02-01
In order to postulate its binding mode in APN, autotaxin inhibitor 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occupi
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Introduction Aldose reductase ALR is the first
2023-02-01
Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr
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br Material and methods br Results br
2023-02-01
Material and methods Results Discussion GRK2 activity has increasingly been shown to contribute to the progression of numerous diseases and organ dysfunction [5], [6]. For instance, a large body of work over the last two decades has identified GRK2 as a major regulator of cardiac dysfunctio
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Qualitative inspection of the single channel traces presente
2023-02-01
Qualitative inspection of the single-channel traces presented in both Figures 3 and 4 shows that within bursts of activity, βAnc-containing AChRs display a marked reduction in open probability. To quantify these differences in single-channel behavior, we performed dwell-time analysis under high-reso
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br Funding This study was supported
2023-01-31
Funding This study was supported by Grant UM1-CA186690 (NCI-CTEP) and R01CA204173 (CJB). This project used the UPCI Cancer Pharmacokinetics and Pharmacodynamics Facility (CPPF) and was supported in part by award P30-CA47904 and R50CA211241. Introduction Despite the efficacy of platinum based
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There are increasing repeated reports of amphotericin B
2023-01-31
There are increasing repeated reports of amphotericin B-resistance in pathogenic fungi including Candida spp. [35], [36]. Nolte et al. characterized some fluconazole and amphotericin B-resistant Candida albicans isolates from leukemia patients [37]. Fan-Havard et al. (1991) have shown multi-antifung
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The reasons why antibiotic treatment
2023-01-31
The reasons why antibiotic treatment may be detrimental are diverse. First, it may result in disruption of multifaceted microbe–microbe, as well as microbe–host, interactions that are key for the maintenance of homeostasis within this ecosystem. This can lead to the expansion of pathogenic microorga
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Initially DPP DPP and prolyl tripeptidyl peptidase A PtpA
2023-01-31
Initially, DPP4, DPP7, and prolyl tripeptidyl peptidase A (PtpA) were the only exopeptidases identified in P. gingivalis. These share substrates according to their altered specificities, as DPP4 is highly specific for Pro at the penultimate position from the N-terminus (P1 position), though it accep
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Imatinib was first approved for the treatment of Philadelphi
2023-01-31
Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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Various compounds have been designed to inhibit
2023-01-31
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 azilsartan medoxomil moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported
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br Experimental section br Introduction Microglia
2023-01-31
Experimental section Introduction Microglia were discovered as a novel cell population in NG,NG-dimethyl-L-Arginine hydrochloride in 1933 by a Spanish physician and histologist Pío del Río-Hortega [1]. In the eye, scientists used Hortega's staining technique to label the microglia in the retin
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Pioneering studies on the immunomodulatory role of adenosine
2023-01-31
Pioneering studies on the immunomodulatory role of adenosine date back to the early ‘70 s of last century (Fig. 1), when the critical role of this nucleoside in shaping the development and the activity of several immune cell populations was first established [[18], [19], [20], [21], [22]]. This then
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