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br Declaration of interest br Funding br Introduction
2023-09-28
Declaration of interest Funding Introduction The endocrine disruptor bisphenol A (BPA) is a high-production chemical used in several consumer products, including polycarbonate bottles, epoxy resins, dental sealants, and thermal paper receipts (Geens et al., 2012). Importantly, BPA monomers
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br The pathogenesis of AD and
2023-09-28
The pathogenesis of AD and the targets of apelin Alzheimer's drugs Conclusions Introduction APJ, first identified from a human genomic library in 1993, belongs to a member of seven trans-membrane G protein-coupled receptor family. Its amino (S)-Methylisothiourea sulfate mg sequence has
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Since ARBs strongly reduce inflammation it was hypothesized
2023-09-28
Since ARBs strongly reduce inflammation, it was hypothesized that the protective effects on cognition were the result of reduction of inflammation and amelioration of neurogenic decrease. However, ARB treatment did not normalize increased inflammation and neurogenic loss. For this reason, the protec
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The first and the best characterized mechanism of receptor d
2023-09-28
The first and the best-characterized mechanism of receptor-dependent internalization of Aβ is mediated via the α7-nicotinic Nemonapride receptor [82]. Lipoprotein receptor protein represents the second best-studied route that facilitates the uptake of Aβ by neurons, involving additional molecules s
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In the MT SGL two regularization parameters need
2023-09-28
In the MT-SGL, two regularization parameters need to be specified: λ1 and λ2. Using recent results on norm regularization (Banerjee et al., 2014), it is possible to express both parameters via a single parameter as follows: and (Meier et al., 2008, Banerjee et al., 2014), where and are computed
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We have previously shown that
2023-09-28
We have previously shown that the human gonadotropins hLH and hCG trigger a partly irreversible stimulation of intracellular cyclic AMP accumulation in mouse Leydig Tumor BET bromodomain inhibitor (MLTC) in contrast to all other tested mammalian LHs and CG (Klett et al., 2016). In order to get a be
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In the late s Solvay Pharmaceuticals discontinued the Phase
2023-09-28
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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As a continuation of our
2023-09-28
As a continuation of our search for a selective AChE radioligand bearing a meta-F substituted N-benzyl moiety, we designed and synthesized a novel meta-F-CP-118,954 analog along with a meta-18F-labeled form via diaryliodonium salt-based precursor (Fig. 1). For comparative purposes, we incorporate th
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Pyrimidine is the important pharmacology
2023-09-27
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 BAY 61-3606 dihydrochlo
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The take home message here is
2023-09-27
The take-home message here is that, although Aurora A phosphorylated on T288 is the activated isoform of Aurora A, measuring the level of phosphorylation of T288 does not reflect Aurora A kinase activity (Figure 5). What would be the most appropriate readout for an in vivo Aurora A kinase activity
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m-Chlorophenylbiguanide hydrochloride br Discussion Herein w
2023-09-27
Discussion Herein, we demonstrate that mice deficient in L-12/15 LO are more sensitive to 3-NP-induced toxicity although a substantial individual variability in striatal lesion size in response to 3-NP in both genotypes was observed. This variability is not atypical; several studies demonstrate s
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A high throughput screening campaign led
2023-09-27
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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As a neuropeptide Apelin also has
2023-09-27
As a neuropeptide, Apelin also has a critical role in cardiovascular diseases. Systemic administration of Apelin exert vasodilatory and antihypertensive effects [33]. Meanwhile, the apelin-APJ signal transduction pathway is related to age-associated cardiovascular diseases [34]. It has been known th
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Bamboo the fastest growing multipurpose woody plant with
2023-09-27
Bamboo, the fastest growing, multipurpose woody plant with a myriad of industrial and domestic uses is intricately associated with the cultural, social and economic conditions of people in many Asian countries. Its uses are not only limited to being used as a substitute for wood in construction, fur
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br Material and methods br Results
2023-09-27
Material and methods Results Discussion Nimodipine administration inhibited the level of AMP-activated protein kinase (AMPK) phosphorylation, a sensor of cellular energy status that directs metabolic Latrunculin B sale to support cellular growth and survival. CCH influences the oxygen and g
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