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Molecular docking simulations were carried
2024-12-18
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic fa
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The discovery of acetylsalicylic acid aspirin
2024-12-18
The discovery of acetylsalicylic (R)-(+)-Etomoxir sodium salt (aspirin) in 1897 paved the way for the development of classical NSAIDs as first-line therapeutics for anti-inflammatory, anti-pyretic and analgesic therapy. Large efforts have been made in the following decades to improve the efficacy a
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Introduction hydroxytryptamine HT is found throughout the
2024-12-18
Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary angiotensin 2 receptor blocker (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). T
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During the year study period of
2024-12-18
During the 4-year study period, 19.9% of men in the dutasteride group developed prostate cancer as compared to 25.1% in the placebo group, which represents an absolute risk adenylate cyclase of 5.1% for men taking dutasteride (Pe weighed against the prospect of undesirable sexual side effects and d
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Using our infection assays we also explored whether
2024-12-18
Using our infection assays, we also explored whether low-pH compartments were required for the entry of ZIKVs in mammalian cells. Lysosomotropic agents such as ammonium chloride, chloroquine and Bafilomycin A1, strongly inhibited the ability of ZIKVs to enter mammalian cells. Our results are in agre
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HCC aetiology is multifactorial and the
2024-12-18
HCC aetiology is multifactorial and the disease is often preceded by other conditions including liver fibrosis and cirrhosis that are associated with HCV, HBV, alcoholic and non-alcoholic hepatitis. The discovery of new therapeutic targets will require a greater understanding of the pathogenic mech
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Compound was docked into the active site of Aurora B
2024-12-18
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the
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The acidification of endocytic compartments
2024-12-18
The acidification of endocytic compartments is closely related to endocytic activity, although the mechanism linking acidification and membrane dynamics is largely unknown. In a recent RNA interference (RNAi)-based screen, V-ATPase depletion blocked the formation of clathrin-coated vesicles, an effe
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AP activation is known to
2024-12-18
AP-1 activation is known to upregulate downstream target genes including SM-164 D1, c-myc, Bcl-xl, MMP-9, EGFR, and specific miRNAs that are involved in progression and metastasis of tumors. Moreover, matrix metalloproteinase-2 has been shown as a downstream gene of AP-1, triggered by 15-HETE in th
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ATM is generally regarded to be the principal mediator of
2024-12-18
ATM is generally regarded to be the principal mediator of the G1 Indomethacin checkpoint, whereas the induction of the intra-S-phase and G2/M checkpoints are usually primarily related to ATR function. However, several studies have demonstrated that, depending on the cellular context and type of DNA
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In this review we will present
2024-12-18
In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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We report here the case of a patient with
2024-12-17
We report here the case of a patient with probable genetic prion disease with a Creutzfeldt-Jakob disease-like phenotype associated with a rare PRNP E196K mutation who initially exhibited atypical clinical manifestations principally characterized by behavioral abnormalities. Case report An 80-ye
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br Eprosartan The AT R antagonist eprosartan is
2024-12-17
Eprosartan The AT1R antagonist eprosartan is approved for the treatment of essential Ciprofloxacin hydrochloride sale and may be administered using a convenient once-daily regimen. The drug is a well-tolerated and effective antihypertensive agent with benefit in the secondary prevention of cereb
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At the top of the S subsite cylinder
2024-12-17
At the top of the S1 subsite cylinder are two “cap” residues: E572 and M1034 [13]. Atomic structures of PfA-M1 have revealed important clues into potential roles for the cap residues in substrate selection. In the PfA-M1:bestatin co-crystal structure ([13]; Fig. 1), the P1 phenyl ring occupies the S
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br Introduction Alzheimer s disease
2024-12-17
Introduction Alzheimer's disease (AD) is a neurodegenerative disorder and the leading cause of dementia. It is characterized by progressive and irreversible damage to different ICG-001 areas, resulting in cognitive impairment and behavioral changes (O'Neill, 2013, De Strooper and Karran, 2016, A
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