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Topic review
Updated time: 23 Aug 2021
Submitted by: Agata Pietrzak
Definition: According to the international societies’ recommendations, the 2-deoxy-2-[18F]fluoro-D-glucose positron emission tomography/computed tomography ([18F]FDG PET/CT) technique should not be used as the method of choice in brain tumour diagnosis. Therefore, the brain region can be omitted during standard [18F]FDG PET/CT scanning. We performed comprehensive literature research and analysed results from 14,222 brain and torso [18F]FDG PET/CT studies collected in 2010–2020 to discuss whether the [18F]FDG PET/CT method may be useful in brain tumours detection.
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Topic review
Updated time: 07 Jul 2021
Submitted by: Kanwal Mahmood
Definition: One-carbon (1-C) metabolism is essential for numerous cancer cell functions, including protein and nucleic acid synthesis and maintaining cellular redox balance, and inhibition of the 1-C pathway has yielded several highly active drugs, such as methotrexate and 5-FU.
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Topic review
Updated time: 23 Aug 2021
Submitted by: Piotr Swiatek
Definition: Compounds containing the 1,2,4-triazole ring in their structure are characterised by multidirectional biological activity.
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Topic review
Updated time: 18 Mar 2021
Submitted by: Qing Wang
Definition: Since the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT2BR) in 1992, significant progress has been made in understanding the biological function, the structure, and small-molecule pharmaceutical ligands of the 5-HT2BR. Emerging evidence has suggested that the 5-HT2BR is implicated in the regulation of the cardiovascular system, fibrosis disorders, cancer, gastrointestinal (GI) tract, and nervous system. Eight crystal complex structures of the 5-HT2BR bound with different ligands provided great insights into ligand recognition, activation mechanism, and biased signaling. Numerous 5-HT2BR antagonists have been discovered and developed, and several of them have been advanced to clinical trials. It is expected that the novel 5-HT2BR antagonists with high potency and selectivity will lead to first-in-class drugs in various therapeutic areas.
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Topic review
Updated time: 09 Sep 2021
Definition: Phosphodiesterases (PDEs) inhibitors are currently a widespread and extensively studied group of anti-inflammatory and anti-fibrotic compounds which may find use in the treatment of numerous lung diseases, including asthma and chronic obstructive pulmonary disease. Several PDE inhibitors are currently in clinical development, and some of them, e.g. roflumilast, are already recommended for clinical use. Due to numerous reports indicating that elevated intracellular adenosine 3’,5’-cyclic monophosphate (cAMP) levels may contribute to alleviation of inflammation and airway fibrosis, new and effective PDE inhibitors are constantly being sought. Recently, a group of 7,8-disubstituted purine-2,6-dione derivatives, representing novel and prominent pan-PDE inhibitors has been synthesized. Some of them were reported to modulate transient receptor potential ankyrin 1 (TRPA1) ion channels as well.Compound 145 (4-(8-butoxy-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(5-(tert-butyl)-2-hydroxyphenyl)butanamide) – a pan-PDE inhibitor and a weak TRPA1 modulator inhibited fibroblast to myofibroblasts transition (FMT) as well as MRC-5 human lung fibroblasts proliferation, migration, and contraction. The effect of this compound appeared to depend mainly on its strong PDE inhibitory properties, and not on its effects on TRPA1 modulation. The strong anti-remodelling effects of 145 required activation of the cAMP/protein kinase A/CREB pathway leading to inhibition of transforming growth factortype β1(TGF-β1) and Smad-dependent signalling in MRC-5 cells.
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Topic review
Updated time: 14 Apr 2021
Submitted by: Federica Cherchi
Definition: Adenosine is a signalling molecule which, by activating specific membrane receptors, acts as an important player during brain insults such as ischemia. or demyelinating injuries. Here we review data in the literature describing A2B receptor-mediated effects in preclinical in vitro and in vivo models of cerebral ischemia and myelination that point to A2B receptor ligands as putative therapeutic targets for the still unmet treatment of stroke or demyelinating diseases.
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Topic review
Updated time: 08 Jan 2021
Submitted by: Eirini Filidou
Definition: Stem cell encapsulation is a technique that utilizes various biomaterials for the creation of a semi-permeable membrane that encases the stem cells. Stem cell encapsulation can be accomplished by employing a great variety of natural and/or synthetic hydrogels, and offers many benefits in regenerative medicine, including protection from host’s immune system and mechanical stress, improved cell viability, proliferation and differentiation, cryopreservation and controlled and continuous delivery of the stem cell secreted therapeutic agents. In this review, we report and discuss almost all natural and synthetic hydrogels used in stem cell encapsulation, along with the benefits that these materials, alone or in combinations, could offer to cell therapy through a functional cell encapsulation.
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Topic review
Updated time: 07 Feb 2021
Definition: The Aflatoxins (AF) are difuranocoumarin compounds produced as secondary metabolites of fungi of the genus Aspergillus spp. following a polyketide path.
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Topic review
Updated time: 05 Nov 2020
Submitted by: Tiziana Guarnieri
Definition: AhR, an environmentally sensitive transcription factor, is one of the more evolutionary conserved molecules in living cells.
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Topic review
Updated time: 12 Aug 2021
Submitted by: Steliana Ghibu
Definition: Cardiovascular complications are rapidly emerging as a major peril in COVID-19 in addition to respiratory disease. The mechanisms underlying the excessive effect of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection on patients with cardiovascular comorbidities remain only partly understood. SARS-CoV-2 infection is caused by binding of the viral surface spike (S) protein to the human angiotensin-converting enzyme 2 (ACE2), followed by the activation of the S protein by transmembrane protease serine 2 (TMPRSS2). ACE2 is expressed in the lung (mainly in type II alveolar cells), heart, blood vessels, small intestine, etc., and appears to be the predominant portal to the cellular entry of the virus. Based on current information, most people infected with SARS-CoV-2 virus have a good prognosis, while a few patients reach critical condition, especially the elderly and those with chronic underlying diseases. The “cytokine storm” observed in patients with severe COVID-19 contributes to the destruction of the endothelium, leading to “acute respiratory distress syndrome” (ARDS), multiorgan failure, and death. At the origin of the general proinflammatory state may be the SARS-CoV-2-mediated redox status in endothelial cells via the upregulation of ACE/Ang II/AT1 receptors pathway or the increased mitochondrial reactive oxygen species (mtROS) production. Furthermore, this vicious circle between oxidative stress (OS) and inflammation induces endothelial dysfunction, endothelial senescence, high risk of thrombosis and coagulopathy. The microvascular dysfunction and the formation of microthrombi in a way differentiate the SARS-CoV-2 infection from the other respiratory diseases and bring it closer to cardiovascular diseases like myocardial infarction and stroke. Due the role played by OS in the evolution of viral infection and in the development of COVID-19 complications, the use of antioxidants as adjuvant therapy seems appropriate in this new pathology. Alpha-lipoic acid (ALA) could be a promising candidate that, through its wide tissue distribution and versatile antioxidant properties, interferes with several signaling pathways.
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