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Topic review
Updated time: 14 Apr 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: 12 Apr 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: 17 Jun 2020
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: 13 Jan 2021
Submitted by: Viviana Bazan
Definition: The discovery of the EML4-ALK fusion gene in a limited subset of patients affected by NSCLC and the subsequent clinical development of crizotinib in 2011 has been an impressive milestone in lung cancer research. Unfortunately, acquired resistances regularly develop, hence disease progression occurs. Afterward, modern tyrosine kinase inhibitors (TKIs), such as ceritinib, alectinib, brigatinib, and lorlatinib, have been approved by the Food and Drug Administration (FDA) for the management of anaplastic lymphoma kinase (ALK)-positive NSCLCs. Several compounds are currently under investigation to achieve the optimal strategy of therapy.
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Biography
Updated time: 29 Oct 2020
Abstract: My laboratory for the Study of Neurohormonal Control of the Circulation studies the molecular pharmacology, physiology, and biology of the G protein-coupled receptors (GPCRs) that regulate cardiac function and systemic circulation in general. Particular emphasis is given to autonomic nervous system`s (specifically adrenergic) receptors and to angiotensin II receptors. The general focus is on studying mechanisms underlying abnormal signaling/function of these GPCRs that contribute to heart failure pathophysiology, aiming at discovering and validating novel molecular targets for cardiovascular disease therapy. Our lab`s studies also include novel molecular effects of beta-blockers and angiotensin receptor blockers, two very important drug classes acting through cardiovascular adrenergic and angiotensin receptors, respectively.
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