Showing papers in "Biochemical Pharmacology in 2018"

TL;DR: This review examines a variety of H2S donor systems classified by their H 2S‐releasing trigger as well as their H1N1 release profiles, byproducts, and potential therapeutic applications.

TL;DR: The most relevant current knowledge is presented and directions for future research in these fields are proposed, from the culinary world to the clinical setting, and how much scientific truth lies in Hippocrates' famous quote: "Let your food be your medicine".

TL;DR: The therapeutic potential of targeted modulation of the macrophage heme-HO-1 system will be discussed in the context of inflammatory disorders and a particular focus will be the intricate interactions of HO-1 with its substrate heme, which play a contradictory role in distinct physiological and pathophysiological settings.

TL;DR: The role of autophagy modulation in tumour suppression is assessed by assessing existing literature in the context of autophile flux and cellular metabolism at the interface of mitochondrial function to help overcome tumour chemoresistance.

TL;DR: Quercetin ameliorates kidney injury via modulating macrophage polarization, and may have therapeutic potential for patients with kidney injury.

TL;DR: The results suggest that ferroptosis induced by erastin and the two most potent structurally unrelated lead compounds was caused by VDAC opening, leading to increased mitochondrial ROS generation and oxidative stress‐induced cell death.

TL;DR: The present study is the first to illustrate that Rh4 triggers apoptosis and autophagy via activating the ROS/JNK/p53 pathway in colorectal cancer cells, providing basic scientific evidence that Rh 4 shows great potential as an anti‐cancer agent.

TL;DR: The results suggest that standardized cannabis drug preparations, rather than pure cannabinoids, could be considered as part of the therapeutic armamentarium to manage breast cancer.

TL;DR: Oral cardamonin significantly inhibited dextran sulfate sodium (DSS)‐ and 2,4,6‐trinitrobenzene sulfonic acid (TNBS)‐induced colitis in mice, evidenced by improvement of disease activity index scores, myeloperoxidase activity, length shortening and histopathological changes of colons.

TL;DR: Results indicated that Canagliflozin might exert anti‐inflammatory effects by inhibiting intracellular glucose metabolism and promoting autophagy in immune cells.

TL;DR: The intent of this review is to focus on the different potentialities of autophagy inducers in cancer prevention versus therapy in order to elicit a desirable clinical response.

TL;DR: The contribution of adaptive immunity to the long‐term clinical benefits of anticancer treatments and the properties of immune memory that can protect cancer patients against relapse are highlighted.

TL;DR: Baicalein and baicalin alleviated APAP‐induced hepatotoxicity both in vitro and in vivo by activating Nrf2 via blocking the binding of NRF2 with Keap1 and inducing Nrf1 phosphorylation and ERK1/2 and PKC inhibitors.

TL;DR: This review summarizes the current knowledge of both the conventional and unconventional pathways for hydrogen sulfide regulation, and describes a number of standard “conventional” pathways that have been described and well characterized.

TL;DR: Ca2+ has been established as a major regulator of VSM contraction, and its sources, cytosolic levels, homeostatic mechanisms and subcellular distribution have been defined andModulators of [ Ca2+]c, PKC and ROCK activity could be useful in mitigating the increased vasoconstriction associated with vascular disease.

TL;DR: The study of EVs may provide specific, precise information regarding the AD transition stage that may offer possibilities to intervene in order to retain cognition and also represent a new therapeutical approach to CNS diseases.

TL;DR: It is concluded that each of the three gasotransmitters play similar, bell‐shaped roles in the control of HCT116 cell proliferation: endogenously produced NO, CO and H2S, at an optimal concentration, support H CT116 proliferation; inhibition of their production as well as exogenous delivery of these gasottransmitter levels above optimal concentrations suppresses colon cancer cell proliferation.

TL;DR: Non‐catalytic functions of the cholinesterases (ChEs) participate in both neurodevelopment and disease, and Manipulating either the catalytic activities or the structure of these enzymes can potentially shift the balance between beneficial and adverse effect in a wide number of physiological processes.

TL;DR: New research strategies are under development to target the endocannabinoid system for drug addiction avoiding these side effects, which include allosteric negative modulators of CB1 receptors and compounds targeting CB2 receptors.

TL;DR: The localization of the molecular components of the ECS and how they are altered under neurodegenerative conditions, either contributing to or protecting cells from degeneration are described, and the most relevant opportunities of cannabinoid pharmacology related to each disease are summarized.

TL;DR: For the first time, GPCR biased agonism is characterized in an heteromeric context and was reduced when assays were performed in cells expressing the two receptors, thus suggesting that the heteromer allows less functional selectivity.

TL;DR: An update of the various strategies employed to assign a function to these receptors and to discover new ligands is presented and several recommendations are proposed in order to strengthen the reporting of new ligand‐receptor pairs are proposed.

TL;DR: Overall, available data indicate that both NO and H2S contribute to vascular (patho)physiology and in regulating blood pressure and boosting NO andH2S using various dietary sources or donors could be a hopeful therapeutic strategy in the management of hypertension.

TL;DR: An overview of the primary polyphenols used for ND and brain tumor prevention and treatment is provided by focusing on recent findings, the principal factors limiting their application in clinical practice, and a promising delivery strategy to improve their bioavailability.

TL;DR: It is found that oral administration of Rd dose‐dependently alleviated DSS‐induced body weight loss, colon length shortening and colonic pathological damage with lower myeloperoxidase (MPO) and inducible nitric oxide synthase (iNOS) activities and higher glutathione level.

TL;DR: The existence of a GSK3‐&bgr;‐TrCP ‘destruction hit‐list’ that allows co‐ordinated removal (or stabilisation) of a set of proteins with a common physiological purpose, through control of Gsk3 is proposed.

TL;DR: This review reports the advances made in the field with a special focus on the last decade and how MAGL has become a promising therapeutic target for the treatment of several diseases that currently lack appropriate therapies.

TL;DR: The findings support the notion that the administration of TMZ together with THC:CBD combinations – and specifically those containing a higher proportion of CBD – may be therapeutically explored to target the population of GICs in GBM.

TL;DR: The dysregulation of ECS has been associated to dermatological disorders such as atopic dermatitis, psoriasis, scleroderma and skin cancer and the druggability of the ECS could open new research avenues for the treatment of the pathologies mentioned.

TL;DR: RSV, which has been suggested to attenuate DOX‐induced cytotoxicity, significantly blocks induction of E2F1/mTORC1 and E2f1/AMPK&agr;2 pathway by DOX, leading to acceleratory autophagy and inhibitory apoptosis.