Showing papers in "Pharmacological Research in 2019"

TL;DR: This review presents the available drug-enzyme X-ray crystal structures for 27 of the approved drugs as well as the chemical structures and physicochemical properties of all of the FDA-approved small molecule protein kinase antagonists.

TL;DR: The EGFR family is among the most investigated receptor protein-tyrosine kinase groups owing to its general role in signal transduction and in oncogenesis, and these receptors are implicated in the pathogenesis of a large proportion of lung and breast cancers.

TL;DR: This review aimed to present the most recent data on the emerging drug candidate targeting enzymes and intermediates involved in glucose metabolism to provide therapeutic opportunities and challenges for antiglycolytic cancer therapy.

TL;DR: A crucial mechanism in controlling cell cycle progression is the precise timing of more than 32,000 phosphorylation and dephosphorylation reactions catalyzed by a network of protein kinases and phosphoprotein phosphatases as determined by mass spectrometry.

TL;DR: This review summarized the interactions between TCM and gut microbiota, and the pharmacological effects and features of metabolites produced during interactions betweenTCM and Gut microbiota, focusing on gut microbiota and metabolites.

TL;DR: The molecular pharmacology of inflammation, chemical components and biological activities of medicinal plants such as, curcumin from Curcuma longa, and epigallocatechin‐3‐gallate from Camellia sinensis as well as their mechanism of action during inflammation at molecular level are reviewed.

TL;DR: This review highlights recent discoveries in the field of IRT and its derivatives, including analogues of the active metabolite SN38 (such as FL118), the recently approved liposomal form Nal-IRI and SN38-based immuno-conjugates currently in development ( such as sacituzumab govitecan).

TL;DR: Interference with the gut microbiota by transplanting fecal bacteria rich in SCFAs and supplementing with butyric acid were found to be effective treatments for cerebral ischemic stroke.

TL;DR: Owing to the large variety of malignancies that are driven by dysregulation of the MAP kinase pathway, additional tumor types should be amenable to MAP kinases pathway inhibitor therapy and the addition of ERK inhibitors should prove helpful.

TL;DR: The existing literature on what is known about the link between 5-HT and the immune system and the effects of 5- HT signaling on different cells of the peripheral immune system are summarized, with a particular focus on T cells.

TL;DR: The findings suggest that shikonin and its derivatives could serve as potential novel drug for the treatment of cancer and inflammation.

TL;DR: The recent progress in the research of hepatoprotective and toxic effects of different licorice-derived bioactive ingredients are summarized and the potency of these compounds are highlighted as promising therapeutic options for the treatment of liver diseases and DILI.

TL;DR: These results are the first to provide essential data showing MCC950 has the potential to become a therapeutic to prevent neurovascular remodeling and worsened cognitive decline in diabetic patients following stroke.

TL;DR: This review aims to provide a comprehensive understanding of the key notions of intestinal microbiota and dysbiosis and highlight the microbiota-phytochemical bidirectional interactions that affects bioavailability and bioactivity of parent phytochemicals and their metabolites.

TL;DR: The nanocomplex can afford a potent anticancer efficacy whereby heat and drug can be effectively deliver to the tumor, and at the same time the high dose‐associated side effects due to the separate application of chemotherapy and thermal therapy could be potentially reduced.

TL;DR: The role of RAS in cancer, the approaches used to develop direct RAS inhibitors, and recent successes in the development of novel RAS inhibitory compounds that target different aspects of R AS biochemistry are discussed.

TL;DR: The results showed that FMT, like phloretin, ameliorated UC by improving disease symptoms and colon inflammation, balancing inflammatory cytokines, maintaining intestinal barrier integrity, restoring systemic immune function, inhibiting NF-κB and NLRP3 inflammasome activation and areeliorating the oxidant stress.

TL;DR: The current review describes in detail the various reports supporting these anti-cancer studies documented with this promising agent honokiol.

TL;DR: The results suggest that FOH may block the PI3K/Akt/mTOR signaling pathway and thus exhibit anti-proliferative and anti-metastatic activity against lung cancer cells.

TL;DR: In this paper, the authors outline the generation of fatigue and put emphasis on the anti-fatigue mechanism, bioactive components and clinic trials of natural medicines, which will contribute to the development of potential antifatigue agents and open up novel treatments for sub-health.

TL;DR: The comprehending of the function of OPN in bone microenvironment is crucial for the development of novel biomarker and potential therapeutic target for the diagnosis and treatment of bone metastasis and against the emergence of drug resistance in advanced cancers.

TL;DR: Current studies and futuristic outlook in this direction are discussed in the review, which can serve as the basis for upcoming research which could boost commercial translational of improved nano‐sized curcumin combination chemotherapy.

TL;DR: The physiological function of PD-1 and its exploitation by developing tumours is outlined, and key mechanisms thought to underpin resistance to PD- 1/PD-L1 blockade are discussed, describing biomarkers that could allow patient responses to be predicted before treatment, and tracked once treatment has started.

TL;DR: This review describes 413 lignans and neolignans which have been isolated between 2016 and mid-2018 being reported in more than 300 peer-reviewed articles and covers their source, structure elucidation, and bioactivity.

TL;DR: The neuropathic pain modifying effects of metformin are sex‐specific supporting a differential role for microglial activation in male and female mice, as well as reversing neuropathic mechanical hypersensitivity when treatment is initiation weeks after injury.

TL;DR: A systematic overview of pharmacological actions, toxicological effects, and molecular targets of rutaecarpine in cardiovascular disease prevention/treatment is provided, aiming to exploit the therapeutic potential of rataecarpines and its derivatives in treating cardiovascular diseases.

TL;DR: How changes in gut microbiota composition can affect the development of hypertension and the progression of kidney diseases is described, highlighting the importance of the gut microbial composition uncovering to improve human health maintenance and, especially, for theDevelopment of new alternative therapies.

TL;DR: The antidepressant effect of certain TCMs are affirmative and encouraging, however, a lot of work needs to be done to evaluate the exact therapeutic effects and mechanisms of those active ingredients, specifically, to establish a unified standard for diagnosis and evaluation of curative effect.

TL;DR: It is shown that vitamin D supplementation can improve OS parameters; however, this finding may not be clinically significant.

TL;DR: In this paper, a systematic review and meta-analysis aimed to summarize the finding of randomized clinical trials (RCTs) examining the effects of omega-3 FAs on Oxidative Stress (OS) markers.