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Current Opinion in Pharmacology

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https://www.readbyqxmd.com/read/28340373/influence-of-sex-on-cardiovascular-drug-responses-role-of-estrogen
#1
REVIEW
Abdel A Abdel-Rahman
In this review we discuss the sex/estrogen-specific modulation of cardiovascular function and responses to current therapeutics. We discuss how anatomical differences such as a smaller kidney size, and lower glomerular filtration rate in females, reduce the clearance and increase the toxicity of some drugs in females. Other important sex differences include the dampening effect of estrogen on central sympathetic and renin angiotensin systems. Further, we discuss how a shift in myocardial redox status leads to paradoxical transformation of estrogen into a pro-inflammatory hormone...
March 21, 2017: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/28288370/the-role-of-gpcrs-in-neurodegenerative-diseases-avenues-for-therapeutic-intervention
#2
REVIEW
Yunhong Huang, Nicholas Todd, Amantha Thathiah
Neurodegenerative diseases represent a large group of neurological disorders with heterogeneous clinical and pathological profiles. The majority of current therapeutic strategies provide temporary symptomatic relief but do not target the underlying disease pathobiology and thus do not affect disease progression. G protein-coupled receptors (GPCRs) are among the most successful targets for therapeutic development of central nervous system (CNS) disorders. Many current clinical therapeutic agents act by targeting this class of receptors and downstream signaling pathways...
March 10, 2017: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/28135635/recent-advances-in-drug-discovery-of-gpcr-allosteric-modulators-for-neurodegenerative-disorders
#3
REVIEW
Robert Lütjens, Jean-Philippe Rocher
The activation or the inhibition of G-protein coupled receptors (GPCRs) implicated in the pathophysiology of neurodegenerative disorders is considered as a relevant approach for the treatment of these diseases. The modulation of the relevant GPCRs targets by positive or by negative allosteric modulators appears to be promising, the major challenge remaining the discovery of these molecules. In this review, we highlight the recent development in this field and the therapeutic potential of selected GPCRs allosteric modulators...
January 27, 2017: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/28027487/functional-selectivity-and-dualsteric-bitopic-gpcr-targeting
#4
REVIEW
Ramona Schrage, Evi Kostenis
Functional selectivity provides a new avenue to selectively engage particular pathways of the pleiotropic signaling repertoire of a G protein-coupled receptor. First examples for signaling biased compounds at the angiotensin II receptor and the μ opioid receptor have progressed to clinical trials and are promising in regard to selective activation of signaling pathways that can be linked to beneficial clinical outcomes. Dualsteric/bitopic hybrid compounds which consist of at least two pharmacophores combined in one single ligand are more recent examples for functionally selective ligands...
December 24, 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27936408/biased-mu-opioid-receptor-ligands-a-promising-new-generation-of-pain-therapeutics
#5
REVIEW
Edward R Siuda, Richard Carr, David H Rominger, Jonathan D Violin
Opioid chemistry and biology occupy a pivotal place in the history of pharmacology and medicine. Morphine offers unmatched efficacy in alleviating acute pain, but is also associated with a host of adverse side effects. The advent of biased agonism at G protein-coupled receptors has expanded our understanding of intracellular signaling and highlighted the concept that certain ligands are able to differentially modulate downstream pathways. The ability to target one pathway over another has allowed for the development of biased ligands with robust clinical efficacy and fewer adverse events...
December 6, 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27930943/analyzing-biased-responses-of-gpcr-ligands
#6
REVIEW
Besma Benredjem, Paul Dallaire, Graciela Pineyro
G protein-coupled receptors (GPCRs) are valuable targets for drug discovery. They exist in interconverting states differentially stabilized by diverse signaling partners. A ligand's capacity to distinguish among receptors associated with different partners is the basis of bias. This feature of GPCR signaling may allow development of ligands which specifically modulate effectors supporting desired actions. However, bias is time-dependent and cell-dependent such that in vitro bias may not predict bias displayed in vivo...
December 5, 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27889687/role-of-inflammation-in-obesity-related-breast-cancer
#7
REVIEW
Elisa Crespi, Giulia Bottai, Libero Santarpia
Chronic inflammation associated with obesity is now recognized to be an important condition in promoting carcinogenesis and progression in breast cancer patients, mostly in postmenopausal women with tumors expressing estrogen and progesterone receptors. In obese patients, altered levels of several inflammatory mediators regulating aromatase and estrogen expression are one of the mechanisms responsible of increase breast cancer risk. Growing attention has also been paid to the local adipose inflammation and the role played by macrophages as determinants of breast cancer risk recurrence and prognosis...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27886642/obesity-and-the-breast-cancer-methylome
#8
REVIEW
William B Coleman
Breast cancer is associated with risk factors such as advancing age and obesity. However, the linkages between these risk factors for breast cancer development and initiation of the disease are not yet clear. Obesity may drive breast cancer development through increases in circulating estrogens in postmenopausal women. Mammary cell susceptibility to neoplastic transformation requires both genetic and epigenetic alterations, including changes in DNA methylation. Obesity is also subject to epigenetic regulation...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27883943/targeted-therapy-for-breast-cancer-and-molecular-mechanisms-of-resistance-to-treatment
#9
REVIEW
Guowei Gu, Derek Dustin, Suzanne Aw Fuqua
In recent years, clinical trials investigating new drugs and therapeutic combinations have led to promising advances in breast cancer therapy. Subtyping breast cancers into hormone receptor (HR) positive, epidermal growth factor receptor (HER2) positive, and triple negative breast cancer (TNBC) is currently the basis of diagnosing and treating this disease. In addition to endocrine and HER2-targeted therapies in their respective subtypes, evidence from recent preclinical studies have shown several targetable pathways that overcome resistance in the clinical setting...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27876260/editorial-overview-endocrine-and-metabolic-diseases-adipocyte-dysfunction-fuels-signalings-for-breast-cancer-progression
#10
EDITORIAL
Sebastiano Andò
No abstract text is available yet for this article.
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27875786/inflammation-dysregulated-metabolism-and-aromatase-in-obesity-and-breast-cancer
#11
REVIEW
Heba Zahid, Evan R Simpson, Kristy A Brown
Obesity is associated with an increased risk of estrogen-dependent breast cancer after menopause. Adipose tissue undergoes important changes in obesity due to excess storage of lipids, leading to adipocyte cell death and the recruitment of macrophages. The resultant state of chronic low-grade inflammation is associated with the activation of NFkB signaling and elevated levels of aromatase, the rate-limiting enzyme in estrogen biosynthesis. This occurs not only in the visceral and subcutaneous fat, but also in the breast fat...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27816025/leptin-obesity-and-breast-cancer-progress-to-understanding-the-molecular-connections
#12
REVIEW
Ines Barone, Cinzia Giordano, Daniela Bonofiglio, Sebastiano Andò, Stefania Catalano
Obesity has a complicated connection to both breast cancer risk and the clinical behaviour of the established disease. The obese setting provides a unique adipose tissue microenvironment that, in association with systemic endocrine modifications, promotes tumor initiation, primary growth, invasion, and metastatic progression. This review presents an overview of the clinical and experimental evidences highlighting the adipokine leptin as the most important molecular mediator of obesity-breast cancer axis. The research of leptin network operating in this context could launch a new field not only in the knowledge of risk factors for breast cancer but also in the development of leptin targeting drugs as promising anticancer agents...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27750091/hedgehog-signaling-in-the-stomach
#13
REVIEW
Daniel Konstantinou, Nina Bertaux-Skeirik, Yana Zavros
The Hedgehog (Hh) signaling pathway not only plays a key part in controlling embryonic development, but in the adult stomach governs important cellular events such as epithelial cell differentiation, proliferation, gastric disease, and regeneration. In particular, Sonic Hedgehog (Shh) signaling has been well studied for its role in gastric physiology and pathophysiology. Shh is secreted from the gastric parietal cells and contributes to the regeneration of the epithelium in response to injury, or the development of gastritis during Helicobacter pylori infection...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27745842/editorial-overview-gastrointestinal-gut-hormones-from-bench-to-bedside
#14
EDITORIAL
Graham J Dockray, Andrea Varro
No abstract text is available yet for this article.
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27710813/potential-clinical-indications-for-a-cck2-receptor-antagonist
#15
REVIEW
Malcolm Boyce, Katie A Lloyd, D Mark Pritchard
Gastrin controls gastric acid secretion and mucosal cell growth, especially of enterochromaffin-like cells, via gastrin/cholecystokinin-2 receptor (CCK2R) binding and downstream signalling. Studies in animal models, healthy subjects and patients with gastric neuroendocrine tumours provide compelling evidence to justify developing a CCK2R antagonist (CCK2RA) for preventing or treating the trophic effects of hypergastrinaemia or conditions expressing CCK2R, and with or without a proton pump inhibitor, for treating gastric acid-related conditions...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27643666/gut-hormone-gpcrs-structure-function-drug-discovery
#16
REVIEW
Arnau Cordomí, Daniel Fourmy, Irina G Tikhonova
Crystallization and determination of the high resolution three-dimensional structure of the β2-adrenergic receptor in 2007 was followed by structure elucidation of a number of other receptors, including those for neurotensin and glucagon. These major advances foster the understanding of structure-activity relationship of these receptors and structure-based rational design of new ligands having more predictable activity. At present, structure determination of gut hormone receptors in complex with their ligands (natural, synthetic) and interacting signalling proteins, for example, G-proteins, arrestins, represents a challenge which promises to revolutionize gut hormone endocrinonology...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27607913/development-of-novel-ligands-for-peptide-gpcrs
#17
REVIEW
Brian M Moran, Aine M McKillop, Finbarr Pm O'Harte
Incretin based glucagon-like peptide-1 receptor (GLP-1R) agonists which target a G-protein coupled receptor (GPCR) are currently used in the treatment of type 2 diabetes. This review focuses on GPCRs from pancreatic β-cells, including GLP-1, glucose-dependent insulinotropic polypeptide (GIP), glucagon, somatostatin, pancreatic polypeptide (PP), cholecystokinin (CCK), peptide YY (PYY), oxyntomodulin (OXM) and ghrelin receptors. In addition, fatty acids GPCRs are thought to have an increasing role in regulating peptide secretions namely short fatty acids GPCR (GPR41, GPR43), medium chain fatty acid GPCR (GPR84), long chain fatty acid GPCR (GPR40, GPR120) and cannabinoid-like GPCR (GPR55, GPR119)...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27597736/neuroendocrine-peptide-mechanisms-controlling-intestinal-epithelial-function
#18
REVIEW
Helen M Cox
Enteroendocrine cells (EECs) contain different combinations of hormones, which are released following stimulation of nutrient receptors that are selectively expressed by these cells. This chemosensation varies according to the intestinal area and species of interest, and responses to meals are rapidly modified following bariatric surgery. Such surgically-induced gastrointestinal (GI) changes highlight considerable enteroplasticity, however our understanding of even the acute physiological control and consequences of neuroendocrine peptide release is still under-developed...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27591964/glp-1-as-a-target-for-therapeutic-intervention
#19
REVIEW
Surya Panicker Rajeev, John Wilding
Glucagon-like peptide receptor agonists (GLP-1 RA) have multiple effects, including control of glycaemia via stimulation of insulin and suppression of glucagon secretion and reduction of adiposity by enhancing satiety, so are an attractive therapeutic option in type 2 diabetes management. Five GLP-1 RA are used currently and more are in development. The HbA1c reduction obtained varies from 1 to 2%; they reduce body weight by about 2-3kg when used to treat T2DM, while liraglutide results in greater weight loss at a higher dose and has recently been approved for the management of obesity...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27591963/novel-developments-in-vagal-afferent-nutrient-sensing-and-its-role-in-energy-homeostasis
#20
REVIEW
Guillaume de Lartigue, Charlene Diepenbroek
Vagal afferent neurons (VANs) play an important role in the control of food intake by signaling nutrient type and quantity to the brain. Recent findings are broadening our view of how VANs impact not only food intake but also energy homeostasis. This review focuses exclusively on studies of the vagus nerve from the past 2 years that highlight major new advancements in the field. We firstly discuss evidence that VANs can directly sense nutrients, and we consider new insights into mechanisms affecting sensing of gastric distension and signaling by gastrointestinal hormones ghrelin and GLP1...
December 2016: Current Opinion in Pharmacology
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