Location, location, location...site-specific GPCR phosphorylation offers a mechanism for cell-type-specific signalling.

abstract：:The rise of multidrug-resistant pathogens and the dearth of new antibiotic development place an existential strain on successful infectious disease therapy. Breakthrough strategies that go beyond classical antibiotic mechanisms are needed to combat this looming public health catastrophe. Reconceptualizing antibiotic t...

journal_title：Trends in pharmacological sciences

authors： Munguia J,Nizet V

更新日期：2017-05-01 00:00:00

abstract：:Apoptosis plays a key role in tumour biology, and the induction of apoptosis forms a cornerstone of most anticancer therapies. New developments in nuclear magnetic resonance spectroscopy (MRS) and magnetic resonance imaging (MRI) have taken these techniques far beyond their original roles as the workhorses of structur...

journal_title：Trends in pharmacological sciences

authors： Hakumäki JM,Brindle KM

更新日期：2003-03-01 00:00:00

abstract：:Platelet activating factor (PAF) is a phospholipid mediator of inflammation and stimulates anion secretion in animals and in isolated preparations of human colon. Nitric oxide (NO), synthesized from the amino acid L-arginine, is an important enteric inhibitory neurotransmitter. In addition, NO-donating compounds stimu...

journal_title：Trends in pharmacological sciences

authors： Izzo AA,Gaginella TS,Mascolo N,Capasso F

更新日期：1998-10-01 00:00:00

abstract：:The metabotropic glutamate (mGlu) receptors are a family of G-protein-coupled receptors (GPCRs) that regulate cell physiology throughout the nervous system. The potential of mGlu receptors as therapeutic targets has been bolstered by current research that has provided insight into the diverse modes of mGlu activation ...

journal_title：Trends in pharmacological sciences

authors： Stansley BJ,Conn PJ

更新日期：2019-04-01 00:00:00

abstract：:Receptors that are coupled to the production of inositol (1,4,5)-trisphosphate cause an increase in cytosolic free Ca2+ concentration as a consequence of both Ca2+ mobilization from intracellular stores and Ca2+ influx through the plasma membrane. Although this latter phenomenon appears attributable to the activation ...

journal_title：Trends in pharmacological sciences

authors： Fasolato C,Innocenti B,Pozzan T

更新日期：1994-03-01 00:00:00

abstract：:Five subtypes of muscarinic acetylcholine receptors have been identified in mammalian tissues, but the selectivity of ligands that are active at these receptors is low. It is possible, however, that selective compounds may be developed by targeting their allosteric site(s). Important new insights into the mechanism of...

journal_title：Trends in pharmacological sciences

authors： Tucek S,Proska J

更新日期：1995-06-01 00:00:00

abstract：:Stem cells derived from pre-implantation human embryos or from somatic cells by reprogramming are pluripotent and self-renew indefinitely in culture. Pluripotent stem cells are unique in being able to differentiate to any cell type of the human body. Differentiation towards the cardiac lineage has attracted significan...

journal_title：Trends in pharmacological sciences

authors： Braam SR,Passier R,Mummery CL

更新日期：2009-10-01 00:00:00

abstract：:During the past decade remarkable progress in molecular genetics and the possibility of manipulating cells so that the expression of genes can directly 'report' on drug activity has produced major changes in drug development strategies. The recent description and pharmacological validation of reporter mice for in vivo...

journal_title：Trends in pharmacological sciences

authors： Maggi A,Ottobrini L,Biserni A,Lucignani G,Ciana P

更新日期：2004-06-01 00:00:00

abstract：:Clodronate is a first-generation bisphosphonate used worldwide for antiresorptive therapy for osteoporosis. Although clodronate is analgesic in nature, its mechanism and efficacy were unknown for some time. Recently, clodronate was identified as a selective and potent inhibitor for vesicular nucleotide transporter (VN...

journal_title：Trends in pharmacological sciences

authors： Moriyama Y,Nomura M

更新日期：2018-01-01 00:00:00

abstract：:Genes encoding glutamate receptor channel subunits were identified in genomes from Drosophila melanogaster and Caenorhabditis elegans by homology search with amino acid sequences that participate in the conserved channel pore. The predicted sequences of the putative glutamate receptor subunits revealed a distinct chan...

journal_title：Trends in pharmacological sciences

authors： Sprengel R,Aronoff R,Völkner M,Schmitt B,Mosbach R,Kuner T

更新日期：2001-01-01 00:00:00

abstract：:Pharmacological studies as well as molecular cloning of 5-HT receptors have revealed a multiplicity of receptor subtypes, not only in mammals but, as discussed in this review by René Hen, also in molluscs and arthropods. Most of these receptors belong to the G protein-coupled receptor family, and their mechanism of ac...

journal_title：Trends in pharmacological sciences

authors： Hen R

更新日期：1992-04-01 00:00:00

abstract：:Kinin B1 and B2 receptors are central to the aetiology of pain and inflammation. Constitutive B2 receptors are commonly associated with the acute phase of inflammation and nociception, whereas the inducible B1 receptors are mostly linked to the chronic or persistent phase (or both). Therefore, selective, orally active...

journal_title：Trends in pharmacological sciences

authors： Campos MM,Leal PC,Yunes RA,Calixto JB

更新日期：2006-12-01 00:00:00

abstract：:In 1964, the psychoactive ingredient of Cannabis sativa, Δ(9)-tetrahydrocannabinol (THC), was isolated. Nearly 30 years later the endogenous counterparts of THC, collectively termed endocannabinoids (eCBs), were discovered: N-arachidonoylethanolamine (anandamide) (AEA) in 1992 and 2-arachidonoylglycerol (2-AG) in 1995...

journal_title：Trends in pharmacological sciences

authors： Maccarrone M,Bab I,Bíró T,Cabral GA,Dey SK,Di Marzo V,Konje JC,Kunos G,Mechoulam R,Pacher P,Sharkey KA,Zimmer A

更新日期：2015-05-01 00:00:00

abstract：:5-HT(3) receptors are widely distributed in the CNS and PNS where they participate in a variety of physiological processes. Native 5-HT(3) receptors in the CNS display functional and pharmacological heterogeneity, suggesting the existence of multiple receptor subunits. However, recent evidence suggests that of the two...

journal_title：Trends in pharmacological sciences

authors： van Hooft JA,Yakel JL

更新日期：2003-04-01 00:00:00

abstract：:The breast cancer resistance protein [BCRP (also known as ABCG2)] belongs to the ATP binding cassette (ABC) family of transmembrane drug transporters. BCRP has a broad substrate specificity and actively extrudes a wide variety of drugs, carcinogens and dietary toxins from cells. Situated in the apical plasma membrane ...

journal_title：Trends in pharmacological sciences

authors： van Herwaarden AE,Schinkel AH

更新日期：2006-01-01 00:00:00

abstract：:Several clinical studies document a greater discrimination between asthmatic and healthy subjects in bronchial responsiveness to a range of stimuli such as cold air, distilled water and sodium metabisulphite, than to conventional bronchoconstrictor agonists including histamine and methacholine. One of the mechanisms t...

journal_title：Trends in pharmacological sciences

authors： Spina D,Shah S,Harrison S

更新日期：1998-11-01 00:00:00

abstract：:Elucidating plant-specialized biosynthetic pathways has always constituted a laborious task, notably for natural products with high pharmaceutical values. Here, we discuss emerging omics-based strategies that facilitate the identification of genes from these complex metabolic pathways, paving the way to engineered sup...

journal_title：Trends in pharmacological sciences

authors： Dugé de Bernonville T,Papon N,Clastre M,O'Connor SE,Courdavault V

更新日期：2020-03-01 00:00:00

abstract：:Neuronal Ca2+-sensor (NCS) proteins constitute a subfamily of closely related EF-hand Ca2+-binding proteins that are expressed mainly in neurons or retinal photoreceptor cells. A variety of different neuronal functions have been attributed to these proteins. However, important new discoveries indicate that these prote...

journal_title：Trends in pharmacological sciences

authors： Braunewell KH

更新日期：2005-07-01 00:00:00

abstract：:Cannabinoids have emerged as powerful drug candidates for the treatment of inflammatory and autoimmune diseases due to their immunosuppressive properties. Significant clinical and experimental data on the use of cannabinoids as anti-inflammatory agents exist in many autoimmune disease settings, but virtually no studie...

journal_title：Trends in pharmacological sciences

authors： Nagarkatti M,Rieder SA,Hegde VL,Kanada S,Nagarkatti P

更新日期：2010-08-01 00:00:00

abstract：:Signal transducer and activator of transcription 3 (STAT3) plays crucial roles in several cellular processes such as cell proliferation and survival, and has been found to be aberrantly activated in many cancers. Much research has explored the leading mechanisms for regulating the STAT3 pathway and its role in promoti...

journal_title：Trends in pharmacological sciences

authors： Zhao C,Li H,Lin HJ,Yang S,Lin J,Liang G

更新日期：2016-01-01 00:00:00

abstract：:HIV-1 integrase (IN) executes the insertion of proviral DNA into the host cell genome, an essential step in the retroviral life cycle. This is a multi-step process that starts in the cytosol and culminates in the nucleus of the infected cell. It is becoming increasingly clear that IN interacts with a wide range of dif...

journal_title：Trends in pharmacological sciences

authors： Al-Mawsawi LQ,Neamati N

更新日期：2007-10-01 00:00:00

abstract：:Adenosine, when given by inhalation, initiates the narrowing of airways in subjects with asthma or chronic obstructive pulmonary disease (COPD). The underlying mechanism of this narrowing appears to involve the stimulation of specific mast cell surface adenosine receptors with the subsequent release of mediators and c...

journal_title：Trends in pharmacological sciences

authors： Spicuzza L,Bonfiglio C,Polosa R

更新日期：2003-08-01 00:00:00

abstract：:The sialic acid-binding immunoglobulin-like lectins (Siglecs) are a family of immunomodulatory receptors whose functions are regulated by their glycan ligands. Siglecs are attractive therapeutic targets because of their cell type-specific expression pattern, endocytic properties, high expression on certain lymphomas/l...

journal_title：Trends in pharmacological sciences

authors： Angata T,Nycholat CM,Macauley MS

更新日期：2015-10-01 00:00:00

abstract：:Exposure of cells to agonists of receptors linked to G proteins can result in downregulation of cellular levels or redistribution of G proteins from membranes to the cytosol. Agonist-induced reductions in G protein levels have been observed for members of each of the Gs, Gi and Gq families of G proteins, are likely to...

journal_title：Trends in pharmacological sciences

authors： Milligan G

更新日期：1993-11-01 00:00:00

abstract：:Ubiquitination is a highly conserved post-translational modification that regulates protein trafficking, function, and turnover. Ubiquitin ligases (E3s) conjugate ubiquitin polypeptides on substrates, whereas deubiquitnases (DUBs) reverse ubiquitination. Engineering of chemical antagonists and inhibitors of ubiquitin ...

journal_title：Trends in pharmacological sciences

authors： Lill JR,Wertz IE

更新日期：2014-04-01 00:00:00

abstract：:Chronic obstructive pulmonary disease (COPD) is caused mostly by cigarette smoking but its specific molecular mechanisms are obscure. Current theories suggest that the inflammation and oxidative stress induced by smoking lead to proteolytic imbalance and progressive lung structural derangement, with disease susceptibi...

journal_title：Trends in pharmacological sciences

authors： Anderson GP,Bozinovski S

更新日期：2003-02-01 00:00:00

abstract：:Schizophrenia is a grave psychiatric disorder with psychotic symptoms and an enigmatic etiology. Family studies have strongly indicated that genetic risk factors have a role in this disease. Recent findings, together with previously established evidence, highlight the PDZ-domain-containing protein interacting with C-k...

journal_title：Trends in pharmacological sciences

authors： Dev KK,Henley JM

更新日期：2006-11-01 00:00:00

abstract：:Recruitment of leukocytes either during development or to the site of injury is crucial. The molecular regulation of cell trafficking is complex but well orchestrated by the temporal and spatial expression of a multitude of chemokines (chemoattractant cytokines) and chemokine receptors. The chemokines, classified prim...

journal_title：Trends in pharmacological sciences

authors： Devalaraja MN,Richmond A

更新日期：1999-04-01 00:00:00

abstract：:New classes of drugs modifying Ca2+ channel activity have become available, this may enlarge the clinical utilities that have been associated with established Ca2+ channel antagonists such as the dihydropyridines (for example, nifedipine). Two such classes are reviewed by Michael Spedding, Barry Kenny and Pierre Chate...

journal_title：Trends in pharmacological sciences

authors： Spedding M,Kenny B,Chatelain P

更新日期：1995-04-01 00:00:00

abstract：:The efficacy of the powerful CRISPR-Cas9 genome-editing platform depends on DNA repair activities in the cells being targeted. Two new papers show that the low efficiency of targeting in some primary human cell lines is the result of p53-dependent cell arrest in response to the Cas9-induced break. This limitation must...

journal_title：Trends in pharmacological sciences

authors： Carroll D

更新日期：2018-09-01 00:00:00