The missing link: chemokine receptors and tissue matrix breakdown in COPD.

abstract：:In drug development, major resources are invested into the development of cellular delivery systems to increase the effectiveness of a large array of potential therapeutics, such as proteins and oligonucleotides. These carriers comprise cell-penetrating peptides (CPPs), cationic lipids and cationic polymers. In recent...

journal_title：Trends in pharmacological sciences

authors： Verdurmen WP,Brock R

更新日期：2011-02-01 00:00:00

abstract：:Inter-organelle signaling plays important roles in many physiological functions. Endoplasmic reticulum (ER)-mitochondrion signaling affects intramitochondrial calcium (Ca(2+)) homeostasis and cellular bioenergetics. ER-nucleus signaling attenuates ER stress. ER-plasma membrane signaling regulates cytosolic Ca(2+) home...

journal_title：Trends in pharmacological sciences

authors： Su TP,Hayashi T,Maurice T,Buch S,Ruoho AE

更新日期：2010-12-01 00:00:00

abstract：:It is generally accepted that muscle wasting is caused by an increase in protein breakdown which seems to be associated with an ATP-dependent, non-lysosomal proteolytic system based on conjugation of proteins to the small polypeptide ubiquitin. Increases in ubiquitin conjugates and in ubiquitin mRNAs are found in the ...

journal_title：Trends in pharmacological sciences

authors： Argilés JM,López-Soriano FJ

更新日期：1996-06-01 00:00:00

abstract：:Recent studies in mice have identified single molecules that can delay multiple diseases of aging and extend lifespan. In theory, such molecules could prevent dozens of diseases simultaneously, potentially extending healthy years of life. In this review, we discuss recent advances, controversies, opportunities, and ch...

journal_title：Trends in pharmacological sciences

authors： Hubbard BP,Sinclair DA

更新日期：2014-03-01 00:00:00

abstract：:Ischaemia-reperfusion (I/R) injury is a common feature of several diseases associated with high morbidity and mortality, such as stroke and myocardial infarction. The damaged tissue displays cardinal signs of inflammation and microvascular injury that, unless resolved, lead to long-term tissue damage with associated d...

journal_title：Trends in pharmacological sciences

authors： Gavins FN

更新日期：2010-06-01 00:00:00

abstract：:The pursuit for drugs that inhibit cyclin-dependent kinases (CDKs) has been an intense area of research for more than 15 years. The first-generation inhibitors, Flavopiridol and CY-202, are in late-stage clinical trials, but so far have demonstrated only modest activity. Several second-generation inhibitors are now in...

journal_title：Trends in pharmacological sciences

authors： Malumbres M,Pevarello P,Barbacid M,Bischoff JR

更新日期：2008-01-01 00:00:00

abstract：:During the past decade, translocator protein 18 kDa (TSPO), previously named peripheral benzodiazepine receptor, has gained a great deal of attention based on its use as a clinical biomarker of neuroinflammation with therapeutic potential. However, there is a paucity of knowledge on the function(s) of TSPO in glial ce...

journal_title：Trends in pharmacological sciences

authors： Guilarte TR,Loth MK,Guariglia SR

更新日期：2016-05-01 00:00:00

abstract：:Dimerization is fairly common in the G-protein-coupled receptor (GPCR) superfamily. First attempts to rationalize this phenomenon gave rise to an idea that two receptors in a dimer could be necessary to bind a single molecule of G protein or arrestin. Although GPCRs, G proteins and arrestins were crystallized only in ...

journal_title：Trends in pharmacological sciences

authors： Gurevich VV,Gurevich EV

更新日期：2008-05-01 00:00:00

abstract：:Gastroesophageal reflux disease (GERD) is very common and advances in drug development over recent years have markedly improved GERD management. A wide range of medications are currently used in GERD treatment, including antacids, Gaviscon, sucralfate, histamine-2 receptor antagonists and prokinetics. However, proton ...

journal_title：Trends in pharmacological sciences

authors： Hershcovici T,Fass R

更新日期：2011-04-01 00:00:00

abstract：:Until recently, release studies have failed to indicate the existence of autoreceptors on motor nerves. Ignaz Wessler now reports on a refinement of the technique - the measurement of newly synthesized [3H]acetylcholine released from the phrenic nerve - which provides clear evidence in support of release-modulating au...

journal_title：Trends in pharmacological sciences

authors： Wessler I

更新日期：1989-03-01 00:00:00

abstract：:It has taken 17 years from the first identification of a voltage-gated Ca2+ channel (CaV) beta-subunit as a band on a gel following purification of skeletal muscle dihydropyridine (DHP) receptors in 1987 to the publication of key information on the structures of Ca2+ channel beta-subunits. Three recent X-ray crystallo...

journal_title：Trends in pharmacological sciences

authors： Richards MW,Butcher AJ,Dolphin AC

更新日期：2004-12-01 00:00:00

abstract：:It has been over 50years since Sir James Black developed the first beta adrenergic receptor (βAR) blocker to treat heart disease. At that time, the concept of cell surface receptors was relatively new and not widely accepted, and most of the tools currently used to characterize plasma membrane receptors had not been d...

journal_title：Trends in pharmacological sciences

authors： Kobilka BK

更新日期：2011-04-01 00:00:00

abstract：:Intercellular transfer of proteins is a mode of communication between cells that is crucial for certain physiological processes. Chemotherapy is the treatment of choice for approximately 50% of all cancers. However, multidrug resistance mediated by drug-efflux pumps such as P-glycoprotein (Pgp) minimizes the effective...

journal_title：Trends in pharmacological sciences

authors： Ambudkar SV,Sauna ZE,Gottesman MM,Szakacs G

更新日期：2005-08-01 00:00:00

abstract：:The use of genetically-engineered mice has identified alpha2- and alpha3-subunit containing GABA(A) receptors as principal contributors to the spinal disinhibition that occurs after inflammation and neuropathic injury. Pharmacological comparison of subtype selective allosteric modulators such as NS11394 and L838417 wi...

journal_title：Trends in pharmacological sciences

authors： Munro G,Ahring PK,Mirza NR

更新日期：2009-09-01 00:00:00

abstract：:Heat shock proteins (HSPs) constitute a large family of proteins involved in protein folding and maturation whose expression is induced by heat shock or other stressors. The major groups are classified based on their molecular weights and include HSP27, HSP40, HSP60, HSP70, HSP90, and large HSPs. HSPs play a significa...

journal_title：Trends in pharmacological sciences

authors： Wu J,Liu T,Rios Z,Mei Q,Lin X,Cao S

更新日期：2017-03-01 00:00:00

abstract：:Cyclic AMP (cAMP) steers the generation of basal heart beat in the sinoatrial node. It also induces sinoatrial tachycardia and increased cardiac force, elicited through activation of Gs-protein-coupled receptors (GsPCRs). Phosphodiesterases (PDEs) hydrolyse cAMP. In the heart mainly PDE3 and PDE4 would be expected to ...

journal_title：Trends in pharmacological sciences

authors： Kaumann AJ

更新日期：2011-07-01 00:00:00

abstract：:The ability to target specific cell types to achieve optimal distribution of therapeutic entities into diseased tissues, while limiting possible adverse off-target effects, has long been a goal of many research groups and pharmaceutical organizations. This review focuses on peptidic tissue-specific biomarkers that all...

journal_title：Trends in pharmacological sciences

authors： Svensen N,Walton JG,Bradley M

更新日期：2012-04-01 00:00:00

abstract：:Recent studies have proposed a functional link between annexin 1 (ANXA1), an endogenous anti-inflammatory mediator, and receptors of the formyl-peptide family. In particular, exogenous and endogenous ANXA1 and its peptidomimetics interact with one member of this family, the formyl-peptide-receptor-like 1. Further anal...

journal_title：Trends in pharmacological sciences

authors： Perretti M

更新日期：2003-11-01 00:00:00

abstract：:Three 'alpha 1-adrenoceptors' and three 'alpha 2-adrenoceptors' have now been cloned. How closely do these receptors match the native receptors that have been identified pharmacologically? What are the properties of these receptors, and how do they relate to other members of the cationic amine receptor family? Kevin L...

journal_title：Trends in pharmacological sciences

authors： Harrison JK,Pearson WR,Lynch KR

更新日期：1991-02-01 00:00:00

abstract：:A family of peptides that shares a common C-terminal sequence (Phe-X-Gly-Leu-MetNH2) exists in mammalian and non-mammalian species. In mammals, three of these peptides (substance P, neurokinin A and neurokinin B) satisfy the criteria to be considered as neurotransmitters either in the central, peripheral or enteric ne...

journal_title：Trends in pharmacological sciences

authors： Maggi CA

更新日期：2000-05-01 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：:Cytochrome P450 3A (CYP3A) enzymes metabolize a wide variety of xenobiotics including many drugs. Because CYP3A is localized in both the liver and intestine, it can make a major contribution to the presystemic elimination of substrate drugs after oral administration ('first-pass metabolism'). However, assessments of t...

journal_title：Trends in pharmacological sciences

authors： van Herwaarden AE,van Waterschoot RA,Schinkel AH

更新日期：2009-05-01 00:00:00

abstract：:The phospholipase A2 enzymes are important components of the cellular machinery that responds to inflammatory stimuli and maintains cell homeostasis by membrane remodelling. Their role as the rate-limiting step in the production of pro-inflammatory lipid mediators makes these enzymes an important therapeutic target fo...

journal_title：Trends in pharmacological sciences

authors： Glaser KB,Mobilio D,Chang JY,Senko N

更新日期：1993-03-01 00:00:00

abstract：:The current classification for 5-HT2 receptors accommodates three subtypes. In addition to the originally defined 5-HT2 receptor, sanctuary is now provided for the structurally related 5-HT1c receptor (now 5-HT2c) and at least one atypical 5-HT receptor subtype. The strong functional union of this family is reflected ...

journal_title：Trends in pharmacological sciences

authors： Baxter G,Kennett G,Blaney F,Blackburn T

更新日期：1995-03-01 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：:Epoxyeicosatrienoic acids (EETs), derived from arachidonic acid by cytochrome P450 epoxygenases, are potent vasodilators that function as endothelium-derived hyperpolarizing factors in some vascular beds. EETs are rapidly metabolized by soluble epoxide hydrolase to form dihydroxyeicosatrienoic acids (DHETs). Recent re...

journal_title：Trends in pharmacological sciences

authors： Larsen BT,Campbell WB,Gutterman DD

更新日期：2007-01-01 00:00:00

abstract：:The fruit fly Drosophila melanogaster has been used for modeling cancer and as an in vivo tool for the validation and/or development of cancer therapeutics. The impetus for the use of Drosophila in cancer research stems from the high conservation of its signaling pathways, lower genetic redundancy, short life cycle, g...

journal_title：Trends in pharmacological sciences

authors： Yadav AK,Srikrishna S,Gupta SC

更新日期：2016-09-01 00:00:00

abstract：:The broad importance of receptor-activated phosphoinositide hydrolysis in the physiological action of hormones, neurotransmitters and growth factors has sparked interest in the study of transmembrane signalling events responsible for activation of phospholipase C. As with receptors involved in regulation of adenylyl c...

journal_title：Trends in pharmacological sciences

authors： Boyer JL,Hepler JR,Harden TK

更新日期：1989-09-01 00:00:00

abstract：:Successful biologics must satisfy multiple properties including activity and particular physicochemical features that are globally defined as developability. These multiple properties must be simultaneously optimized in a very broad design space of protein sequences and buffer compositions. In this context, artificial...

journal_title：Trends in pharmacological sciences

authors： Narayanan H,Dingfelder F,Butté A,Lorenzen N,Sokolov M,Arosio P

更新日期：2021-01-23 00:00:00

abstract：:Network and systems biology offer a novel way of approaching drug discovery by developing models that consider the global physiological environment of protein targets, and the effects of modifying them, without losing the key molecular details. Here we review some recent advances in network and systems biology applied...

journal_title：Trends in pharmacological sciences

authors： Pujol A,Mosca R,Farrés J,Aloy P

更新日期：2010-03-01 00:00:00