CDK inhibitors in cancer therapy: what is next?

abstract：:Cardiovascular disease remains the leading cause of death worldwide. Among many potential targets for pharmacological intervention, a promising strategy involves epoxyeicosatrienoic acid (EET) and soluble epoxide hydroxylase (sEH) inhibition. sEH is the enzyme that converts EET to its less potent metabolite; therefore...

journal_title：Trends in pharmacological sciences

authors： Romashko M,Schragenheim J,Abraham NG,McClung JA

更新日期：2016-11-01 00:00:00

abstract：:For more than 30 years, WNT/β-catenin and planar cell polarity signaling has formed the basis for what we understand to be the primary output of the interaction between WNTs and their cognate receptors known as Frizzleds (FZDs). In the shadow of these pathways, evidence for the involvement of heterotrimeric G proteins...

journal_title：Trends in pharmacological sciences

authors： Schulte G,Wright SC

更新日期：2018-09-01 00:00:00

abstract：:Traditional African medicine (TAM) is a shorthand reference to indigenous forms of healing that are practiced all over Africa. Although TAM is based on the accumulated experience of ancient Africans, its mode of transmission by word-of-mouth has hindered emergence of a generally accepted theory and hence of the system...

journal_title：Trends in pharmacological sciences

authors： Okpako DT

更新日期：1999-12-01 00:00:00

abstract：:Release of cytotoxic granule proteins from activated eosinophil granules is considered to be a key pathogenic mechanism in eosinophilic diseases. Degenerated eosinophils and extracellular eosinophil granules have been repeatedly depicted. The present overview describes evidence that eosinophil lysis and distribution o...

journal_title：Trends in pharmacological sciences

authors： Persson CG,Erjefält JS

更新日期：1997-04-01 00:00:00

abstract：:Hypercontraction or abnormal contraction of vascular smooth muscle is a major cause of diseases such as hypertension and vasospasm of the coronary and cerebral arteries. A better understanding of the mechanism of regulation of smooth muscle contraction should lead to improved treatments for such diseases. Recent studi...

journal_title：Trends in pharmacological sciences

authors： Fukata Y,Amano M,Kaibuchi K

更新日期：2001-01-01 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：:For many years the prevailing view of how steroid hormone receptors exert their effects on gene transcription has been that these intracellular receptor proteins, upon association with their specific cognate ligands, undergo a transformation to a state where they are capable of interacting with chromatin and regulatin...

journal_title：Trends in pharmacological sciences

authors： Power RF,Conneely OM,O'Malley BW

更新日期：1992-08-01 00:00:00

abstract：:Upregulation of binding to nicotinic acetylcholine receptors (nAChRs) is observed in the brains of both smokers and animals chronically exposed to nicotine, although whether this in vivo change is accompanied by an increase in receptor function is unknown. In vitro recordings indicate that alpha4beta2- and alpha7-subt...

journal_title：Trends in pharmacological sciences

authors： Buisson B,Bertrand D

更新日期：2002-03-01 00:00:00

abstract：:Much regarding the engagement of the G(12) family of heterotrimeric G proteins (G(12) and G(13)) by agonist-activated receptors remains unclear. For example, the identity of receptors that couple unequivocally to G(12) and G(13) and how signals are allocated among these and other G proteins remain open questions. Part...

journal_title：Trends in pharmacological sciences

authors： Riobo NA,Manning DR

更新日期：2005-03-01 00:00:00

abstract：:Apoptosis is an area of intense scientific interest, which encompasses the study of and triggers mechanisms involved in mediating the cell biology of programmed cell death. A number of low molecular weight compounds have been used to inhibit or enhance this fundamental cellular process and so apoptosis has now become ...

journal_title：Trends in pharmacological sciences

authors： Kinloch RA,Treherne JM,Furness LM,Hajimohamadreza I

更新日期：1999-01-01 00:00:00

abstract：:Clinical experience with muscarinic agonists in the symptomatic treatment of Alzheimer's disease includes studies of the effects of pilocarpine, arecoline, bethanechol, oxotremorine and RS 86. Although the results are somewhat conflicting, there is evidence that a subgroup of patients may respond with an improvement o...

journal_title：Trends in pharmacological sciences

authors： Gray JA,Enz A,Spiegel R

更新日期：1989-12-01 00:00:00

abstract：:Within the past six months, isolation of cDNA or genomic clones has been reported for three 5-HT receptors, the 5-HT1C, 5-HT1A and 5-HT2 subtypes. As members of the G protein receptor superfamily, all three 5-HT receptor clones encode single-subunit proteins containing approximately 450 amino acids arrayed as seven in...

journal_title：Trends in pharmacological sciences

authors： Hartig PR

更新日期：1989-02-01 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：:An unlikely animal model is gaining popularity in neuropharmacological research: the 2-mm fruit fly (Drosophila melanogaster). Drugs have been administered to adult flies in their food and, more recently, via gasses and injections. Pharmacological tools have introduced behavioral alterations in Drosophila reminiscent ...

journal_title：Trends in pharmacological sciences

authors： Manev H,Dimitrijevic N,Dzitoyeva S

更新日期：2003-01-01 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：:Transcription factors comprise just over 7% of the human proteome and serve as gatekeepers of cellular function, integrating external signal information into gene expression programs that reconfigure cellular physiology at the most basic levels. Surface-initiated cell signaling pathways converge on transcription facto...

journal_title：Trends in pharmacological sciences

authors： Filtz TM,Vogel WK,Leid M

更新日期：2014-02-01 00:00:00

abstract：:Progress in understanding the genetic changes that drive tumorigenesis has enabled the development of molecularly targeted anticancer therapy. The first small molecule targeted to a specific protein was imatinib mesylate (Gleevec, STI571), which is used to treat chronic myeloid leukemia (CML). A recent article present...

journal_title：Trends in pharmacological sciences

authors： Michor F

更新日期：2007-05-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) comprise a large and diverse class of signal-transducing receptors that undergo dynamic and isoform-specific membrane trafficking. GPCRs thus have an inherent potential to initiate or regulate signaling reactions from multiple membrane locations. This review discusses emerging insig...

journal_title：Trends in pharmacological sciences

authors： Eichel K,von Zastrow M

更新日期：2018-02-01 00:00:00

abstract：:Benzodiazepines in clinical use have a range of pharmacological activities. Some, e.g. sedation, tolerance and addiction, are not welcome. Undesirable side-effects of drugs are often controlled by developing compounds that bind more selectively to one particular receptor subtype. An alternative approach, discussed her...

journal_title：Trends in pharmacological sciences

authors： Haefely W,Martin JR,Schoch P

更新日期：1990-11-01 00:00:00

abstract：:Molecular forms of acetylcholinesterase exhibit tissue-specific distribution, and each form is anchored to the cell surface via a particular post-translational modification of the catalytic subunit. Nibaldo Inestrosa and Alejandra Perelman review evidence that heparan sulphate proteoglycans are the extracellular matri...

journal_title：Trends in pharmacological sciences

authors： Inestrosa NC,Perelman A

更新日期：1989-08-01 00:00:00

abstract：:The purpose of this Opinion is to present a case for targeting sphingosine kinase 2 (SK2) in autoimmune/inflammatory disease. Data obtained using Sphk2-/- mice suggest that SK2 is an anti-inflammatory enzyme, although this might be misleading because of a compensatory increase in the expression of a second isoform, sp...

journal_title：Trends in pharmacological sciences

authors： Pyne NJ,Adams DR,Pyne S

更新日期：2017-07-01 00:00:00

abstract：:Controversy over the meaning of pharmacological parameters often arises because of a lack of appreciation of different hierarchical levels of analysis. In a recent letter in Trends in Pharmacological Sciences, Zhang and Kavana [1] concluded that my two-state model for allosterism lacks cooperativity, even though Figur...

journal_title：Trends in pharmacological sciences

authors： Ehlert FJ

更新日期：2016-08-01 00:00:00

abstract：:K(+) channels are macromolecules embedded in biological membranes, where they play a key role in cellular excitability and signal transduction pathways. Knowledge of their structure should help improve our understanding of their function and lead to the design of therapeutic compounds. Most pharmacological and structu...

journal_title：Trends in pharmacological sciences

authors： Rodríguez de la Vega RC,Merino E,Becerril B,Possani LD

更新日期：2003-05-01 00:00:00

abstract：:Zn(2+) is the second most prevalent trace element in the body and is present in particularly large concentrations in the mammalian brain. Although Zn(2+) is a cofactor for many enzymes in all tissues, a unique feature of brain Zn(2+) is its vesicular localization in presynaptic terminals, where its release is dependen...

journal_title：Trends in pharmacological sciences

authors： Weiss JH,Sensi SL,Koh JY

更新日期：2000-10-01 00:00:00

abstract：:During the past decade a great number of genes encoding high- and low-voltage-dependent Ca(2+) channels and their accessory subunits have been cloned. Studies of Ca(2+) channel structure-function relationships and channel regulation using cDNA expression in heterologous expression systems have revealed intricate detai...

journal_title：Trends in pharmacological sciences

authors： Muth JN,Varadi G,Schwartz A

更新日期：2001-10-01 00:00:00

abstract：:Amyotrophic lateral sclerosis (ALS) is an incurable disease that arises from the progressive loss of motoneurons. Even when caused by a single gene defect, as in the case of mutations in the enzyme Cu-Zn superoxide dismutase (SOD1), ALS is the result of a complex cascade that involves crosstalk among motoneurons, glia...

journal_title：Trends in pharmacological sciences

authors： Carrì MT,Grignaschi G,Bendotti C

更新日期：2006-05-01 00:00:00

abstract：:All currently available general anesthetics produce potentially deadly side effects. Unfortunately, few approaches have been developed to design safer ones, despite important advances in anesthetic mechanisms research. Cayla and colleagues recently showed that computational methods can be used to identify anesthetic l...

journal_title：Trends in pharmacological sciences

authors： McGrath M,Pence A,Raines DE

更新日期：2019-11-01 00:00:00

abstract：:Non-steroidal anti-inflammatory drugs (NSAIDs) have been considered for treatment and prevention of Alzheimer's disease (AD) for more than two decades. Biochemical markers in the brains of individuals with AD suggest that inflammation might be a driving cause of the disease that can be suppressed by drug treatment. In...

journal_title：Trends in pharmacological sciences

authors： Weggen S,Rogers M,Eriksen J

更新日期：2007-10-01 00:00:00

abstract：:Lithium is the simplest therapeutic agent available for the treatment of depression and has been used for over 100 years, yet no definitive mechanism for its effect has been established. Among the proposed mechanisms, two lithium-sensitive signal transduction pathways are active in the brain; these are mediated by gly...

journal_title：Trends in pharmacological sciences

authors： Williams RS,Harwood AJ

更新日期：2000-02-01 00:00:00

abstract：:Drugs of abuse are very powerful reinforcers, and even in conditions of limited access (where the organism is not dependent) these drugs will motivate high rates of operant responding. This presumed hedonic property and the drugs' neuropharmacological specificity provide a means of studying the neuropharmacology and n...

journal_title：Trends in pharmacological sciences

authors： Koob GF

更新日期：1992-05-01 00:00:00