当前位置： SCI文献检索 > BIOCHEMICAL PHARMACOLOGY期刊下所有文献 > Identification of novel transplantable GPCR recycling motif for drug discovery.

Identification of novel transplantable GPCR recycling motif for drug discovery.

Abstract：

:β1-Adrenergic receptor (β1-AR) agonists and antagonists are widely used in the treatment of major cardiovascular diseases such as heart failure and hypertension. The β1-AR like other G protein-coupled receptors (GPCRs) are endocytosed in response to intense agonist activation. Recycling of the agonist-internalized β1-AR is dependent on its carboxy-terminal type-1 PSD-95/DLG/ZO1 (PDZ) and on phospho-serine312 in the third intracellular loop of the β1-AR. Progressive elongation of the β1-AR at its C-tail inactivated the PDZ-biding domain and inhibited the recycling of the β1-AR. However, fusing a twenty amino acid peptide derived from the multiple cloning region of the mammalian expression vector pCDNA3 to the C-tail of the β1-AR (β1-AR[+20]) produced a chimeric β1-AR that recycled rapidly and efficiently. The β1-AR[+20] recycled in a type-1 PDZ and phospho-Ser312-independent manner, indicating that this peptide provided a general GPCR recycling signal. Fusing the enhanced yellow fluorescent protein (EYFP) down-stream of β1-AR[+20] generated a β1-AR-EYFP chimera that was expressed on the membrane and recycled efficiently after agonist-induced internalization. This construct trafficked in a PDZ-SNX27/retromer-independent manner. We also fused EYFP to the N-terminus of the β1-AR to created EYFP-WT β1-AR. This construct recycled in PDZ and SNX27/retromer dependent manner. These β1-AR-EYFP constructs would be useful for high throughput screening (HTS) programs to identify new entities that would interfere with the recycling of agonist internalized GPCR that traffic in PDZ-dependent vs. PDZ-independent roadmaps.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Nooh MM,Mancarella S,Bahouth SW

doi

10.1016/j.bcp.2016.09.011

subject

Has Abstract

pub_date

2016-11-15 00:00:00

pages

22-32

eissn

0006-2952

issn

1873-2968

pii

S0006-2952(16)30290-8

journal_volume

120

pub_type

杂志文章

相关文献

BIOCHEMICAL PHARMACOLOGY文献大全
  • The bioactivation of amodiaquine by human polymorphonuclear leucocytes in vitro: chemical mechanisms and the effects of fluorine substitution.

    abstract：:Amodiaquine, a 4-aminoquinoline antimalarial, has been associated with hepatitis and agranulocytosis in humans. Drug hypersensitivity reactions, especially agranulocytosis, have been attributed to reactive intermediates generated by the oxidants discharged from stimulated polymorphonuclear leucocytes (PMN). The metabo...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(95)00236-s

    authors： Tingle MD,Jewell H,Maggs JL,O'Neill PM,Park BK

    更新日期：1995-09-28 00:00:00

  • Modification of platelet function and arachidonic acid metabolism by bioflavonoids. Structure-activity relations.

    abstract：:The mechanism of the antiaggregating activity of flavonoids was studied in vitro. The activity of fifteen different compounds was tested on platelet aggregation and arachidonic acid metabolism. The effect of flavonoids on platelet adenosine 3',5'-cyclic monophosphate (cyclic AMP) levels under basal conditions, as well...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(84)90423-4

    authors： Landolfi R,Mower RL,Steiner M

    更新日期：1984-05-01 00:00:00

  • Relationship between 5-fluoro-2'-deoxyuridylate, 2'-deoxyuridylate, and thymidylate synthase activity subsequent to 5-fluorouracil administration, in xenografts of human colon adenocarcinomas.

    abstract：:5-Fluorouracil (FUra) has been administered to mice bearing xenografts of human colon adenocarcinomas. In two tumor lines, HxGC3 and HxVRC5, intrinsically resistant to FUra, 2'-deoxyuridylate (dUMP) accumulated 13.4- and 23.9-fold above basal levels. In HxELC2 xenografts, which demonstrated some sensitivity to FUra, t...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(86)90281-9

    authors： Houghton JA,Weiss KD,Williams LG,Torrance PM,Houghton PJ

    更新日期：1986-04-15 00:00:00

  • Stimulation of drug and carcinogen metabolism by prolonged oral tobacco consumption.

    abstract：:Oral administration of tobacco to rats for 21 days caused remarkable stimulation of the metabolism of phenacetin, aniline and benzo[a]pyrene, a carcinogen, by hepatic microsomal mixed function oxidases (MFO). Such treatment for 6 days resulted in a small increase in the activities of phenacetin O-dealkylase and aromat...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(82)90386-0

    authors： Kaur S,Ali B

    更新日期：1982-04-15 00:00:00

  • Effects of dihydropyridine derivatives and anticonvulsant drugs on [3H]nitrendipine binding and calcium and sodium fluxes in brain.

    abstract：:The binding of [3H]nitrendipine to rat cortical membranes was reduced by phenytoin, phenobarbital, and pentobarbital. The IC50 values were 0.09, 0.40, and 0.76 mM respectively. The drugs reduced the apparent binding affinity of [3H]nitrendipine with little effect on the maximum number of binding sites. The inhibitory ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(85)90416-2

    authors： Harris RA,Jones SB,Bruno P,Bylund DB

    更新日期：1985-06-15 00:00:00

  • Role of the endocannabinoid system in drug addiction.

    abstract：:Drug addiction is a chronic relapsing disorder that produces a dramaticglobal health burden worldwide. Not effective treatment of drug addiction is currently available probably due to the difficulties to find an appropriate target to manage this complex disease raising the needs for further identification of novel the...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2018.09.013

    authors： Manzanares J,Cabañero D,Puente N,García-Gutiérrez MS,Grandes P,Maldonado R

    更新日期：2018-11-01 00:00:00

  • Src-family kinase inhibitors block early steps of caveolin-1-enhanced lung metastasis by melanoma cells.

    abstract：:In advanced stages of cancer disease, caveolin-1 (CAV1) expression increases and correlates with increased migratory and invasive capacity of the respective tumor cells. Previous findings from our laboratory revealed that specific ECM-integrin interactions and tyrosine-14 phosphorylation of CAV1 are required for CAV1-...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2020.113941

    authors： Ortiz R,Díaz J,Díaz-Valdivia N,Martínez S,Simón L,Contreras P,Lobos-González L,Guerrero S,Leyton L,Quest AFG

    更新日期：2020-07-01 00:00:00

  • Modification of the plasma clearance and liver uptake of steroid ester-conjugated oligodeoxynucleotides by association with (lactosylated) low-density lipoprotein.

    abstract：:Low-density lipoprotein (LDL) has been proposed as carrier for the selective delivery of anticancer drugs to tumor cells. We reported earlier the association of several lipidic steroid-conjugated anticancer oligodeoxynucleotides (ODNs) with LDL. In the present study, we determined the stability of these complexes. Whe...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(00)00243-4

    authors： Rump ET,de Vrueh RL,Manoharan M,Waarlo IH,van Veghel R,Biessen EA,van Berkel TJ,Bijsterbosch MK

    更新日期：2000-06-01 00:00:00

  • Fifty years of Biochemical Pharmacology: the discipline and the journal.

    abstract：:The discipline of biochemical pharmacology emerged in the late 1940s as a result of an increasing emphasis on understanding drug mechanisms at the cellular level. This research approach has contributed significantly to the development of many new drug classes including antihypertensive, antifective, cholesterol loweri...

    journal_title：Biochemical pharmacology

    pub_type： 历史文章,杂志文章

    doi：10.1016/j.bcp.2008.03.024

    authors： Enna SJ,Feuerstein GZ,Piette J,Williams M

    更新日期：2008-07-01 00:00:00

  • Identification and characterization of a plasma membrane phosphoprotein which is present in Chinese hamster lung cells resistant to adriamycin.

    abstract：:Studies have been carried out to analyze the phosphoprotein composition of plasma membranes from Chinese hamster lung cells resistant to the action of adriamycin. Gel electrophoretic analysis of [32Pi]-labeled proteins revealed that plasma membranes from resistant cells contain a phosphoprotein of 180,000 molecular we...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(83)90315-5

    authors： Garman D,Albers L,Center MS

    更新日期：1983-12-01 00:00:00

  • Rosuvastatin reduces platelet recruitment by inhibiting NADPH oxidase activation.

    abstract：:Rosuvastatin increased vascular endothelial NO and attenuated platelet activation after ischemia-reperfusion in mice; nevertheless, the influence of rosuvastatin on the activation of human platelets and the underlying mechanism has never been investigated. In an in vitro study platelets from 8 healthy donors were incu...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2012.09.011

    authors： Pignatelli P,Carnevale R,Di Santo S,Bartimoccia S,Nocella C,Vicario T,Loffredo L,Angelico F,Violi F

    更新日期：2012-12-15 00:00:00

  • Proteasomal inhibition potentiates drugs targeting DNA topoisomerase II.

    abstract：:The reaction mechanism of DNA topoisomerase II (TOP2) involves a covalent double-strand break intermediate in which the enzyme is coupled to DNA via a 5'-phosphotyrosyl bond. This normally transient enzyme-bridged break is stabilised by drugs such as mitoxantrone, mAMSA, etoposide, doxorubicin, epirubicin and idarubic...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2015.12.015

    authors： Lee KC,Bramley RL,Cowell IG,Jackson GH,Austin CA

    更新日期：2016-03-01 00:00:00

  • Effect of D- or L-methionine and cysteine on the growth inhibitory effects of feeding 1% paracetamol to rats.

    abstract：:Rats fed 1% paracetamol in the diet failed to grow and a dose-dependent inhibition of growth was observed and found to be independent of hepatoxicity. Addition of 0.5% D- or L-methionine, or L-cysteine to a diet containing 1% paracetamol restored growth. Addition of L-methionine to the drinking water was equally effec...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(89)90048-8

    authors： McLean AE,Armstrong GR,Beales D

    更新日期：1989-01-15 00:00:00

  • Hydrolysis and binding of a toxic stereoisomer of soman in plasma and tissue homogenates from rat, guinea pig and marmoset, and in human plasma.

    abstract：:The fallen concentration of one of the two isomers of soman (1,2,2-trimethylpropyl methylphosphonofluoridate), i.e., C(+)P(-)-soman, was investigated in plasma and in homogenates of brain, lung, liver, kidney, diaphragm, skeletal muscle and mucosa of small intestines from rat, guinea pig and marmoset, and in human pla...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(93)90106-7

    authors： de Jong LP,van Dijk C,Berhitoe D,Benschop HP

    更新日期：1993-10-19 00:00:00

  • Synthesis of ATP derivatives of compounds of the mevalonate pathway (isopentenyl di- and triphosphate; geranyl di- and triphosphate, farnesyl di- and triphosphate, and dimethylallyl diphosphate) catalyzed by T4 RNA ligase, T4 DNA ligase and other ligases

    abstract：:Compounds of the mevalonate pathway containing a terminal di- or triphosphate (mev-PP or mev-PPP) were tested as substrates of several enzyme ligases (T4 RNA ligase, T4 DNA ligase, firefly luciferase and other ligases) for the synthesis of ATP derivatives of the mev-pppA or mev-ppppA type. T4 RNA ligase, in the presen...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2009.04.028

    authors： Sillero MA,de Diego A,Tavares JE,Silva JA,Pérez-Zúñiga FJ,Sillero A

    更新日期：2009-08-15 00:00:00

  • Modifications of oxido-reductase activities in adriamycin-resistant leukaemia K562 cells.

    abstract：:Adriamycin (ADR), a well-known antitumoral drug, interacts with DNA (nuclear and mitochondrial) and cardiolipin. Moreover, ADR induces numerous mitochondrial modifications in sensitive cells. However, no results have yet been obtained as to the repercussions of drug effects on oxido-reductase activities in ADR-resista...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(98)00084-7

    authors： Denis-Gay M,Petit JM,Mazat JP,Ratinaud MH

    更新日期：1998-08-15 00:00:00

  • 5-phenylthioacyclouridine: a potent and specific inhibitor of uridine phosphorylase.

    abstract：:5-Phenylthioacyclouridine (PTAU or 1-[(2-hydroxyethoxy)methyl]-5-phenylthiouracil) was synthesized as a highly specific and potent inhibitor of uridine phosphorylase (UrdPase, EC 2.4.2.3). PTAU has inhibition constant (K(is)) values of 248 and 353 nM towards UrdPase from mouse and human livers, respectively. PTAU was ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(00)00410-x

    authors： el Kouni MH,Goudgaon NM,Rafeeq M,Al Safarjalani ON,Schinazi RF,Naguib FN

    更新日期：2000-09-15 00:00:00

  • Differential activation of CYP2C9 variants by dapsone.

    abstract：:Studies have shown that CYP2C9.1 mediated metabolism of flurbiprofen or naproxen is activated by co-incubation with dapsone. However, dapsone activation has not been examined in the known variant forms of CYP2C9. Six concentrations of flurbiprofen (2-300microM) or naproxen (10-1800 microM) were co-incubated with six c...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2004.01.017

    authors： Hummel MA,Dickmann LJ,Rettie AE,Haining RL,Tracy TS

    更新日期：2004-05-15 00:00:00

  • Novel iminobenzoxathiolone compound inhibits nuclear factor-kappaB activation targeting inhibitory kappaB kinase beta and down-regulating interleukin-1beta expression in lipopolysaccharide-activated macrophages.

    abstract：:Benzoxathiolone derivatives have been reported to show pharmacological potentials in the psoriasis and acne. However, molecular basis for these pharmacological properties is little known. We postulated that the derivatives could mediate some of their pharmacological actions by modulating nuclear factor (NF)-kappaB act...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2008.05.013

    authors： Kim MH,Lee HY,Roh E,Kim BH,Chung EY,Lee YR,Lee IJ,Lee H,Lee CK,Han SB,Kim Y

    更新日期：2008-08-01 00:00:00

  • Stimulation and inhibition of adenylyl cyclase by distinct 5-hydroxytryptamine receptors.

    abstract：:5-Hydroxytryptamine (serotonin, 5-HT) stimulates basal adenylyl cyclase activity in membranes from guinea pig or rat hippocampi, but 5-HT inhibits forskolin-stimulated adenylyl cyclase activity in these same membranes. The opposing effects of 5-HT on adenylyl cyclase activity indicate that distinct 5-HT receptors, pos...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(90)90453-r

    authors： De Vivo M,Maayani S

    更新日期：1990-10-01 00:00:00

  • Binding of nitropyrenes and benzo[a]pyrene to mouse lung deoxyribonucleic acid after pretreatment with inducing agents.

    abstract：:In assessing the biological effects of exposure to a complex chemical mixture, it is important to determine how the behavior of one compound may be influenced by the presence of other compounds in the mixture. In this study the effect of pre-exposure to an organic extract of diesel exhaust or to selected compounds in ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(86)90581-2

    authors： Howard AJ,Mitchell CE,Dutcher JS,Henderson TR,McClellan RO

    更新日期：1986-07-01 00:00:00

  • The rigid steroid 21-hydroxy-6,19-epoxyprogesterone (21OH-6,19OP) is a dissociated glucocorticoid receptor modulator potentially useful as a novel coadjuvant in breast cancer chemotherapy.

    abstract：:Glucocorticoids (GCs) are steroid hormones widely used as coadjuvants in the treatment of solid tumors due to their anti-inflammatory effects. However, evidence show that they also may induce chemotherapy resistance, probably through their capacity to inhibit apoptosis triggered by antineoplastic drugs. GCs exert thei...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2014.04.006

    authors： Orqueda AJ,Dansey MV,Español A,Veleiro AS,Bal de Kier Joffé E,Sales ME,Burton G,Pecci A

    更新日期：2014-06-15 00:00:00

  • Dinner at Orazio's--David Triggle the model of a mentor.

    abstract：:What does it mean to be a mentor in science? Definitions of mentorship are freely spouted in publications and include concepts such as academic support, professional development, role modeling, interaction, impartment of knowledge, evaluation of work, demonstration of methodology, etc. Perhaps most of us would agree w...

    journal_title：Biochemical pharmacology

    pub_type： 传,历史文章,杂志文章,评审

    doi：10.1016/j.bcp.2015.06.025

    authors： Smith SL

    更新日期：2015-11-15 00:00:00

  • Novel cannabis flavonoid, cannflavin A displays both a hormetic and neuroprotective profile against amyloid β-mediated neurotoxicity in PC12 cells: Comparison with geranylated flavonoids, mimulone and diplacone.

    abstract：BACKGROUND:Flavonoids form a diverse class of naturally occurring polyphenols ascribed various biological activities, including inhibition of amyloid β (Aβ) fibrillisation and neurotoxicity of relevance to Alzheimer's disease. Cannabis contains a unique subset of prenylated flavonoids, the cannflavins. While selected c...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2019.08.011

    authors： Eggers C,Fujitani M,Kato R,Smid S

    更新日期：2019-11-01 00:00:00

  • Binding of dihydrodigitoxin to beef and human cardiac (Na+ + K+)-ATPase: evidence for two binding sites in cell membranes.

    abstract：:The specific binding of three cardiac glycosides, 3H-ouabain, 3H-digitoxin and 3H-dihydrodigitoxin, to beef cardiac (Na+ + K+)-ATPase was compared. Non-specific binding was defined as that in the presence of 0.1 mM unlabelled compound, or in the absence of ligands. The dissociation constants (KD-values) calculated fro...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(83)90202-2

    authors： Brown L,Erdmann E

    更新日期：1983-11-01 00:00:00

  • Effect of 3-aminobenzamide on antigenic variation of Trypanosoma brucei.

    abstract：:African trypanosomes, like Trypanosoma brucei, depend on antigenic variation to evade the immune response of the vertebrate host. An antigenic switch corresponds to the activation of a variable surface glycoprotein (VSG) gene from a large silent repertoire. Most switches require the duplicative transposition of a VSG ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(85)90208-4

    authors： Cornelissen AW,Michels PA,Borst P,Spanjer W,Versluijs-Broers JA,Van der Meer C,Farzaneh F,Shall S

    更新日期：1985-12-01 00:00:00

  • Histamine H1 receptor-induced Ca2+ mobilization and prostaglandin E2 release in human gingival fibroblasts. Possible role of receptor-operated Ca2+ influx.

    abstract：:Stimulation of human gingival fibroblasts with histamine elicited an increase in the intracellular concentration of free calcium ([Ca2+]i) and the formation of inositol 1,4,5-trisphosphate (InsP3) in a concentration- and time-dependent manner. The histamine-induced increase in [Ca2+]i was attenuated completely by chlo...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(96)00417-0

    authors： Niisato N,Ogata Y,Furuyama S,Sugiya H

    更新日期：1996-10-11 00:00:00

  • Structure-activity relationships for inhibition of human 5alpha-reductases by polyphenols.

    abstract：:The enzyme steroid 5 alpha-reductase (EC 1.3.99.5) catalyzes the NADPH-dependent reduction of the double bond of a variety of 3-oxo-Delta(4) steroids including the conversion of testosterone to 5 alpha-dihydrotestosterone. In humans, 5 alpha-reductase activity is critical for certain aspects of male sexual differentia...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(02)00848-1

    authors： Hiipakka RA,Zhang HZ,Dai W,Dai Q,Liao S

    更新日期：2002-03-15 00:00:00

  • IL-18BPa:Fc cooperates with immunosuppressive drugs in human whole blood.

    abstract：:The proinflammatory cytokine interleukin (IL)-18 appears to be involved in the pathogenesis of diseases associated with immunoactivation and inflammation. Consequently, blockage of IL-18 bioactivity by use of IL-18 binding protein (IL-18 BP) is likely a promising therapeutic concept. In the present study, we investiga...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(03)00294-6

    authors： Nold M,Hauser IA,Höfler S,Goede A,Eberhardt W,Ditting T,Geiger H,Pfeilschifter J,Mühl H

    更新日期：2003-08-01 00:00:00

  • Solubilization of active somatostatin receptors from rabbit retina.

    abstract：:Somatostatin receptors from rabbit retinal membranes were solubilized in an active form using a mixture of the detergent n-octyl b-D-glucopyranoside (OG) and CHAPS. The binding of [125I]-Try11-somatostatin to the soluble extract was saturable and of high affinity, with an apparent affinity constant (Kd) of 0.60 +/- 0....

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(93)90439-4

    authors： Liapakis G,Politou E,Thermos K

    更新日期：1993-05-05 00:00:00