Abstract:
:Two peptides, which have no significant homology with known protein structures, were obtained by microsequencing of a mu-opioid binding protein purified to homogeneity from bovine striatal membranes. Polyclonal antibodies generated against portions of these peptides immunoprecipitated up to 65% of radiolabeled purified opioid binding protein. Sequential immunoprecipitations, using antibodies directed against portions of the two different peptides, confirmed that the peptides are derived from the same protein. Immunoblots of the protein with antipeptide antibodies revealed a protein band corresponding to the molecular weight of denatured reduced mu-opioid binding protein. The immunoresponse was blocked by the appropriate peptide and was not observed with irrelevant antisera. The antipeptide antibodies were used for immunoblots of sodium dodecyl sulfate extracts of tissues from bovine brain regions and of the mu receptor-containing cell line SK-N-SH. Affinity-purified antipeptide antibody detected an immunoreactive protein of molecular weight 65,000 in brain regions containing high levels of mu-opioid receptors (striatum, thalamus, hippocampus, and frontal cortex) and in the cell line SK-N-SH. Pons, which contains low levels of receptors, produced a a barely detectable signal, whereas white matter, HeLa cells, and C6 glioma cells, devoid of opioid binding activity, produced no detectable signal. The correlation between immunoreactivity and the presence of mu-opioid binding in brain regions and cell lines and the correspondence of the molecular weight of the immunoreactive protein to that of mu-opioid receptors provide strong evidence that the peptide antisera recognize mu receptors.
journal_name
Mol Pharmacoljournal_title
Molecular pharmacologyauthors
Gioannini TL,Yao YH,Hiller JM,Taylor LP,Simon EJsubject
Has Abstractpub_date
1993-10-01 00:00:00pages
796-801issue
4eissn
0026-895Xissn
1521-0111journal_volume
44pub_type
杂志文章abstract::The cytotoxic efficacy of antitumor drugs targeted at DNA topoisomerase II (topo II) in many cases varies in direct proportion to cellular topo II content. To investigate the transcriptional control of the predominant alpha form of topo II, the 5' flanking region of the human topo II alpha gene (positions -562 to +90)...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1995-04-01 00:00:00
abstract::Chronic morphine treatment has been shown to produce constitutive activation of mu-opioid receptors, and this transition might contribute to the development of tolerance and dependence. The apparent ability of chronic morphine to increase the spontaneous, agonist-independent activation of mu-opioid receptors may be un...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.60.1.53
更新日期:2001-07-01 00:00:00
abstract::Beta-adrenergic receptors were characterized in a particulate fraction of human auricles obtained from patients operated upon for coronary insufficiency or valvular disease. [125I] Hydroxybenzylpindolol binding was evaluated in terms of kinetics; KD and Bmax values; and inhibition of binding in the presence of 10 micr...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1983-09-01 00:00:00
abstract::The presence and properties of the Ah receptor were examined in the guinea pig, rat, hamster, monkey, and three different strains of mice. These species and strains have demonstrated differences in sensitivity and variability of response to 2,3,7,8-tetrachlorodibenzo-p-dioxin and related compounds. All species examine...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1984-07-01 00:00:00
abstract::Cardiac-directed expression of AC6 has pronounced favorable effects on cardiac function possibly not linked with cAMP production. To determine rigorously whether cAMP generation is required for the beneficial effects of increased AC6 expression, we generated a catalytically inactive AC6 mutant (AC6mut) that has marked...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.110.067298
更新日期:2011-03-01 00:00:00
abstract::For several GPCRs, discrimination between agonism and antagonism is possible on the basis of thermodynamics parameters, such as binding enthalpy and entropy. In this study, we analyze whether agonists and antagonists can also be discriminated thermodynamically at the histamine H(1) receptor (H(1)R). Because previous s...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.109.055384
更新日期:2009-07-01 00:00:00
abstract::G protein-coupled receptor (GPCR) kinases (GRKs) play a key role in terminating signals initiated by agonist-bound GPCRs. However, chronic stimulation of GPCRs, such as that which occurs during heart failure, leads to the overexpression of GRKs and maladaptive downregulation of GPCRs on the cell surface. We previously...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.119.118661
更新日期:2020-06-01 00:00:00
abstract::Resveratrol (RES), a natural plant polyphenol, has gained interest as a nontoxic chemopreventive agent capable of inducing tumor cell death in a variety of cancer types. However, the early molecular mechanisms of RES-induced apoptosis are not well defined. Using the human breast cancer cell lines MDA-MB-231 and MCF-7,...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.107.039040
更新日期:2007-12-01 00:00:00
abstract::The binding of two anthranilic acid derivatives, glafenic and floctafenic acids, to human erythrocytes and plasma proteins has been investigated in vitro by equilibrium dialysis. Despite their close chemical structures it was shown that the binding of the two compounds to serum albumin, lipoproteins, and erythrocytes ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1987-03-01 00:00:00
abstract::The peripheral cannabinoid receptor (CB2) is a G protein-coupled receptor that is both positively and negatively coupled to the mitogen-activated protein kinase (MAPK) and cAMP pathways, respectively, through a Bordetella pertussis toxin-sensitive G protein. CB2 receptor-transfected Chinese hamster ovary cells exhibit...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1999-03-01 00:00:00
abstract::There are now several examples of single G protein-coupled receptors to which binding of specific agonists causes differential effects on the associated signaling pathways. The dopamine D(2) receptor is of special importance because the selective activation of functional pathways has been shown both in vitro and in si...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.66.1.97
更新日期:2004-07-01 00:00:00
abstract::2-Methyl-2-nitrosopropane (MNP) has long been known to undergo photochemical and thermal decomposition, generating di-tert-butyl nitroxide, in organic solvent. The present study was undertaken to demonstrate that MNP can be used as a caged-nitric oxide (NO), which can liberate NO upon illumination. Photolysis of MNP l...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1994-10-01 00:00:00
abstract::Electrical recordings were made in Xenopus oocytes to study the modulatory effects of steroids on gamma-aminobutyric acid (GABA) receptors expressed by RNA from mammalian brain and retina. GABA responses expressed by rat cerebral cortex poly(A)+ RNA were bicuculline-sensitive Cl- currents mediated by GABAA receptors. ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1992-01-01 00:00:00
abstract::5-Hydroxytryptamine3 (5-HT3) receptors are ligand-gated ion channels that mediate neurotransmission by serotonin in the central nervous system. Pharmacological inhibition of 5-HT3 receptor activity has therapeutic potential in several psychiatric diseases, including depression and anxiety. The recently approved multim...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.118.113530
更新日期:2018-12-01 00:00:00
abstract::The efficacy of antineoplastic compounds can depend heavily on the genetic background of the cells exposed to the drugs. This becomes evident by the fact that HT-29 human colon cancer cells but not primary murine nontransformed colonocytes are efficiently submitted to apoptosis by the flavonoid flavone. By determining...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.64.6.1494
更新日期:2003-12-01 00:00:00
abstract::The gonadotropin-releasing hormone receptor (GnRH-R) of the African catfish couples to phospholipase C and belongs to the large family of G protein-coupled receptors. We recently demonstrated that removal of the carboxyl-terminal tail (S331-Q379) from the catfish GnRH-R results in a loss of agonist binding; the curren...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.56.6.1229
更新日期:1999-12-01 00:00:00
abstract::Na+-d-glucose cotransporter 1 (SGLT1) is rate-limiting for glucose absorption in the small intestine. Shortly after intake of glucose-rich food, SGLT1 abundance in the luminal membrane of the small intestine is increased. This upregulation occurs via glucose-induced acceleration of the release of SGLT1-containing vesi...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.116.104521
更新日期:2016-11-01 00:00:00
abstract::The anticancer agent 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO) and its methyl ester (CDDO-Me) typically induce a broad spectrum of growth-inhibitory, proapoptotic, and antiangiogenic responses. Treatment of Panc1, Panc28, and L3.6pL pancreatic cancer cells with low micromolar concentrations of CDDO or CDDO-...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.110.064451
更新日期:2010-08-01 00:00:00
abstract::Extracellular ATP activates two distinct types of P2 purinoreceptor-mediated signaling pathways in macrophages, 1) the rapid formation of nonselective pores/channels in the plasma membrane and 2) a guanine nucleotide-binding protein-dependent stimulation of phosphotidylinositol-specific phospholipase C, with subsequen...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1993-07-01 00:00:00
abstract::Chronic stimulation of beta-adrenoceptors leads to increased mRNA and protein levels of pertussis toxin (PTX)-sensitive guanine nucleotide-binding proteins (G proteins) in the heart. In the present study the time course is reported of the effect of isoprenaline infusions on myocardial mRNA levels of Gi alpha-2, Gi alp...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1992-11-01 00:00:00
abstract::The ability of four antidepressant drugs, imipramine, alaproclate, norzimelidine, and fluvoxamine, to inhibit serotonin transport into platelet plasma membrane vesicles was tested over a range of external Na+ concentrations. Imipramine affinity, as we previously reported [J. Biol. Chem. 258:6115-6119 (1983)] increases...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1988-06-01 00:00:00
abstract::Previous studies have demonstrated that the quinone group may play an important role in modulating the alkylating activity of quinone alkylating agents. Introduction of a quinone moiety markedly increased the alkylating activity and cytotoxic activity of the model quinone alkylating agents benzoquinone mustard and ben...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1991-09-01 00:00:00
abstract::Ryanodine receptors (RyRs) are intracellular membrane channels playing key roles in many Ca(2+) signaling pathways and, as such, are emerging novel therapeutic and insecticidal targets. RyRs are so named because they bind the plant alkaloid ryanodine with high affinity and although it is established that ryanodine pro...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.114.093757
更新日期:2014-09-01 00:00:00
abstract::Arrestins mediate G protein-coupled receptor desensitization, internalization, and signaling. Dopamine D(2) and D(3) receptors have similar structures but distinct characteristics of interaction with arrestins. The goals of this study were to compare arrestin-binding determinants in D(2) and D(3) receptors other than ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.108.050534
更新日期:2009-01-01 00:00:00
abstract::Angiotensin II (AII) stimulates rapid increases in cytosolic Ca2+ concentrations in Xenopus laevis oocytes after binding to specific receptors located in the surrounding follicular cells. In follicular oocytes, the peptide AII receptor antagonists saralasin (IC50 = 25 nM) and CGP 42112A (IC50 = 400 nM) were orders of ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1991-02-01 00:00:00
abstract::We show here that arsenite (As(3+)) elicits multiple effects on gene control, such as the interruption of cell cycle control by initiating G(2)/M arrest as well as inhibiting the aryl hydrocarbon (Ah) receptor-mediated 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-inducible expression of CYP1A1. This raises the question ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.104.006130
更新日期:2005-04-01 00:00:00
abstract::ATP-binding cassette (ABC) membrane proteins comprise a superfamily of transporters with a wide variety of substrates. Humans have 49 members in this superfamily. Several human ABC transporters, such as ABCB1 and ABCC1, have been attributed to cause multidrug resistance (MDR) in cancer treatment when over-expressed. I...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.105.011015
更新日期:2005-08-01 00:00:00
abstract::Norcocaine nitroxide and N-hydroxynorcocaine were found to stimulate hepatic microsomal lipid peroxidation in vitro, as measured by spin-trapping techniques using the spin trap alpha-[4-pyridyl-1-oxide]-N-tert-butylnitrone. It was determined that either norcocaine nitroxide or N-hydroxynorcocaine markedly enhanced the...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1982-11-01 00:00:00
abstract::The anti-human immunodeficiency virus (-HIV) nucleoside analogs azidothymidine (AZT), dideoxycytidine (ddC), dideoxyinosine (ddl), dideoxydidehydrothymidine (D4T), and dideoxydidehydrocytidine (D4C) and the anticancer drug cytosine arabinoside (AraC) were compared for their effects on the mitochondrial DNA (mtDNA) con...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1991-05-01 00:00:00
abstract::The Integrated Stress Response (ISR) is a signaling program that enables cellular adaptation to stressful conditions like hypoxia and nutrient deprivation in the tumor microenvironment. An important effector of the ISR is activating transcription factor 4 (ATF4), a transcription factor that regulates genes involved in...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.112.081810
更新日期:2013-03-01 00:00:00