Abstract：
:The cDNAs for the four murine aryl hydrocarbon (Ah) receptor alleles were cloned and sequenced, and the deduced amino acid sequences were compared. The Ahb-1 allele encodes a protein of 805 amino acids, the Ahd and Ahb-2 alleles encode proteins of 848 amino acids, and the Ahb-3 allele encodes a protein of 883 amino acids. The alleles differ by eight point mutations in the common open reading frame (the initial 805 amino acids) and by additional sequences at the carboxyl end. The amino halves of the proteins, containing a spliced leader sequence, a basic helix-loop-helix motif, and two 50-amino acid repeats (PAAS), have identical sequences except for a single amino acid change in the second PAAS box. The Ahd allele, which has a lower ligand binding affinity, differs from the Ahb-2 receptor by only two amino acids. Mutagenesis experiments with these cloned cDNAs, using in vitro transcription and translation and 2-[125I]iodo-7,8-dibromodibenzo-p-dioxin binding, indicate that the low ligand binding affinity of the Ahd allele is attributable to a valine at residue 375; changing this amino acid to an alanine, as in the Ahb-2 protein, enhances the affinity 4-fold. For in vitro translated Ahb-1 and Ahb-2 alleles the Kd values were approximately 6-10 pM and for Ahd the Kd value was approximately 37 pM. Using 5' truncation and mutations to produce 3' translation truncation sites, we mapped the ligand binding region for the Ahb-1 allele.
journal_name
Mol Pharmacoljournal_title
Molecular pharmacologyauthors
Poland A,Palen D,Glover Esubject
Has Abstractpub_date
1994-11-01 00:00:00pages
915-21issue
5eissn
0026-895Xissn
1521-0111journal_volume
46pub_type
杂志文章abstract：:N-formyl peptide receptor (FPR1) and N-formyl peptide receptor-like 1 (FPRL1, now known as FPR2) are G protein-coupled receptors involved in host defense and sensing cellular dysfunction. Because of the potential for FPR1/FPR2 as a therapeutic target, our recent high-throughput screening efforts have focused on the id...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.109.060673
更新日期：2010-02-01 00:00:00
abstract：:The cis and trans isomers of the photoisomerizable compound, 3,3'-bis-[alpha-(trimethylammonium)methyl]azobenzene (Bis-Q), were purified by high-performance liquid chromatography using the ion-pair partitioning technique on a reverse-phase column. Solutions of cis-Bis-Q are stable at -20 degrees; at 25 degrees, therma...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1983-03-01 00:00:00
abstract：:The aryl hydrocarbon receptor (AHR) binds planar aromatic compounds and up-regulates the transcription of a battery of xenobiotic-metabolizing enzymes. To identify proteins involved in the biosynthesis of endogenous AHR ligands, we screened extracts of various mouse tissues for AHR signaling activity. We found heart e...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.64.3.550
更新日期：2003-09-01 00:00:00
abstract：:Nafazatrom, an antithrombotic and antimetastatic agent containing a pyrazolone functionality, is a reducing substrate for the peroxidase activity of prostaglandin H (PGH) synthase. Nafazatrom inhibits the hydroperoxide-dependent oxidation of phenylbutazone, stimulates the reduction of 15-hydroperoxy-5,8,11,13-eicosate...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1984-09-01 00:00:00
abstract：:Hypertriglyceridemia is a frequent complication accompanying the treatment of patients with either retinoids or rexinoids, [retinoid X receptor (RXR)-selective retinoids]. To investigate the cellular and molecular basis for this observation, we have studied the effects of rexinoids on triglyceride metabolism in both n...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.59.2.170
更新日期：2001-02-01 00:00:00
abstract：:CC and CXC chemokines coinduced in fibroblasts and leukocytes by cytokines and microbial agents determine the number of phagocytes infiltrating into inflamed tissues. Interleukin-8/CXCL8 and stromal cell-derived factor-1/CXCL12 significantly and dose-dependently increased the migration of monocytes, expressing the cor...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.108.045146
更新日期：2008-08-01 00:00:00
abstract：:This article describes the expected phenotypic behavior of all types of ligands in constitutively active receptor systems and, in particular, the molecular mechanisms of inverse agonism. The possible physiological relevance of inverse agonism also is discussed. Competitive antagonists with the molecular property of ne...
journal_title：Molecular pharmacology
pub_type： 杂志文章,评审
doi：10.1124/mol.65.1.2
更新日期：2004-01-01 00:00:00
abstract：:The diphosphoinositol polyphosphates ("inositol pyrophosphates") are a specialized subgroup of the inositol phosphate signaling family. This review proposes that many of the current data concerning the metabolic turnover and biological effects of the diphosphoinositol polyphosphates are linked by a common theme: these...
journal_title：Molecular pharmacology
pub_type： 杂志文章,评审
doi：10.1124/mol.109.055897
更新日期：2009-08-01 00:00:00
abstract：:A novel cloned polymorphism of the human concentrative nucleoside transporter hCNT3 was described and functionally characterized. This variant consists of a T/C transition leading to the substitution of cysteine 602 by an arginine residue in the core of transmembrane domain 13. The resulting hCNT3(C602R) protein has t...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.107.041848
更新日期：2008-02-01 00:00:00
abstract：:The cDNA for the rat alpha 1c-adrenergic receptor (AR) has been cloned using a probe derived from the bovine alpha 1c-AR sequence. Clone rB7a has a 2.6-kilobase insert with a 1390-base pair open reading frame and encodes a receptor of 466 amino acids. The cloned receptor has 91% amino acid identity with the bovine alp...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1994-09-01 00:00:00
abstract：:Bovine adrenal zona fasciculata (AZF) cells express a noninactivating K+ current (IAC) that sets the resting membrane potential and may mediate depolarization-dependent cortisol secretion. External ATP stimulates cortisol secretion through activation of a nucleotide receptor. In whole-cell patch clamp recordings from ...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.55.2.364
更新日期：1999-02-01 00:00:00
abstract：:In cells expressing both the insulin receptor isoform A (IRA) and the insulin-like growth factor-1 receptor (IGF1R), the presence of hybrid receptors, made up of an alphabeta-IRA chain associated with an alphabeta-IGF1R chain, has been demonstrated. These heterodimers are found in normal cells, and they also seem to p...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.106.026989
更新日期：2006-11-01 00:00:00
abstract：:In previous studies, it was shown that the overexpression of beta2-adrenoceptor (beta2AR) in the hearts of transgenic mice (Tg) leads to agonist-independent activation of adenylate cyclase and enhanced myocardial function. Here, we measured the physical coupling of beta2AR and Gs by evaluating the coimmunoprecipitatio...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.52.2.187
更新日期：1997-08-01 00:00:00
abstract：:Voltage-gated sodium channels are inhibited by many local anesthetics, antiarrhythmics, and antiepileptic drugs. The local anesthetic lidocaine appears to be able to access its binding site in the sodium channel only from the membrane phase or from the internal face of the channel. In contrast, the antiepileptic drug ...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.113.090472
更新日期：2014-02-01 00:00:00
abstract：:Tumor necrosis factor α (TNFα) plays a vital role in cancer progression as it is associated with inflammation and promotion of cancer angiogenesis and metastasis. The effects of TNFα are mediated by its downstream target, the oncogene lysine-rich CEACAM1 coisolated protein (LYRIC, also known as metadherin or astrocyte...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.116.107870
更新日期：2017-05-01 00:00:00
abstract：:By limiting unrestricted activation of intracellular effectors, compartmentalised signalling of cyclic nucleotides confers specificity to extracellular stimuli and is critical for the development and health of cells and organisms. Dissecting the molecular mechanisms that allow local control of cyclic nucleotide signal...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.119.118869
更新日期：2020-02-28 00:00:00
abstract：:The effect of the neuromuscular blocker alcuronium on the binding of N-[3H]-methylscopolamine [( 3H]NMS) and l-[3H]quinuclidinylbenzilate ([3H]QNB) to muscarinic binding sites in rat heart atria, longitudinal smooth muscle of the ileum, cerebral cortex, cerebellum, and submaxillary glands was measured using filtration...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1990-11-01 00:00:00
abstract：:The expression and molecular regulation of the cytochrome P450IA (P450IA) gene subfamily have been examined in rat hepatic tissue after treatment with pyridine. The microsomal ethoxyresorufin O-deethylase activity, which has been shown to be specific for the P450IA subfamily, was increased approximately 2- and 3.5-fol...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1991-07-01 00:00:00
abstract：:The anti-arrhythmic quinidine has been reported to be a competitive inhibitor of the catalytic activities of human liver P-450DB, including sparteine delta 2-oxidation and bufuralol 1'-hydroxylation, and we confirmed the observation that submicromolar concentrations are strongly inhibitory. Human liver microsomes oxid...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1986-09-01 00:00:00
abstract：:Herein we provide evidence for the coexpression of two distinct prostacyclin (PGI(2)) receptors (IP) on BEAS-2B human airway epithelial cells. IP receptor heterogeneity initially was suggested by the finding that the rank orders of potency of PGI(2) and three structurally similar analogs [taprostene, iloprost, 15-deox...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.110.069674
更新日期：2011-03-01 00:00:00
abstract：:Styrylquinoline derivatives (SQ) efficiently inhibit the 3'-processing activity of integrase (IN) with IC50 values of between 0.5 and 5 microM. We studied the mechanism of action of these compounds in vitro. First, we used steady-state fluorescence anisotropy to assay the effects of the SQ derivatives on the formation...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.65.1.85
更新日期：2004-01-01 00:00:00
abstract：:SR33557 belongs to a new class of molecules (indolizinsulfones) that act on the same receptor complex that has been characterized for other classical calcium channel effectors. The main binding properties of SR33557 to rabbit skeletal muscle are as follows. (i) Unlabeled SR33557 completely inhibits the specific bindin...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1989-06-01 00:00:00
abstract：:Histone deacetylase inhibitors (HDACis) are currently in trial or are in clinical use for the treatment of a number of tumor types. The clinical efficacy of HDACis can be partly attributed to the modulation of the cell cycle by the HDACis. Here, we have examined the effects of N-(2-aminophenyl)-4-((4-pyridin-3-ylpyrim...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.110.065169
更新日期：2010-09-01 00:00:00
abstract：:Cyclic nucleotide analogs were used to study relaxation of pig coronary arteries and guinea pig tracheal smooth muscle in an attempt to determine the roles of cAMP- and cGMP-dependent protein kinases (cA-K and cG-K). In pig coronary artery strips, cGMP analogs were generally more effective than cAMP analogs in promoti...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1988-10-01 00:00:00
abstract：:Monoclonal antibodies specific for cytochromes P-450 induced by 3-methylcholanthrene (Mab 1-7-1) and phenobarbital (Mab 2-66-3) have been used in an unlabeled peroxidase-antiperoxidase immunohistochemical procedure to investigate the intralobular distribution and induction sites of the hemoproteins within the livers o...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1988-12-01 00:00:00
abstract：:The new olivacine derivative S16020-2 (NSC-659687) is a DNA topoisomerase II inhibitor endowed with a remarkable antitumor activity against various experimental tumors. In vitro physicochemical properties of this compound, in particular its interaction with DNA and DNA topoisomerase II, were very similar to those of e...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.58.4.709
更新日期：2000-10-01 00:00:00
abstract：:In the last years, reactive oxygen species (ROS) have been proposed as mediators of proliferative/hypertrophic responses to angiotensin II (Ang II), both in vivo and in vitro. However, the hypothesis that the Ang II-dependent cell contraction could be mediated by ROS, particularly H2O2, has not been tested. Present ex...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.59.1.104
更新日期：2001-01-01 00:00:00
abstract：:Lysosomes degrade cellular proteins and organelles and regulate cell signaling by providing a surface for the formation of critical protein complexes, notably molecular target of rapamycin (mTOR) complex 1 (mTORC1). Striking differences in the lysosomes of cancer versus normal cells suggest that they could be targets ...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.118.113118
更新日期：2019-01-01 00:00:00
abstract：:To understand the molecular mechanism by which the angiotensin II (AII) type 1 receptor (AT1 receptor) transduces its biological signal, we examined the role of various signaling molecules involved in AT1 receptor signaling in Chinese hamster ovary cells stably transfected with the AT1 receptor. AT1 receptor-transfect...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：
更新日期：1996-09-01 00:00:00
abstract：:We previously demonstrated that murine bone marrow stromal cells express high levels of cytochrome P4501B1 (CYP1B1) that metabolizes 7,12-dimethylbenza[a]anthracene (DMBA), and that DMBA activates the Ah receptor (AhR) in these cells in vitro. More recently, we reported that CYP1B1 is required for DMBA-induced lymphob...
journal_title：Molecular pharmacology
pub_type： 杂志文章
doi：10.1124/mol.56.6.1317
更新日期：1999-12-01 00:00:00
