Abstract:
:The effect of halothane on synthesis of retained and secreted proteins was investigated using isolated perfused rat livers. Anesthetic exposure rapidly inhibited synthesis of total liver proteins in a dose-dependent manner by a mechanism which appeared to involve reduced rates of both peptide chain initiation and elongation. While halothane concentrations comparable to the clinical dose resulted in small changes in protein metabolism, higher concentrations (4%) of the anesthetic had marked effects. At early time points, relative rates of albumin synthesis were unaffected by halothane, but, as anesthetic exposure was prolonged, production of albumin and of total secreted plasma proteins was inhibited more extensively than that of retained liver proteins. Thus, halothane appeared to exert differential inhibitory effects on synthesis of these two classes of liver proteins.
journal_name
Mol Pharmacoljournal_title
Molecular pharmacologyauthors
Flaim KE,Jefferson LS,McGwire JB,Rannels DEsubject
Has Abstractpub_date
1983-09-01 00:00:00pages
277-81issue
2eissn
0026-895Xissn
1521-0111journal_volume
24pub_type
杂志文章abstract::Two newly identified, overlapping (1 bp) glucocorticoid response elements (GREs) at -759 and -773 bp in the promoter of the rat phenylethanolamine N-methyltransferase (PNMT; EC 2.1.1.28) gene are primarily responsible for its glucocorticoid sensitivity, rather than the originally identified -533-bp GRE. A dose-depende...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.61.6.1385
更新日期:2002-06-01 00:00:00
abstract::Prostaglandin E(2) (PGE(2)), originally discovered as a pro-inflammatory mediator, also inhibits several chemoattractant-elicited neutrophil functions, including adhesion, secretion of cytotoxic enzymes, production of superoxide anions, and chemotaxis. In this study, we have examined the effects of PGE(2) and prostagl...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.66.2.293
更新日期:2004-08-01 00:00:00
abstract::Taxanes act by inhibiting microtubule dynamics; in this study, we have investigated mitochondria as an additional target of taxanes. We incubated isolated mitochondria in the presence of taxanes with or without stimulation of the mitochondrial respiratory state. Results showed that they rapidly induced the loss of del...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.64.1.51
更新日期:2003-07-01 00:00:00
abstract::Cyclic nucleotide phosphodiesterases (PDEs) from canine trachealis were characterized with respect to their kinetic properties, sensitivity to selective inhibitors, and subcellular distribution. Extracts from whole tissue homogenates were applied to DEAE-Sepharose anion exchange columns and eluted with a linear sodium...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1990-02-01 00:00:00
abstract::Voltage-gated potassium (Kv) channels regulate many physiological functions and represent important therapeutic targets in the treatment of several clinical disorders. Although some of these channels have been well-characterized, the study of others, such as Kv3 channels, has been hindered because of limited pharmacol...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.105.011064
更新日期:2005-05-01 00:00:00
abstract::Pyrethroid insecticides are synthetic neurotoxins patterned after the naturally occurring pyrethrins. Their mechanism of action is thought to involve effects primarily at the voltage-sensitive sodium channel of both insect and mammalian neurons, although recent studies have raised the possibility that these compounds ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1988-07-01 00:00:00
abstract::Cu/Zn-superoxide dismutase (SOD)-accelerated oxidation of the benzene metabolite 1,4-hydroquinone (HQ) results in the enhanced formation of semiquinone anion radicals, electrophilic 1,4-benzoquinone (BQ), and H202. We selected bone marrow stromal cells and phiX-174 double stranded plasmid DNA as model systems to inves...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1996-03-01 00:00:00
abstract::To study the functional role of individual alpha1-adrenergic (AR) subtypes in blood pressure (BP) regulation, we used mice lacking the alpha1B-AR and/or alpha1D-AR with the same genetic background and further studied their hemodynamic and vasoconstrictive responses. Both the alpha1D-AR knockout and alpha1B-/alpha1D-AR...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.104.007500
更新日期:2005-03-01 00:00:00
abstract::Prostate cancer is a highly heterogenous disease in which a patient-tailored care program is much desired. Central to this goal is the development of novel targeted pharmacological interventions. To develop these treatment strategies, an understanding of the integration of cellular pathways involved in both tumorigene...
journal_title:Molecular pharmacology
pub_type: 杂志文章,评审
doi:10.1124/mol.108.053066
更新日期:2009-03-01 00:00:00
abstract::The phosphorylation of μ-opioid receptors (MOPRs) by G protein-coupled receptor kinases (GRKs), followed by arrestin binding, is thought to be a key pathway leading to desensitization and internalization. The present study used the combination of intracellular and whole-cell recordings from rats and mice, as well as l...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.111.076208
更新日期:2012-03-01 00:00:00
abstract::Guanine nucleotide-binding proteins (G proteins) transduce signals from agonist- and light-sensitive receptors. In the visual excitation system, the photon receptor rhodopsin is coupled to the G protein Gt (transducin). Gt is composed of alpha, beta, and gamma subunits; the alpha subunit binds guanine nucleotide, wher...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1990-06-01 00:00:00
abstract::The decrease in mu-opioid receptor activity after chronic agonist exposure (1 microM [D-Ala(2),N-MePhe(4),Gly-ol(5)]-enkephalin) is largely due to kinase-mediated phosphorylation of intracellular receptor domains. We have recently shown that the substitution of two putative Ca(2+)/calmodulin-dependent protein kinase I...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.58.2.328
更新日期:2000-08-01 00:00:00
abstract::Molecular chaperone heat shock protein 90 (HSP90) is involved in oncogenic signaling pathways including epithelial-mesenchymal transition (EMT), a key process in tumor initiation, progression, metastasis, and chemoresistance. The molecular mechanisms underlying the involvement of HSP90 in EMT are still under investiga...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.119.116137
更新日期:2019-08-01 00:00:00
abstract::UDP-glucuronosyltransferase (UGT) 1A1 (UGT1A1) catalyzes the glucuronidation of bilirubin in liver. Among all UGT isoforms identified to date, it is the only relevant bilirubin-glucuronidating enzyme in human. Because glucuronoconjugation is the major route of bilirubin elimination, any genetic alteration that affects...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.56.3.526
更新日期:1999-09-01 00:00:00
abstract::G protein-coupled receptors are sensors that interact with a large variety of elements, including photons, ions, and large proteins. Not surprisingly, these receptors participate in the numerous normal physiologic processes that we refer to as health and in its perturbations that constitute disease. It has been estima...
journal_title:Molecular pharmacology
pub_type:
doi:10.1124/mol.116.106062
更新日期:2016-11-01 00:00:00
abstract::The hexapeptide [pGlu6,Pro9]substance P (SP)6-11, septide, has been shown to be an agonist as potent as SP in eliciting smooth muscle contraction in several in vitro preparations, while being a poor competitor of labeled SP binding. These results, as well as other pharmacological data, have suggested the existence of ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1994-02-01 00:00:00
abstract::Regulation of beta2-adrenergic receptor (beta2AR) levels by glucocorticoids is a physiologically important mechanism for altering beta2AR responsiveness. Glucocorticoids increase beta2AR density by increasing the rate of beta2AR gene transcription, but the cis-elements involved have not been well characterized. We now...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.54.6.1016
更新日期:1998-12-01 00:00:00
abstract::Camptothecin (CPT) is an effective chemotherapeutic agent for treatment of patients with cancer. The mechanisms underlying CPT-mediated responses in cancer cells are not fully understood. MicroRNA (miRNA) play important roles in tumorigenesis and drug sensitivity. However, the interaction between camptothecin and miRN...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.111.076794
更新日期:2012-04-01 00:00:00
abstract::To learn more about the binding conformation of phencyclidine (PCP) and to arrive at analogues of higher affinity, which may serve as noncompetitive N-methyl-D-aspartate receptor antagonists, eight optically pure PCP analogues were designed with the aid of computer. These compounds represent conformationally constrain...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1990-03-01 00:00:00
abstract::The phosphatidylcholine-using phospholipase D (PLD) isoform PLD2 is widely expressed in mammalian cells and is activated in response to a variety of promitogenic agonists. In this study, active and inactive hemagglutinin-tagged human PLD2 (HA-PLD2) constructs were stably expressed in an EL4 cell line lacking detectabl...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.107.040105
更新日期:2008-09-01 00:00:00
abstract::Iron is a biologically essential metal, but excess iron can cause damage to the cardiovascular and nervous systems. We examined the effects of extracellular Fe²⁺ on permeation and gating of Ca(V)3.1 channels stably transfected in HEK293 cells, by using whole-cell recording. Precautions were taken to maintain iron in t...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.112.080184
更新日期:2012-12-01 00:00:00
abstract::Transmembrane domain 6 of the muscarinic acetylcholine (ACh) receptors is important in ligand binding and in the conformational transitions of the receptor but the roles of individual residues are poorly understood. We have carried out a systematic alanine-scanning mutagenesis study on residues Tyr381 to Val387 within...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.56.5.1031
更新日期:1999-11-01 00:00:00
abstract::The blocking effects of guanethidine on electrically induced, neurally mediated, contractions of the guinea pig vas deferens in vitro could be markedly antagonized by the bee venom polypeptide apamin (20-60 nM), by 0.1 mM methylene blue, and (less regularly) by 0.1-0.15 mM quinine, three substances known to inhibit ca...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1983-03-01 00:00:00
abstract::K-252b, a member of the staurosporine family of protein kinase inhibitors, selectively potentiates the activation of the nerve growth factor receptor, TrkA, by a nonpreferred ligand, neurotrophin-3 (NT-3), in a variety of cell types. At higher (micromolar) concentrations of K-252b, an inhibitory effect occurs because ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.56.1.185
更新日期:1999-07-01 00:00:00
abstract::Allosteric modulators of G-protein-coupled receptors can regulate conformational states involved in receptor activation ( Mol Pharmacol 58: 1412-1423, 2000 ). This hypothesis was investigated for the corticotropin-releasing factor type 1 (CRF(1)) receptor using a novel series of ligands with varying allosteric effect ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.107.042978
更新日期:2008-05-01 00:00:00
abstract::Receptors for the serine protease thrombin and for lysophospholipids are coupled to G proteins and control a wide range of cellular functions, including mitogenesis. Activators of these receptors are present in blood, and can enter the brain during central nervous system (CNS) injury. Reactive astrogliosis, a prominen...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.64.5.1199
更新日期:2003-11-01 00:00:00
abstract::It has been demonstrated previously that cannabinol (CBN) differentially modulates interleukin-2 (IL-2) protein secretion by T cells with a corresponding change in extracellular signal-regulated kinase activity. The objective of the present studies was to further investigate the molecular mechanism by which CBN enhanc...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.61.2.446
更新日期:2002-02-01 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::P2X receptors are trimeric membrane proteins. When they bind extracellular ATP, a conformational change occurs that opens a transmembrane ion channel. The ATP-binding pocket is formed in a cleft between two subunits, and a critical amino acid residue for ATP contact is Lys⁶⁹ (P2X2 numbering). In the present work, we s...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.112.080903
更新日期:2012-10-01 00:00:00
abstract::Specific toxic and biochemical responses elicited by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) in human thymic epithelial (TE) cells in culture are mediated by the TCDD receptor protein. Characterization of the physicochemical properties of the TCDD receptor in cytosol fractions from cultured human TE cells indicates...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1989-05-01 00:00:00