Abstract:
:[This corrects the article on p. 21 in vol. 81, PMID: 21984254.].
journal_name
Mol Pharmacoljournal_title
Molecular pharmacologyauthors
doi
10.1124/mol.115.075234errsubject
Has Abstractpub_date
2016-01-01 00:00:00pages
214issue
1eissn
0026-895Xissn
1521-0111pii
MOL_075234errjournal_volume
89pub_type
已发布勘误abstract::Previous studies showed that lapatinib and obatoclax interact in a greater-than-additive fashion to cause cell death and do so through a toxic form of autophagy. The present studies sought to extend our analyses. Lapatinib and obatoclax killed multiple tumor cell types, and cells lacking phosphatase and tensin homolog...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.112.081539
更新日期:2012-12-01 00:00:00
abstract::The members of the Cys-loop ligand-gated ion channel (LGIC) gene family play a major role in fast synaptic transmission, and these receptors represent an important class of targets for therapeutic agents. Each member of this gene family is a pentameric complex containing one or more different subunits, and a large num...
journal_title:Molecular pharmacology
pub_type: 评论,杂志文章,评审
doi:10.1124/mol.105.020727
更新日期:2006-02-01 00:00:00
abstract::1-[6-[[(17beta)-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione (U73122) is widely used to inhibit phospholipase C (PLC)-mediated signaling, but we and others have also reported a PLC-independent block of Kir3 channels in native cells. To elaborate on this major side effect, we examined the acti...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.108.047837
更新日期:2008-11-01 00:00:00
abstract::Recently, inositol hexakisphosphate (phytic acid) was shown to bind to photoreceptor arrestin and block its interaction with rhodopsin. Such an interaction might predict that inositol polyphosphates could alter G protein-coupled receptor desensitization. To investigate the possible roles of higher inositol polyphospha...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1994-08-01 00:00:00
abstract::To identify novel factors or mechanisms that are important for the resistance of tissues to chemical toxicity, we have determined the mechanisms underlying the previously observed increases in resistance to acetaminophen (APAP) toxicity in the lateral nasal gland (LNG) of the male Cyp2g1-null/Cyp2a5-low mouse. Initial...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.110.070045
更新日期:2011-04-01 00:00:00
abstract::The chemical reaction of 1,4-benzoquinone with glutathione results in the formation of adducts that exhibit increasing degrees of glutathione substitution. Purification of these adducts and analysis by 1H and 13C nuclear magnetic resonance spectroscopy revealed the products of the reaction to be 2-(glutathion-S-yl)hyd...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1988-12-01 00:00:00
abstract::The availability of high-affinity agonists for peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) has led to significant advances in our understanding of the functional role of PPARbeta/delta. In this study, a new PPARbeta/delta antagonist, 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethy...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.110.065508
更新日期:2010-09-01 00:00:00
abstract::Smad4, a key transcription factor in the transforming growth factor-β signaling pathway, is involved in a variety of cell physiologic and pathologic processes. Here, we characterized megakaryocyte/platelet-specific Smad4 deficiency in mice to elucidate its effect on platelet function. We found that megakaryocyte/plate...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.116.107417
更新日期:2017-09-01 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::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 delta family of ionotropic glutamate receptors consists of glutamate delta-1 (GluD1) and glutamate delta-2 receptors. We have previously shown that GluD1 knockout mice exhibit features of developmental delay, including impaired spine pruning and switch in the N-methyl-D-aspartate receptor subunit, which are releva...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.116.104786
更新日期:2016-08-01 00:00:00
abstract::The flexible dopamine (DA) molecule exists in one or the other of its two conformational extremes (alpha- or beta-rotamer) and its receptor in the anterior pituitary gland exists in a high and a low affinity state. A series of novel, rigid DA congeners (2-substituted octahydrobenzo[f]quinolines) was synthesized and us...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1988-01-01 00:00:00
abstract::The tetrapeptide Arg-Leu-Tyr-Glu (RLYE), a vascular endothelial growth factor (VEGF) receptor-2 antagonist, has been used previously either alone or in combination with chemotherapeutic drugs for treating colorectal cancer in a mouse model. We analyzed the half-life of the peptide and found that because of degradation...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.119.117234
更新日期:2019-12-01 00:00:00
abstract::The ligand specificity of rat adenohypophyseal vasopressin receptors was directly compared to that of peripheral receptors of the V1 and V2 types. For this purpose a series of 15 recently designed vasopressin antagonists was used. The affinities of these antagonists for rat adenohypophyseal membranes were deduced from...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1986-08-01 00:00:00
abstract::Anthracyclines are effective anticancer agents. However, their use is limited by cardiotoxicity, an effect linked to their ability to chelate iron and to perturb iron metabolism (Mol Pharmacol 68:261-271, 2005). These effects on iron-trafficking remain poorly understood, but they are important to decipher because trea...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.107.041335
更新日期:2008-03-01 00:00:00
abstract::The in vitro binding of [3H]LY354740, the first high affinity group II-selective metabotropic glutamate (mGlu) receptor radioligand, was characterized in rat cortical, hippocampal, and thalamic membranes as well as in rat brain sections. [3H]LY354740 binding was saturable in all regions investigated. Nonspecific bindi...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1998-02-01 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::The class Frizzled (FZD) or class F of G protein-coupled receptors consists of 10 FZD paralogues and Smoothened (SMO). FZDs coordinate wingless/Int-1 signaling and SMO mediates Hedgehog signaling. Class F receptor signaling is intrinsically important for embryonic development and its dysregulation leads to diseases, i...
journal_title:Molecular pharmacology
pub_type: 杂志文章,评审
doi:10.1124/mol.119.117986
更新日期:2020-02-01 00:00:00
abstract::The aim of this study was to use pharmacological inhibition of protein kinase A and mutation of potential protein kinase A phosphorylation sites to determine the role of protein kinase A-catalyzed phosphorylation of the dopamine D(1) receptor in agonist-stimulated desensitization and internalization of the receptor. T...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.61.4.806
更新日期:2002-04-01 00:00:00
abstract::In rat pancreatic zymogen granules (ZG), an ATP-sensitive K(+) conductance and a Cl(-) conductance have been characterized that are inversely regulated by an approximately 65-kDa multidrug resistance P-glycoprotein (mdr1) gene product. In search of a label for purification of this protein, we found that the dihydropyr...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:2000-02-01 00:00:00
abstract::We recently reported the cloning of a novel alpha 1-adrenergic receptor (AR), the alpha 1CAR. By transient and stable expression of the alpha 1CAR and the previously cloned alpha 1BAR in COS-7 and HeLa cells, respectively, we have now compared their ability to interact with major signal-transduction pathways (includin...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1991-11-01 00:00:00
abstract::The highly conserved aspartate residue in the second transmembrane domain of G protein-coupled receptors is present in position 113 in the type 1 neurotensin receptor (NTR1) but is replaced by an Ala residue in position 79 in the type 2 neurotensin receptor (NTR2). NTR1 couples to Galphaq to stimulate phospholipase C ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.55.2.210
更新日期:1999-02-01 00:00:00
abstract::Adenosine receptors of the A1 and A2 subtypes were characterized in membranes from DDT1 MF-2 smooth muscle cells. These cells possess a high density of A1 adenosine receptors (Bmax = 0.8-0.9 pmol/mg of protein), as measured by both agonist and antagonist radioligands. Agonists compete for [125I]N6-[2-(4-amino-3-iodoph...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1990-02-01 00:00:00
abstract::The alpha2-adrenergic receptors (alpha2-ARs) mediate signals to intracellular second messengers via guanine nucleotide binding proteins. Three human genes encoding alpha2-AR subtypes (alpha2A, alpha2B, alpha2C) have been cloned. Several chemical compounds display subtype differences in their binding and/or functional ...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.53.3.370
更新日期:1998-03-01 00:00:00
abstract::G protein-coupled receptor kinases (GRKs) play a key role in the process of receptor homologous desensitization. In the present study, we address the question of whether a variety of receptors coupled to different G protein subtypes and naturally expressed on the same cell are selectively regulated by GRK2. The signal...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.56.2.316
更新日期:1999-08-01 00:00:00
abstract::Autophagy is a response of cancer cells to various anticancer therapies. It is designated as programmed cell death type II and characterized by the formation of autophagic vacuoles in the cytoplasm. The Akt/mammalian target of rapamycin (mTOR)/p70 ribosomal protein S6 kinase (p70S6K) and the extracellular signal-regul...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.106.033167
更新日期:2007-07-01 00:00:00
abstract::Metabotropic glutamate receptor 5 (mGlu5) is a target for the treatment of central nervous system (CNS) disorders, such as schizophrenia and Alzheimer's disease. Furthermore, mGlu5 has been shown to play an important role in hippocampal synaptic plasticity, specifically in long-term depression (LTD) and long-term pote...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:10.1124/mol.112.082891
更新日期:2013-04-01 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::The interaction of hormones acting via the mobilization of calcium and stimulation of cAMP levels in cells was examined by determining the effects of carbachol and forskolin on cAMP and cGMP accumulation in mouse parotid gland. Treatment of isolated acini with either carbachol (0.01 to 20 microM) or forskolin (1 micro...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1990-10-01 00:00:00
abstract::An investigation of the conformational profiles of two cyclic delta-selective opioid peptides, [D-Pen2,D-Pen5]-enkephalin and [D-Pen2,L-Pen5]-enkephalin, has been made. The methods and procedures used are more extensive and systematic than those previously reported, involving a combination of nested grid rotations, cy...
journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1991-04-01 00:00:00