Discovery of an ectopic activation site on the M(1) muscarinic receptor.

abstract：:Mutations that inhibit Kv11.1 ion channel activity contribute to abnormalities of cardiac repolarization that can lead to long QT2 (LQT2) cardiac arrhythmias and sudden death. However, for most of these mutations, nothing is known about the molecular mechanism linking Kv11.1 malfunction to cardiac death. We have previ...

journal_title：Molecular pharmacology

authors： Donovan AJ,Lansu K,Williams JG,Denning MF,Gentile S

更新日期：2012-09-01 00:00:00

abstract：:The involvement of mitogen-activated protein (MAP) kinases in the mitogenic effect of thyrotropin (TSH) is not fully elucidated. In FRTL-5 cells, we found that the MAP kinase kinase (MEK) inhibitors UO126 and PD98059 substantially decreased TSH-induced DNA synthesis, indicating that MAP kinases are involved in the TSH...

journal_title：Molecular pharmacology

authors： Iacovelli L,Capobianco L,Salvatore L,Sallese M,D'Ancona GM,De Blasi A

更新日期：2001-11-01 00:00:00

abstract：:Our laboratory recently isolated and sequenced cDNAs encoding the microsomal flavin-containing monooxygenases (FMOs) from rabbit liver and rabbit lung. As a first step in understanding the molecular bases for the catalytic and physical differences between these enzymes, we have expressed them in COS-1 cells and compar...

journal_title：Molecular pharmacology

authors： Lawton MP,Kronbach T,Johnson EF,Philpot RM

更新日期：1991-11-01 00:00:00

abstract：:The rat mu-opioid receptor clone in which novel exon 5 was found in the place of exon 4 (MOR-1B) was one of the first MOR-1 variants described. We now have identified the mouse homolog of the rat MOR-1B as well as four additional variants derived from splicing from exon 3 into different sites within exon 5. The sequen...

journal_title：Molecular pharmacology

authors： Pan YX,Xu J,Bolan E,Moskowitz HS,Xu M,Pasternak GW

更新日期：2005-09-01 00:00:00

abstract：:Valproic acid (VPA) is an effective antiepileptic drug with an additional activity for the treatment of bipolar disorder. It has been assumed that both activities arise from a common target. At the molecular level, VPA targets a number of distinct proteins that are involved in signal transduction. VPA inhibition of in...

journal_title：Molecular pharmacology

authors： Shimshoni JA,Dalton EC,Jenkins A,Eyal S,Ewan K,Williams RS,Pessah N,Yagen B,Harwood AJ,Bialer M

更新日期：2007-03-01 00:00:00

abstract：:The use of classic antipsychotic drugs is limited by the occurrence of extrapyramidal motor symptoms, which are caused by dopamine (DA) receptor blockade in the neostriatum. We examined the impact of early-life stress on haloperidol-induced catalepsy using the rat model of prenatal restraint stress (PRS). Adult "PRS r...

journal_title：Molecular pharmacology

authors： Marrocco J,Mairesse J,Bucci D,Lionetto L,Battaglia G,Consolazione M,Ravasi L,Simmaco M,Morley-Fletcher S,Maccari S,Nicoletti F

更新日期：2013-08-01 00:00:00

abstract：:Advances in proteomic methodologies based on quantitative mass spectrometry are now transforming pharmacology and experimental biology more broadly. The present review will discuss several examples, based on work in the author's laboratory that focuses on delineating relationships between GPCR signaling and traffickin...

journal_title：Molecular pharmacology

authors： von Zastrow M

更新日期：2020-12-22 00:00:00

abstract：:Seven transmembrane G protein-coupled receptors (GPCRs) are often phosphorylated at the C terminus and on intracellular loops in response to various extracellular stimuli. Phosphorylation of GPCRs by GPCR kinases and certain other kinases can promote the recruitment of arrestin molecules. The arrestins critically regu...

journal_title：Molecular pharmacology

authors： Yang Z,Yang F,Zhang D,Liu Z,Lin A,Liu C,Xiao P,Yu X,Sun JP

更新日期：2017-09-01 00:00:00

abstract：:Enzalutamide is a potent second-generation androgen receptor (AR) antagonist with activity in metastatic castrate-resistant prostate cancer (CRPC). Although enzalutamide is initially effective, disease progression inevitably ensues with the emergence of resistance. Intratumoral hypoxia is also associated with CRPC pro...

journal_title：Molecular pharmacology

authors： Fernandez EV,Reece KM,Ley AM,Troutman SM,Sissung TM,Price DK,Chau CH,Figg WD

更新日期：2015-06-01 00:00:00

abstract：:The action of tetrahydroaminoacridine (THA), a centrally active cholinesterase inhibitor that may provide symptomatic benefit in Alzheimer's disease, was studied on responses to the excitatory amino acid N-methyl-D-aspartate (NMDA) in cultured hippocampal neurons, using whole-cell voltage-clamp and single-channel reco...

journal_title：Molecular pharmacology

authors： Hershkowitz N,Rogawski MA

更新日期：1991-05-01 00:00:00

abstract：:Previous studies have shown that the transcription factor signal transducer and activator of transcription-3 (STAT3) in podocytes plays an important role in progression of HIV nephropathy and in collapsing forms of glomerulonephritis. Here, we have observed that application of 100 nM angiotensin II (Ang II) to culture...

journal_title：Molecular pharmacology

authors： Abkhezr M,Dryer SE

更新日期：2014-08-01 00:00:00

abstract：:The growth of Plasmodium falciparum, a human malaria parasite, is sensitive to inhibition by chelators of several types. The alkylthiocarbamates and 8-hydroxyquinoline at pharmacologic doses selectively inhibit glycolysis within 6 hr in parasitized erythrocytes. The mechanism attributed to these agents is through the ...

journal_title：Molecular pharmacology

authors： Scheibel LW,Stanton GG

更新日期：1986-10-01 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

authors： Marjamaki A,Pihlavisto M,Cockcroft V,Heinonen P,Savola JM,Scheinin M

更新日期：1998-03-01 00:00:00

abstract：:Supplemental oxygen therapy is frequently used in the treatment of pulmonary insufficiency, as is encountered in premature infants, and in patients with acute respiratory distress syndrome. However, hyperoxia causes lung damage in experimental animals and may do so in humans. Cytochrome P4501A enzymes have been implic...

journal_title：Molecular pharmacology

authors： Couroucli XI,Welty SE,Geske RS,Moorthy B

更新日期：2002-03-01 00:00:00

abstract：:TWIK-related K+ channel TREK1, a background leak K+ channel, has been strongly implicated as the target of several general and local anesthetics. Here, using the whole-cell and single-channel patch-clamp technique, we investigated the effect of lidocaine, a local anesthetic, on the human (h)TREK1 channel heterologousl...

journal_title：Molecular pharmacology

authors： Nayak TK,Harinath S,Nama S,Somasundaram K,Sikdar SK

更新日期：2009-10-01 00:00:00

abstract：:The regulation of the cellular distribution and intracellular signaling properties of the alpha(1B)- and alpha(1D)- adrenoceptor (alpha(1)-AR) subtypes was examined in stably transfected Rat 1 fibroblasts. In unstimulated cells, alpha(1B)-AR expression was noted primarily on the cell surface. Treatment with phenylephr...

journal_title：Molecular pharmacology

authors： McCune DF,Edelmann SE,Olges JR,Post GR,Waldrop BA,Waugh DJ,Perez DM,Piascik MT

更新日期：2000-04-01 00:00:00

abstract：:The effects of tournefolic acid B (TAB) and two ester derivatives, TAB methyl ester (TABM) and TAB ethyl ester (TABE), on N-methyl-D-aspartate (NMDA)-mediated excitotoxicity and the underlying mechanisms were investigated. Treatment with 50 microM NMDA elicited neuronal death by 48.7 +/- 5.1%, coinciding with the appe...

journal_title：Molecular pharmacology

authors： Wang CN,Pan HC,Lin YL,Chi CW,Shiao YJ

更新日期：2006-03-01 00:00:00

abstract：:We have studied the molecular mechanism by which the nuclear xenobiotic receptors pregnane X receptor (PXR) and constitutive active/androstane receptor (CAR) regulate transcription of the vitamin D(3) 24-hydroxylase (CYP24A1) gene. In the absence of vitamin D(3), PXR activates the CYP24A1 gene by directly binding to a...

journal_title：Molecular pharmacology

authors： Konno Y,Kodama S,Moore R,Kamiya N,Negishi M

更新日期：2009-02-01 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

authors： Xi R,Pun IH,Menezes SV,Fouani L,Kalinowski DS,Huang ML,Zhang X,Richardson DR,Kovacevic Z

更新日期：2017-05-01 00:00:00

abstract：:Cholinesterase inhibitors are commonly used to improve cognition and treat psychosis and other behavioral symptoms in Alzheimer's disease, Parkinson's disease, and other neuropsychiatric conditions. However, mechanisms may exist that down-regulate the synaptic response to altered cholinergic transmission, thus limitin...

journal_title：Molecular pharmacology

authors： Volpicelli-Daley LA,Hrabovska A,Duysen EG,Ferguson SM,Blakely RD,Lockridge O,Levey AI

更新日期：2003-12-01 00:00:00

abstract：:Healing of gastrointestinal mucosal lesions occurs through two processes: an early one involving cell migration and a later one in which cell division replaces lost cells. Both processes require the presence of polyamines, but the mechanism of action of these compounds is unknown. In the present study, we examined the...

journal_title：Molecular pharmacology

authors： McCormack SA,Zimmerman BJ,Israel M,Blanner P,Johnson LR

更新日期：1995-10-01 00:00:00

abstract：:Small-molecule restoration of wild-type structure and function to mutant p53 (so-called mutant reactivation) is a highly sought-after goal in cancer drug development. We previously discovered that small-molecule zinc chelators called zinc metallochaperones (ZMCs) reactivate mutant p53 by restoring zinc binding to zinc...

journal_title：Molecular pharmacology

authors： Yu X,Blanden A,Tsang AT,Zaman S,Liu Y,Gilleran J,Bencivenga AF,Kimball SD,Loh SN,Carpizo DR

更新日期：2017-06-01 00:00:00

abstract：:Previous biochemical studies have demonstrated that synergy between non-nucleoside reverse transcriptase (RT) inhibitors (NNRTI) and nucleoside RT inhibitors (NRTIs) is due to inhibition by the NNRTI of the rate at which HIV-1 RT facilitates ATP-mediated excision of NRTIs from chain-terminated template/primers (T/P). ...

journal_title：Molecular pharmacology

authors： Radzio J,Sluis-Cremer N

更新日期：2008-02-01 00:00:00

abstract：:The response of myeloid leukemia cells to treatment with 1-beta-D-arabinofuranosylcytosine (ara-C) includes activation of the c-Abl protein tyrosine kinase and the stress-activated protein kinase (SAPK). The present studies demonstrate that treatment of human U-937 leukemia cells with ara-C is associated with transloc...

journal_title：Molecular pharmacology

authors： Raina D,Mishra N,Kumar S,Kharbanda S,Saxena S,Kufe D

更新日期：2002-06-01 00:00:00

abstract：:The in vivo bioavailability of exogenous fibroblast growth factor 2 (FGF2) was studied after i.v. injection of uniformly 14C-labeled FGF2 into young rats. 14C-FGF2 was rapidly accumulated in almost all solid organs within 5 min. After 30 min, more than 65% of FGF2 was retained in liver, 4.5% in kidneys, 1.2% in spleen...

journal_title：Molecular pharmacology

authors： Colin S,Jeanny JC,Mascarelli F,Vienet R,Al-Mahmood S,Courtois Y,Labarre J

更新日期：1999-01-01 00:00:00

abstract：:Platelet-activating factor (PAF) receptor-coupled activation of phosphoinositide-specific phospholipase C (PLC) was studied in platelets that were made refractory, by short-term pretreatments, to either PAF or thrombin. Generation of [3H]inositol triphosphate ( [3H]IP3) was monitored specifically for this purpose. [3H...

journal_title：Molecular pharmacology

authors： Morrison WJ,Shukla SD

更新日期：1988-01-01 00:00:00

abstract：:Previous analyses suggested that potent aryl hydrocarbon receptor (AhR) antagonists were planar, with a lateral electron-rich center. To further define structural requirements and mechanism for antagonism, ten additional flavone derivatives were synthesized. Based on their ability to 1) compete with 2,3,7, 8-tetrachlo...

journal_title：Molecular pharmacology

authors： Henry EC,Kende AS,Rucci G,Totleben MJ,Willey JJ,Dertinger SD,Pollenz RS,Jones JP,Gasiewicz TA

更新日期：1999-04-01 00:00:00

abstract：:Rates of glucuronidation were measured at high substrate concentrations in specific zones of the liver lobule using micro-light guides placed on periportal and pericentral regions on the surface of livers from phenobarbital-treated rats. Livers were perfused with sulfate-free buffer under normoxic conditions, and fluo...

journal_title：Molecular pharmacology

authors： Conway JG,Kauffman FC,Tsukada T,Thurman RG

更新日期：1984-05-01 00:00:00

abstract：:The transient receptor potential cation channel subfamily V member 1 (TRPV1) is known as a thermosensor and integrator of inflammation-induced hyperalgesia. TRPV1 is expressed in a subpopulation of primary afferent neurons that express several different neurotransmitters. The role of the TRPV1 channel in the developme...

journal_title：Molecular pharmacology

authors： Rogoz K,Andersen HH,Kullander K,Lagerström MC

更新日期：2014-02-01 00:00:00

abstract：:Structural changes in the macromolecular targets of pharmacological agents can result in alterations in the efficacy of these agents. In previous studies, we identified a variant structural form of thymidylate synthase (TS) that is associated with relative resistance to 5-fluoro-2'-deoxyuridine, in a human colonic tum...

journal_title：Molecular pharmacology

authors： Barbour KW,Hoganson DK,Berger SH,Berger FG

更新日期：1992-08-01 00:00:00