Fusion polypeptides that inhibit exocytosis: fusing aptamer and cell-penetrating peptide technologies and pharmacologies.

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

authors： Ladefoged LK,Munro L,Pedersen AJ,Lummis SCR,Bang-Andersen B,Balle T,Schiøtt B,Kristensen AS

更新日期：2018-12-01 00:00:00

abstract：:Dysfunction of p53 and resistance to cancer drugs can arise through mutually exclusive overexpression of MDM2 or MDM4. Cisplatin-resistant cells, however, can demonstrate increased binding of both MDM2 and MDM4 to p53 but in absence of cellular overexpression. Whether MDM2 inhibitors alone can activate p53 in these re...

journal_title：Molecular pharmacology

authors： Xie X,He G,Siddik ZH

更新日期：2020-04-01 00:00:00

abstract：:The cannabinoid field is currently an active research area. Anandamide (AEA) and 2-arachidonoylglycerol (2-AG) are the most characterized endogenous cannabinoids (also known as endocannabinoids). These neuromodulators have been implicated in various physiologically relevant phenomena, including mood (Witkin et al., 20...

journal_title：Molecular pharmacology

authors： Yates ML,Barker EL

更新日期：2009-07-01 00:00:00

abstract：:Although ATP-sensitive K+ channels continue to be explored for their therapeutic potential, developments in high-affinity radioligands to investigate native and recombinant KATP channels have been less forthcoming. This study reports the identification and pharmacological characterization of a novel iodinated 1,4-dihy...

journal_title：Molecular pharmacology

authors： Davis-Taber R,Molinari EJ,Altenbach RJ,Whiteaker KL,Shieh CC,Rotert G,Buckner SA,Malysz J,Milicic I,McDermott JS,Gintant GA,Coghlan MJ,Carroll WA,Scott VE,Gopalakrishnan M

更新日期：2003-07-01 00:00:00

abstract：:α-Conotoxins are subtype-selective nicotinic acetylcholine receptor (nAChR) antagonists. Although potent α3β2 nAChR-selective α-conotoxins have been identified, currently characterized α-conotoxins show no or only weak affinity for α4β2 nAChRs, which are, besides α7 receptors, the most abundant nAChRs in the mammalian...

journal_title：Molecular pharmacology

authors： Beissner M,Dutertre S,Schemm R,Danker T,Sporning A,Grubmüller H,Nicke A

更新日期：2012-10-01 00:00:00

abstract：:In an attempt to better understand the role of the cyclohexene ring (ring A) in the biochemical and pharmacological properties of anthracyclines related to doxorubicin and daunorubicin, we investigated the effects of introduction of a fluorine atom at position 8 of idarubicin (4-demethoxydaunorubicin) on drug molecula...

journal_title：Molecular pharmacology

authors： Animati F,Arcamone F,Bigioni M,Capranico G,Caserini C,De Cesare M,Lombardi P,Pratesi G,Salvatore C,Supino R,Zunino F

更新日期：1996-09-01 00:00:00

abstract：:The bisdioxopiperazines such as (+)-(S)-4,4'-propylenedi-2,6-piperazinedione (dexrazoxane; ICRF-187), 1,2-bis(3,5-dioxopiperazin-1-yl)ethane (ICRF-154), and 4,4'-(1,2-dimethyl-1,2-ethanediyl)bis-2,6-piperazinedione (ICRF-193) are agents that inhibit eukaryotic topoisomerase II, whereas their ring-opened hydrolysis pro...

journal_title：Molecular pharmacology

authors： Grauslund M,Thougaard AV,Füchtbauer A,Hofland KF,Hjorth PH,Jensen PB,Sehested M,Füchtbauer EM,Jensen LH

更新日期：2007-10-01 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：:The compound 4-(5-(4-bromophenyl)-3-(6-methyl-2-oxo-4-phenyl-1,2-dihydroquinolin-3-yl)-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoic acid (DQP-1105) is a representative member of a new class of N-methyl-d-aspartate (NMDA) receptor antagonists. DQP-1105 inhibited GluN2C- and GluN2D-containing receptors with IC(50) values ...

journal_title：Molecular pharmacology

authors： Acker TM,Yuan H,Hansen KB,Vance KM,Ogden KK,Jensen HS,Burger PB,Mullasseril P,Snyder JP,Liotta DC,Traynelis SF

更新日期：2011-11-01 00:00:00

abstract：:The 90-kDa heat shock family (HSP90) of protein and two-component histidine kinases, although quite distinct at the primary amino acid sequence level, share a common structural ATP-binding domain known as the Bergerat fold. The Bergerat fold is important for the ATPase activity and associated chaperone function of HSP...

journal_title：Molecular pharmacology

authors： Besant PG,Lasker MV,Bui CD,Turck CW

更新日期：2002-08-01 00:00:00

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 ac...

journal_title：Molecular pharmacology

authors： Poland A,Palen D,Glover E

更新日期：1994-11-01 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

authors： Pupo AS,García-Sáinz JA

更新日期：2016-11-01 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

abstract：:The intracellular pathways taken by galactose-terminal glycoproteins were examined following endocytosis by the asialoglycoprotein receptor in monolayers of the human hepatoma cell line, Hep G2. In addition to a pathway leading to lysosomal degradation, single cohort kinetics revealed that up to 28% of surface-bound a...

journal_title：Molecular pharmacology

authors： Simmons CF Jr,Schwartz AL

更新日期：1984-11-01 00:00:00

abstract：:Effects of pimaric acid (PiMA) and eight closely related compounds on large-conductance K(+) (BK) channels were examined using human embryonic kidney (HEK) 293 cells, in which either the alpha subunit of BK channel (HEKBKalpha) or both alpha and beta1 (HEKBKalphabeta1) subunits were heterologously expressed. Effects o...

journal_title：Molecular pharmacology

authors： Imaizumi Y,Sakamoto K,Yamada A,Hotta A,Ohya S,Muraki K,Uchiyama M,Ohwada T

更新日期：2002-10-01 00:00:00

abstract：:We have reported previously that the transmembrane domains of the cholecystokinin-B/gastrin receptor (CCK-BR) comprise a putative ligand binding pocket. In the present study, we examined whether amino acid substitutions within the CCK-BR pocket altered the affinities and/or functional activities of L-365,260 (the prot...

journal_title：Molecular pharmacology

authors： Bläker M,Ren Y,Gordon MC,Hsu JE,Beinborn M,Kopin AS

更新日期：1998-11-01 00:00:00

abstract：:The endogenous bronchodilator, S-nitrosoglutathione (GSNO), increases expression, maturation, and function of both the wild-type and the DeltaF508 mutant of the cystic fibrosis transmembrane conductance regulatory protein (CFTR). Though transcriptional mechanisms of action have been identified, GSNO seems also to have...

journal_title：Molecular pharmacology

authors： Zaman K,Carraro S,Doherty J,Henderson EM,Lendermon E,Liu L,Verghese G,Zigler M,Ross M,Park E,Palmer LA,Doctor A,Stamler JS,Gaston B

更新日期：2006-10-01 00:00:00

abstract：:The structure-activity relationships for vasoactive intestinal peptide (VIP) receptor binding were studied using N-terminally modified VIP analogs. VIP fragments, and VIP receptor antagonists. Tissue sources included bovine coronary artery, rat mesenteric artery, rat pituitary, rat brain synaptosomes, and rat liver. E...

journal_title：Molecular pharmacology

authors： Rorstad OP,Wanke I,Coy DH,Fournier A,Huang M

更新日期：1990-06-01 00:00:00

abstract：:Inhibition of multidrug resistance protein 1 (MRP1) mediated cytostatic drug efflux might be useful in the treatment of drug resistant tumors. Because the glutathione (GSH) conjugate of ethacrynic acid (EA), GS-EA, is a good substrate of MRP1, GS-EA derivatives are expected to be good inhibitors of MRP1. To study stru...

journal_title：Molecular pharmacology

authors： Burg D,Wielinga P,Zelcer N,Saeki T,Mulder GJ,Borst P

更新日期：2002-11-01 00:00:00

abstract：:We investigated the mechanisms of MDR1 gene activation by CCAAT/enhancer binding protein beta (C/EBPbeta, or nuclear factor for interleukin 6) in human cancer cells. Transfection of the breast cancer cell line MCF-7 and its doxorubicin-selected variant MCF-7/ADR by either C/EBPbeta or C/EBPbeta-LIP (a dominant-negativ...

journal_title：Molecular pharmacology

authors： Chen KG,Sale S,Tan T,Ermoian RP,Sikic BI

更新日期：2004-04-01 00:00:00

abstract：:Compound BM5 [N-methyl-N(1-methyl-4-pyrrolidino-2-butynyl) acetamide] has previously been described as an agonist at postsynaptic muscarinic receptors and as an antagonist at presynaptic receptors. In the current work, we studied the ability of this compound to selectively stimulate phosphoinositide (PI) turnover in C...

journal_title：Molecular pharmacology

authors： Baumgold J,Drobnick A

更新日期：1989-09-01 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：:Immune-mediated drug hypersensitivity reactions (IDHRs) represent a significant problem due to their unpredictable and severe nature, as well as the lack of understanding of the pathogenesis. Sulfamethoxazole (SMX), a widely used antibiotic, has been used as a model compound to investigate the underlying mechanism of ...

journal_title：Molecular pharmacology

authors： Cheng L,Stewart BJ,You Q,Petersen DR,Ware JA,Piccotti JR,Kawabata TT,Ju C

更新日期：2008-06-01 00:00:00

abstract：:Dantrolene was recently identified as a novel inhibitor of the plasmodial surface anion channel (PSAC), an unusual ion channel on Plasmodium falciparum-infected human red blood cells. Because dantrolene is used clinically, has a high therapeutic index, and has desirable chemical synthetic properties, it may be a lead ...

journal_title：Molecular pharmacology

authors： Kang M,Lisk G,Hollingworth S,Baylor SM,Desai SA

更新日期：2005-07-01 00:00:00

abstract：:The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor with constitutive activities and those induced by xenobiotic ligands, such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). One unexplained cellular role for the AHR is its ability to promote cell cycle progression in the absence of exogenous...

journal_title：Molecular pharmacology

authors： Barhoover MA,Hall JM,Greenlee WF,Thomas RS

更新日期：2010-02-01 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

authors： Blomenröhr M,Heding A,Sellar R,Leurs R,Bogerd J,Eidne KA,Willars GB

更新日期：1999-12-01 00:00:00

abstract：:A polyamine component of Agelenopsis aperta spider venom designated FTX is reported to be a selective antagonist of P-type calcium channels in the mammalian brain. Consequently, this component has frequently been used as a pharmacological tool to determine the presence, distribution, and function of P-type channels in...

journal_title：Molecular pharmacology

authors： Norris TM,Moya E,Blagbrough IS,Adams ME

更新日期：1996-10-01 00:00:00

abstract：:Cultured murine hepatoma 1c1c7 cells were treated with either the actin filament-disrupting drug cytochalasin D or the microtubule inhibitors colchicine and nocadazole (NOC) to assess the role of the cytoskeleton in the process of cytochrome P450 Cyp1a-1 induction. Indirect fluorescence analyses demonstrated that micr...

journal_title：Molecular pharmacology

authors： Schöller A,Hong NJ,Bischer P,Reiners JJ Jr

更新日期：1994-05-01 00:00:00

abstract：:For a series of antitumor-active 5-substituted 9-aminoacridine-4-carboxamide topoisomerase II poisons, we have used X-ray crystallography and stopped-flow spectrophotometry to explore relationships between DNA binding kinetics, biological activity, and the structures of their DNA complexes. The structure of 5-F-9-amin...

journal_title：Molecular pharmacology

authors： Adams A,Guss JM,Collyer CA,Denny WA,Prakash AS,Wakelin LP

更新日期：2000-09-01 00:00:00

abstract：:Dietary lipids and fat-soluble micronutrients are solubilized in mixed micelles and absorbed in the small intestine. Based on an assumption that cholesterol and other fat-soluble molecules share a number of transport mechanisms and the fact that Niemann-Pick C1-like 1 (NPC1L1) is critical for intestinal cholesterol ab...

journal_title：Molecular pharmacology

authors： Narushima K,Takada T,Yamanashi Y,Suzuki H

更新日期：2008-07-01 00:00:00