2-Fluoroestradiol. Separation of estrogenicity from carcinogenicity.

abstract：:Recent reports regarding the significance of chemokine receptors in disease have put a spotlight on atypical chemokine receptor 3 (ACKR3). This atypical chemokine receptor is overexpressed in numerous cancer types and has been involved in the modulation of tumor cell proliferation and migration, tumor angiogenesis, or...

journal_title：Molecular pharmacology

authors： Neves M,Fumagalli A,van den Bor J,Marin P,Smit MJ,Mayor F

更新日期：2019-12-01 00:00:00

abstract：:The interaction of quinidine with a cloned human cardiac potassium channel (HK2) expressed in a stable mouse L cell line was studied using the whole-cell tight-seal voltage-clamp technique. Quinidine (20 microM) did not affect the initial sigmoidal activation time course of the current. However, it reduced the peak cu...

journal_title：Molecular pharmacology

authors： Snyders J,Knoth KM,Roberds SL,Tamkun MM

更新日期：1992-02-01 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

authors： Ward SD,Curtis CA,Hulme EC

更新日期：1999-11-01 00:00:00

abstract：:A methylcholanthrene-induced rat sarcoma that can be propagated in vitro or in vivo was evaluated for resistance to antifolates and was found to be relatively resistant to methotrexate and 10-ethyl-10-deazaaminopterin but sensitive to trimetrexate. Rat sarcoma cell extracts contained low levels of dihydrofolate reduct...

journal_title：Molecular pharmacology

authors： Li WW,Lin JT,Schweitzer BI,Bertino JR

更新日期：1991-11-01 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：:Neuroactive steroids have been postulated to cause anesthesia by binding to unique steroid recognition sites on gamma-aminobutyric acid (GABA) receptors and modulating GABA receptor function. Steroids interact with these sites diastereoselectively, but it is unknown whether steroid sites show enantioselectivity. To ad...

journal_title：Molecular pharmacology

authors： Wittmer LL,Hu Y,Kalkbrenner M,Evers AS,Zorumski CF,Covey DF

更新日期：1996-12-01 00:00:00

abstract：:We previously described the development of genetic models to study the in vivo functions of the hepatic cytochrome P450 (P450) system, through the hepatic deletion of either cytochrome P450 oxidoreductase [POR; HRN (hepatic reductase null) line] or cytochrome b(5) [HBN (hepatic cytochrome b(5) null) line]. However, HR...

journal_title：Molecular pharmacology

authors： Henderson CJ,McLaughlin LA,Wolf CR

更新日期：2013-06-01 00:00:00

abstract：:The neuropeptides vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating peptide (PACAP) and their class II G protein-coupled receptors VPAC(1), VPAC(2), and PAC(1) play important roles in human physiology. No small molecule modulator has ever been reported for the VIP/PACAP receptors, and ther...

journal_title：Molecular pharmacology

authors： Chu A,Caldwell JS,Chen YA

更新日期：2010-01-01 00:00:00

abstract：:The mechanisms underlying mastoparan-induced elevation of the intracellular free calcium concentration ([Ca2+]i) were investigated in the insulin-secreting cell lines RINm5F and HIT. In both cell types, micromolar concentrations of mastoparan induced a prompt increase of [Ca2+]i, measured as an increase in fura-2 fluo...

journal_title：Molecular pharmacology

authors： Eddlestone GT,Komatsu M,Shen L,Sharp GW

更新日期：1995-04-01 00:00:00

abstract：:Tumor suppressor gene BRCA1 is frequently mutated in familial breast and ovarian cancer. BRCA1 plays pivotal roles in maintaining genomic stability by interacting with numerous proteins in cell cycle control and DNA repair. Irofulven (6-hydroxymethylacylfulvene, HMAF, MGI 114, NSC 683863) is one of a new class of anti...

journal_title：Molecular pharmacology

authors： Wiltshire T,Senft J,Wang Y,Konat GW,Wenger SL,Reed E,Wang W

更新日期：2007-04-01 00:00:00

abstract：:Ethanol (ETOH) can cause apoptotic death of neurons by depleting GSH with an associated increase in oxidative stress. The current study illustrates a means to overcome this ETOH-induced neurotoxicity by enhancing GSH through boosting Nrf2, a transcription factor that controls GSH homeostasis. ETOH treatment caused a s...

journal_title：Molecular pharmacology

authors： Narasimhan M,Mahimainathan L,Rathinam ML,Riar AK,Henderson GI

更新日期：2011-12-01 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

authors： Laz TM,Forray C,Smith KE,Bard JA,Vaysse PJ,Branchek TA,Weinshank RL

更新日期：1994-09-01 00:00:00

abstract：:Five separate guanine nucleotide-binding proteins (G proteins) were immunologically identified in membranes from neuroblastoma x glioma NG108-15 hybrid cells. These alpha subunit proteins were Gi2 alpha, two isoforms of Gi3 alpha, and two isoforms of Go alpha. The G proteins that interacted with delta-opioid receptors...

journal_title：Molecular pharmacology

authors： Roerig SC,Loh HH,Law PY

更新日期：1992-05-01 00:00:00

abstract：:Multidrug and toxin extrusion 1 (MATE1/SLC47A1) is important for excretion of organic cations in the kidney and liver, where it is located on the luminal side. Although its functional and regulatory characteristics have been clarified, its pharmacokinetic roles in vivo have yet to be elucidated. In the present study, ...

journal_title：Molecular pharmacology

authors： Tsuda M,Terada T,Mizuno T,Katsura T,Shimakura J,Inui K

更新日期：2009-06-01 00:00:00

abstract：:Endothelin (ET) receptors are present in pituitary cells and stimulate hormone release through the phosphoinositide/Ca2+ signaling system. In pituitary cell suspensions, ET caused [Ca2+]i elevations of much higher amplitudes than those induced by other vasoactive hormones, including angiotensin II, vasopressin, and no...

journal_title：Molecular pharmacology

authors： Stojilković SS,Iida T,Merelli F,Catt KJ

更新日期：1991-06-01 00:00:00

abstract：:In an effort to combine the benefits of fibrinolytics, such as staphylokinase, with those of thrombin inhibitors for the prevention of vessel reocclusion after vascular injury, we have produced several chimeric proteins with plasminogen-activating and thrombin-inhibiting properties. Fusion proteins were constructed co...

journal_title：Molecular pharmacology

authors： Icke C,Schlott B,Ohlenschläger O,Hartmann M,Gührs KH,Glusa E

更新日期：2002-08-01 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

authors： Burelout C,Thibault N,Levasseur S,Simard S,Naccache PH,Bourgoin SG

更新日期：2004-08-01 00:00:00

abstract：:The retinoid-related orphan receptors (RORs) and liver X receptors (LXRs) were postulated to have distinct functions. RORs play a role in tissue development and circadian rhythm, whereas LXRs are sterol sensors that affect lipid homeostasis. In this study, we revealed a novel function of RORalpha (NR1F1) in regulating...

journal_title：Molecular pharmacology

authors： Wada T,Kang HS,Angers M,Gong H,Bhatia S,Khadem S,Ren S,Ellis E,Strom SC,Jetten AM,Xie W

更新日期：2008-03-01 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：:The vitamin D receptor (VDR) mediates vitamin D signaling in numerous physiological and pharmacological processes, including bone and calcium metabolism, cellular growth and differentiation, immunity, and cardiovascular function. Although transcriptional regulation by VDR has been investigated intensively, an understa...

journal_title：Molecular pharmacology

authors： Choi M,Yamada S,Makishima M

更新日期：2011-12-01 00:00:00

abstract：:The cannabinoid analog abnormal cannabidiol [abn-cbd; (-)-4-(3-3,4-trans-p-menthadien-[1,8]-yl)-olivetol] does not bind to CB(1) or CB(2) receptors, yet it acts as a full agonist in relaxing rat isolated mesenteric artery segments. Vasorelaxation by abn-cbd is endothelium-dependent, pertussis toxin-sensitive, and is i...

journal_title：Molecular pharmacology

authors： Offertáler L,Mo FM,Bátkai S,Liu J,Begg M,Razdan RK,Martin BR,Bukoski RD,Kunos G

更新日期：2003-03-01 00:00:00

abstract：:Olanzapine was shown to be oxidized to a reactive intermediate by HOCl, which is the major oxidant produced by activated neutrophils. A mass spectrum obtained using a flow system in which the reactants were fed into a mixing chamber and the products flowed directly into a mass spectrometer revealed a reactive intermed...

journal_title：Molecular pharmacology

authors： Gardner I,Zahid N,MacCrimmon D,Uetrecht JP

更新日期：1998-06-01 00:00:00

abstract：:We have examined alpha1beta2gamma2L GABAA receptor modulation by the endogenous steroids allopregnanolone (3alpha5alphaP), pregnenolone sulfate, and beta-estradiol in the absence and presence of ethanol. Coapplication of 0.1 to 1% (17-170 mM) ethanol influenced receptor modulation by 3alpha5alphaP but not that by preg...

journal_title：Molecular pharmacology

authors： Akk G,Li P,Manion BD,Evers AS,Steinbach JH

更新日期：2007-02-01 00:00:00

abstract：:The human monoamine oxidase (MAO) B plays a major role in the degradation of biogenic and dietary amines such as phenylethylamine, benzylamine, dopamine, and tyramine. We previously showed that the -246/-99 MAO B promoter region exhibited the highest activity and contained two clusters of overlapping Sp1 sites, a CACC...

journal_title：Molecular pharmacology

authors： Wong WK,Chen K,Shih JC

更新日期：2001-04-01 00:00:00

abstract：:Westernization of dietary habits increases lipid intake and is responsible for increased numbers of patients with atherosclerotic diseases. Niemann-Pick C1-Like 1 (NPC1L1)-a cholesterol importer-plays a crucial role in dietary cholesterol absorption in the intestine and is closely associated with several lipid-related...

journal_title：Molecular pharmacology

authors： Yamamoto H,Yamanashi Y,Takada T,Mu S,Tanaka Y,Komine T,Suzuki H

更新日期：2019-07-01 00:00:00

abstract：:Activation of N-methyl-D-aspartate (NMDA) receptors is required for induction of some lasting changes in nervous system structure and function. The cellular mechanisms involved in transducing receptor stimulation into long-lasting changes in cellular activity are unknown. Immediate-early genes (IEGs) have been implica...

journal_title：Molecular pharmacology

authors： Lerea LS,Carlson NG,McNamara JO

更新日期：1995-06-01 00:00:00

abstract：:The binding kinetics of [3H]Ro 15-1788, a selective benzodiazepine receptor antagonist, to synaptosomal membranes of rat cerebral cortices was studied. [3H]Ro 15-1788 binds with high affinity (dissociation constant, 0.53 nM) to a single class of binding sites (maximal binding capacity, 1.97 pmoles/mg of protein). Equi...

journal_title：Molecular pharmacology

authors： Chiu TH,Rosenberg HC

更新日期：1983-03-01 00:00:00

abstract：:ATP-binding cassette (ABC) membrane proteins comprise a superfamily of transporters with a wide variety of substrates. Humans have 49 members in this superfamily. Several human ABC transporters, such as ABCB1 and ABCC1, have been attributed to cause multidrug resistance (MDR) in cancer treatment when over-expressed. I...

journal_title：Molecular pharmacology

authors： Liu Y,Peng H,Zhang JT

更新日期：2005-08-01 00:00:00

abstract：:The human histamine H(4)-receptor (hH(4)R) possesses high constitutive activity and, like the human H(1)-receptor (hH(1)R), is involved in the pathogenesis of type-I allergic reactions. The study aims were to explore the value of dual H(1)/H(4)R antagonists as antiallergy drugs and to address the question of whether H...

journal_title：Molecular pharmacology

authors： Deml KF,Beermann S,Neumann D,Strasser A,Seifert R

更新日期：2009-11-01 00:00:00

abstract：:Dysregulation of the chemokine system is implicated in a number of autoimmune and inflammatory diseases, as well as cancer. Modulation of chemokine receptor function is a very promising approach for therapeutic intervention. Despite interest from academic groups and pharmaceutical companies, there are currently few ap...

journal_title：Molecular pharmacology

authors： Bobkov V,Arimont M,Zarca A,De Groof TWM,van der Woning B,de Haard H,Smit MJ

更新日期：2019-12-01 00:00:00