The 2016 John J. Abel Award Lecture: Targeting the Mechanical Microenvironment in Cancer.

abstract：:Nuclear receptors play important roles in the maintenance of the endocrine system, regulation of organ differentiation, and fetal development. Endocrine disruptors exert their adverse effects by disrupting the endocrine system via various mechanisms. To assess the effects of endocrine disruptors on nuclear receptors, ...

journal_title：Molecular pharmacology

authors： Kanayama T,Kobayashi N,Mamiya S,Nakanishi T,Nishikawa J

更新日期：2005-03-01 00:00:00

abstract：:Inhibitors of the proteasome, a multicatalytic proteinase complex responsible for intracellular proteolysis, activate programmed cell death in part through the c-Jun-N-terminal kinase (JNK). Proteasome inhibitors also induce mitogen-activated protein kinase phosphatase-1 (MKP-1), however, which can inactivate JNK, and...

journal_title：Molecular pharmacology

authors： Small GW,Shi YY,Edmund NA,Somasundaram S,Moore DT,Orlowski RZ

更新日期：2004-12-01 00:00:00

abstract：:Nitric oxide (NO) possesses potent anti-inflammatory properties; however, an over-production of NO will promote inflammation and induce cell and tissue dysfunction. Thus, the ability to precisely regulate NO production could prove beneficial in controlling damage. In this study, advantage was taken of the well charact...

journal_title：Molecular pharmacology

authors： Bian K,Harari Y,Zhong M,Lai M,Castro G,Weisbrodt N,Murad F

更新日期：2001-04-01 00:00:00

abstract：:We have previously reported that endocytic sorting of ET(A) endothelin receptors to the recycling pathway is dependent on a signal residing in the cytoplasmic carboxyl-terminal region. The aim of the present work was to characterize the carboxyl-terminal recycling motif of the ET(A) receptor. Assay of truncation mutan...

journal_title：Molecular pharmacology

authors： Paasche JD,Attramadal T,Kristiansen K,Oksvold MP,Johansen HK,Huitfeldt HS,Dahl SG,Attramadal H

更新日期：2005-05-01 00:00:00

abstract：:Up-regulation of fractalkine is involved in vascular and tissue damage in inflammatory conditions. Resveratrol has been shown to have anti-inflammatory, antioxidant, and antitumor activities. Its regulatory effects on expression of fractalkine in vascular endothelial cells and fractalkine receptor CX3CR1 in monocytes ...

journal_title：Molecular pharmacology

authors： Moon SO,Kim W,Sung MJ,Lee S,Kang KP,Kim DH,Lee SY,So JN,Park SK

更新日期：2006-07-01 00:00:00

abstract：:We examined the effect of trichosporin-B-III, an alpha-aminoisobutyric acid-containing antibiotic peptide consisting of 19 amino acid residues and a phenylalaninol, on catecholamine secretion from cultured bovine adrenal chromaffin cells. Incubation of the cells with trichosporin-B-III (3-20 microM) caused an increase...

journal_title：Molecular pharmacology

authors： Tachikawa E,Takahashi S,Furumachi K,Kashimoto T,Iida A,Nagaoka Y,Fujita T,Takaishi Y

更新日期：1991-11-01 00:00:00

abstract：:The D2 dopamine receptor (D2R) was examined for its ability to mediate nuclear factor-kappaB (NF-kappaB) activation through G proteins. Stimulation of D2R-transfected HeLa cells with its agonist quinpirole induced the expression of a NF-kappaB luciferase reporter and formation of NF-kappaB-DNA complex. This response w...

journal_title：Molecular pharmacology

authors： Yang M,Zhang H,Voyno-Yasenetskaya T,Ye RD

更新日期：2003-08-01 00:00:00

abstract：:Hepatocyte nuclear factor 4alpha (HNF4alpha) is a key transcription factor for the constitutive expression of cytochromes P450 (P450s) in the liver. However, human hepatoma HepG2 cells show a high level of HNF4alpha but express only marginal P450 levels. We found that the HNF4alpha-mediated P450 transcription in HepG2...

journal_title：Molecular pharmacology

authors： Martínez-Jiménez CP,Castell JV,Gómez-Lechón MJ,Jover R

更新日期：2006-11-01 00:00:00

abstract：:Differential display reverse transcription-polymerase chain reaction was used to identify mRNAs that are differentially expressed in the brain of rats treated chronically with the reference tricyclic antidepressant, imipramine, in comparison with control rats. The gene encoding for a mutation suppressor for Sec4-8 yea...

journal_title：Molecular pharmacology

authors： Andriamampandry C,Muller C,Schmidt-Mutter C,Gobaille S,Spedding M,Aunis D,Maitre M

更新日期：2002-12-01 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：:Activation of mitogen-activated protein kinase (MAPK) is induced by adding thyrotropin-releasing hormone (TRH) to COS-7 cells cotransfected with TRH receptors and an epitope-tagged MAPK. Long term treatment of the cells with pertussis toxin has no effect on TRH-induced MAPK activation. Incubation of the cells with the...

journal_title：Molecular pharmacology

authors： Palomero T,Barros F,del Camino D,Viloria CG,de la Peña P

更新日期：1998-04-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) contribute to the regulation of every aspect of human physiology and are therapeutic targets for the treatment of numerous diseases. As a consequence, understanding the myriad of mechanisms controlling GPCR signaling and trafficking is essential for the development of new pharmacolo...

journal_title：Molecular pharmacology

authors： Dunn HA,Ferguson SS

更新日期：2015-10-01 00:00:00

abstract：:Guanidine and its alkyl analogs stimulate the neuromuscular junction presynaptically by inhibiting voltage-gated potassium (Kv) channels, leading to enhanced release of acetylcholine in the synaptic cleft. This stimulatory effect of guanidine underlies its use in the therapy for the neuromuscular diseases myasthenic s...

journal_title：Molecular pharmacology

authors： Kalia J,Swartz KJ

更新日期：2011-12-01 00:00:00

abstract：:We investigated the interactions of the anticancer drug vinorelbine with drug efflux transporters and cytochrome P450 3A drug-metabolizing enzymes. Vinorelbine was transported by human multidrug-resistance associated protein (MRP) 2, and Mrp2 knockout mice displayed increased vinorelbine plasma exposure after oral adm...

journal_title：Molecular pharmacology

authors： Lagas JS,Damen CW,van Waterschoot RA,Iusuf D,Beijnen JH,Schinkel AH

更新日期：2012-10-01 00:00:00

abstract：:The diphosphoinositol polyphosphates ("inositol pyrophosphates") are a specialized subgroup of the inositol phosphate signaling family. This review proposes that many of the current data concerning the metabolic turnover and biological effects of the diphosphoinositol polyphosphates are linked by a common theme: these...

journal_title：Molecular pharmacology

authors： Shears SB

更新日期：2009-08-01 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

authors： Sasakawa N,Ferguson JE,Sharif M,Hanley MR

更新日期：1994-08-01 00:00:00

abstract：:Cadmium is a dangerous metal distributed widely in the environment. Members of our laboratory recently identified the ZIP8 transporter protein, encoded by the mouse Slc39a8 gene, to be responsible for genetic differences in response to cadmium damage of the testis. Stable retroviral infection of the ZIP8 cDNA in mouse...

journal_title：Molecular pharmacology

authors： He L,Girijashanker K,Dalton TP,Reed J,Li H,Soleimani M,Nebert DW

更新日期：2006-07-01 00:00:00

abstract：:Gemcitabine and pemetrexed are effective agents in the treatment of non-small-cell lung cancer (NSCLC), and the present study investigates cellular and genetic aspects of their interaction against A549, Calu-1, and Calu-6 cells. Cells were treated with pemetrexed and gemcitabine, and their interaction was assessed usi...

journal_title：Molecular pharmacology

authors： Giovannetti E,Mey V,Nannizzi S,Pasqualetti G,Marini L,Del Tacca M,Danesi R

更新日期：2005-07-01 00:00:00

abstract：:The ligand-binding sites of many G protein-coupled receptors (GPCRs) are situated around and deeply embedded within the central pocket formed by their seven transmembrane-spanning α-helical domains. Generally, these binding sites are assumed accessible to endogenous ligands from the aqueous phase. Recent advances in t...

journal_title：Molecular pharmacology

authors： Szlenk CT,Gc JB,Natesan S

更新日期：2019-11-01 00:00:00

abstract：:The dopamine D3 receptor, although structurally similar to the dopamine D2 receptor, has 100-fold higher affinity for agonists such as dopamine and quinpirole, when these receptors are expressed in 293 cells. Additionally, the D3 receptor has generally lower affinity for several antagonists than does the D2 receptor. ...

journal_title：Molecular pharmacology

authors： Robinson SW,Jarvie KR,Caron MG

更新日期：1994-08-01 00:00:00

abstract：:In this study, we investigated the effects of single alanine substitutions of amino acid residues in the supposed ATP binding site of the human P2X3 receptor on the agonistic effect of nucleotide analogs. The wild-type and mutant receptors were expressed in HEK293 cells, and the nucleotide effects were measured by mea...

journal_title：Molecular pharmacology

authors： Riedel T,Wiese S,Leichsenring A,Illes P

更新日期：2012-07-01 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：:The total CYP3A5 mRNA level is significantly greater in carriers of the CYP3A5*1 allele than in CYP3A5*3 homozygotes. Most of the CYP3A5*3 mRNA includes an intronic sequence (exon 3B) containing premature termination codons (PTCs) between exons 3 and 4. Two models were used to investigate the degradation of CYP3A5 mRN...

journal_title：Molecular pharmacology

authors： Busi F,Cresteil T

更新日期：2005-09-01 00:00:00

abstract：:The microtubule-binding taxanes, docetaxel and cabazitaxel, are administered intravenously for the treatment of castration-resistant prostate cancer (CRPC) as the oral administration of these drugs is largely hampered by their low and highly variable bioavailabilities. Using a simple, rapid, and environmentally friend...

journal_title：Molecular pharmacology

authors： Liao VWY,Kumari A,Narlawar R,Vignarajan S,Hibbs DE,Panda D,Groundwater PW

更新日期：2020-06-01 00:00:00

abstract：:Ceramides are naturally occurring compounds recognized to mediate apoptosis. N-acylsphingosines, containing a double bond at carbons 4 and 5 of their sphingoid backbone, are thought to be the active form, because N-acylsphinganines with completely saturated sphingoid are inactive. In the present study, we synthesized ...

journal_title：Molecular pharmacology

authors： Hwang O,Kim G,Jang YJ,Kim SW,Choi G,Choi HJ,Jeon SY,Lee DG,Lee JD

更新日期：2001-05-01 00:00:00

abstract：:Rat and human lung microsomal cytochrome P-450 (P-450) enzymes have been characterized with regard to their catalytic activities towards several xenobiotic chemicals, including procarcinogens, in different microsomal preparations. Rat lung microsomal P-450s were more active than the human P-450s in catalyzing most of ...

journal_title：Molecular pharmacology

authors： Shimada T,Yun CH,Yamazaki H,Gautier JC,Beaune PH,Guengerich FP

更新日期：1992-05-01 00:00:00

abstract：:The X-ray and NMR structural study of 3-carbomethoxy rifamycin S5 was undertaken in order to determine whether its low antimicrobial activity was related to a conformation of the molecule which was unfavorable for interaction with bacterial DNA-dependent RNA polymerase. However, the molecule assumes a conformation sim...

journal_title：Molecular pharmacology

authors： Brufani M,Cellai L,Cerrini S,Fedeli W,Segre A,Vaciago A

更新日期：1982-03-01 00:00:00

abstract：:We have observed that rodent cell lines (mouse, hamster) contain approximately 10 times the levels of dihydrofolate reductase as human cell lines, yet the sensitivity to methotrexate (ED(50)), the folate antagonist that targets this enzyme, is similar. Our previous studies showed that dihydrofolate reductase protein l...

journal_title：Molecular pharmacology

authors： Hsieh YC,Skacel NE,Bansal N,Scotto KW,Banerjee D,Bertino JR,Abali EE

更新日期：2009-10-01 00:00:00

abstract：:A series of isoflavone and tyrphostin compounds were found to inhibit the degradation of cAMP by several cyclic nucleotide phosphodiesterase (PDE) isozymes. Specific hydroxyl groups on the isoflavone structure were critical for PDE isozyme-selective inhibition. Replacement of the C-7 hydroxyl group of the isoflavone w...

journal_title：Molecular pharmacology

authors： Nichols MR,Morimoto BH

更新日期：2000-04-01 00:00:00

abstract：:Comparative molecular field analysis (CoMFA) predicts that the large electrostatic field around the phosphate groups of ATP plays a crucial role in stabilizing the open state of the cardiac ryanodine receptor (RyR) channel. We therefore investigated the effects of adenosine-5'-(beta,gamma-methylenetriphosphate) (AMP-P...

journal_title：Molecular pharmacology

authors： Chan WM,Welch W,Sitsapesan R

更新日期：2003-01-01 00:00:00