当前位置： SCI文献检索 > Chemical Biology & Drug Design期刊下所有文献 > Structure-dependent activation of gene expression by bis-indole and quinoline-derived activators of nuclear receptor 4A2.

Structure-dependent activation of gene expression by bis-indole and quinoline-derived activators of nuclear receptor 4A2.

Abstract：

:Bis-indole derivatives including 1,1-bis(3'-indolyl)-1-(4-chlorophenyl)methane (DIM-C-pPhCl) and substituted quinolines such as chloroquine (CQ) and amodiaquine (AQ) are nuclear receptor 4A2 (NR4A2, Nurr1) ligands, and they exhibit anti-inflammatory activities in mouse and rat models of Parkinson's disease, respectively. However, computational modeling demonstrates that the quinoline derivatives interact with the ligand-binding domain, whereas the bis-indoles preferentially interact with a C-terminal cofactor binding site of NR4A2. In this study, the effects of DIM-C-pPhCl and related analogs were compared with CQ/AQ as inducers of NR4A2-responsive genes including vasoactive intestinal peptide, osteopontin, proopiomelanocortin, and neuropilin 1 in Panc1 and Panc28 pancreatic cancer cells. The results demonstrate that, among the bis-indole analogs, their relative potencies as inducers were structure-gene- and cell context dependent. In contrast, CQ and AQ were significantly less potent than the bis-indole derivatives and, for some of the NR4A2-regulated genes, CQ and AQ were inactive as inducers. These results demonstrate that although bis-indole and quinoline derivatives have been characterized as activators of NR4A2-dependent gene expression, these two classes of compounds exhibit different activities, indicating that they are selective NR4A2 modulators.

journal_name

Chem Biol Drug Des

journal_title

Chemical biology & drug design

authors

Li X,Tjalkens RB,Shrestha R,Safe S

doi

10.1111/cbdd.13564

subject

Has Abstract

pub_date

2019-10-01 00:00:00

pages

1711-1720

issue

4

eissn

1747-0277

issn

1747-0285

journal_volume

94

pub_type

杂志文章,评审

相关文献

Chemical Biology & Drug Design文献大全
  • Receptor-dependent 4D-QSAR analysis of peptidemimetic inhibitors of Trypanosoma cruzi trypanothione reductase with receptor-based alignment.

    abstract：:Receptor-dependent four-dimensional quantitative structure-activity relationship (RD-4D-QSAR) studies were applied on a series of 21 peptides reversible inhibitors of Trypanosoma cruzi trypanothione reductase (TR) (Amino Acids, 20, 2001, 145). The RD-4D-QSAR (J Chem Inform Comp Sci, 43, 2003, 1591) approach can evalua...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2012.01338.x

    authors： da Rocha Pita SS,Albuquerque MG,Rodrigues CR,Castro HC,Hopfinger AJ

    更新日期：2012-05-01 00:00:00

  • Physicochemical and biological evaluation of a cinnamamide derivative R,S-(2E)-1-(3-hydroxypiperidin-1-yl)-3-phenylprop-2-en-1-one (KM-608) for nervous system disorders.

    abstract：:A cinnamamide scaffold has been successfully incorporated in several compounds possessing desirable pharmacological activities in central and peripheral nervous system such as anticonvulsant, antidepressant, neuroprotective, analgesic, anti-inflammatory, muscle relaxant, and sedative/hypnotic properties. R,S-(2E)-1-(3...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.12943

    authors： Gunia-Krzyżak A,Żesławska E,Bareyre FM,Nitek W,Waszkielewicz AM,Marona H

    更新日期：2017-08-01 00:00:00

  • Investigation into potent inflammation inhibitors from traditional Chinese medicine.

    abstract：:Microsomal prostaglandin E synthase-1 (mPGES-1) is the key enzyme for prostaglandin E2 (PGE2) generation during inflammation and is a potential target for designing anti-inflammatory drugs. Potential inhibitors of m-PGES-1 were selected from traditional Chinese medicine (TCM Database@Taiwan) based on the pharmacophore...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2011.01202.x

    authors： Chen KC,Sun MF,Yang SC,Chang SS,Chen HY,Tsai FJ,Chen CY

    更新日期：2011-10-01 00:00:00

  • Membrane permeability of acylated cystatin depends on the fatty acyl chain length.

    abstract：:Hydrophobization of proteins, such as chemical acylation, has been recognized as an efficient method for improving their membrane permeability. In this research, chicken cystatin, a model protein inhibitor of cysteine proteinases, was acylated with fatty acyl residues of 6-18 carbon atoms. The chemical modification wa...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2008.00693.x

    authors： Kocevar N,Obermajer N,Kreft S

    更新日期：2008-09-01 00:00:00

  • Dimethylthiazolidine carboxylic acid as a rigid p3 unit in inhibitors of serine proteases: application to two targets.

    abstract：:Serine proteases are a very large class of enzymes, many of which represent important targets for therapeutic agents against a wide variety of disease states. The similarity in active site architecture for these proteases has often allowed inhibitor design strategies for a particular target to be successfully applied ...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2009.00870.x

    authors： Kawai SH,Aubry N,Duceppe JS,Llinàs-Brunet M,LaPlante SR

    更新日期：2009-11-01 00:00:00

  • Ligand- and structure-based drug design strategies and PPARδ/α selectivity.

    abstract：:Peroxisome-proliferator-activated receptors are a class of nuclear receptors with three subtypes: α, γ and δ. Their main function is regulating gene transcription related to lipid and carbohydrate metabolism. Currently, there are no peroxisome-proliferator-activated receptors δ drugs being marketed. In this work, we s...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2012.01424.x

    authors： Maltarollo VG,Honório KM

    更新日期：2012-10-01 00:00:00

  • Efficient use of the iron ortho-nitrophenylporphyrin chloride to mimic biological oxidations of dimethylaminoantipyrine.

    abstract：:Major metabolites of dimethylaminoantipyrine have been synthesized using iron ortho-nitrophenylporphyrin chloride as biomimetic catalyst. Reactivity of iron tetrakis-ortho-nitrophenylporphyrin chloride [Fe(TNO2PP)Cl] has been compared with iron tetrakis-pentafluorophenylporphyrin chloride and iron tetrakis-2,6-dichlor...

    journal_title：Chemical biology & drug design

    pub_type： 信件

    doi：10.1111/j.1747-0285.2007.00568.x

    authors： Bazin MJ,Shi H,Delaney J,Kline B,Zhu Z,Kuhn C,Berlioz F,Farley KA,Fate G,Lam W,Walker GS,Yu L,Pollastri MP

    更新日期：2007-10-01 00:00:00

  • Synthesis and SAR study of opioid receptor ligands: mono- and bis-indolomorphinans.

    abstract：:Mono- and bis-indolomorphinans were synthesized through a multi-step synthetic approach from the alkaloid, thebaine, to further explore the C-ring SAR (structure-activity relationship) of morphinan scaffold. Both mono-indoles displayed good binding affinity and selectivity for the delta receptor, with compound 6b poss...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2009.00849.x

    authors： Li F,Yin C,Chen J,Liu J,Xie X,Zhang A

    更新日期：2009-10-01 00:00:00

  • Synthesis, Activity, and Docking Study of Novel Phenylthiazole-Carboxamido Acid Derivatives as FFA2 Agonists.

    abstract：:Free fatty acid receptor 2 (FFA2), also known as GPR43, is activated by short-chain fatty acids (SCFAs) that are mainly produced by the gut microbiota through the fermentation of undigested carbohydrates and dietary fibers. FFA2 currently appears to be a potential target in the management of obesity, diabetes, inflamm...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.12729

    authors： Ma L,Wang T,Shi M,Fu P,Pei H,Ye H

    更新日期：2016-07-01 00:00:00

  • A specific pharmacophore model of Aurora B kinase inhibitors and virtual screening studies based on it.

    abstract：:In this study, 3D-pharmacophore models of Aurora B kinase inhibitors have been developed by using HipHop and HypoGen modules in Catalyst software package. The best pharmacophore model, Hypo1, which has the highest correlation coefficient (0.9911), consists of one hydrogen-bond acceptor, one hydrogen-bond donor, one hy...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2008.00751.x

    authors： Wang HY,Li LL,Cao ZX,Luo SD,Wei YQ,Yang SY

    更新日期：2009-01-01 00:00:00

  • Quantitative analysis of RNA-mediated protein-protein interactions in living cells by FRET.

    abstract：:Specific assembly of ribonucleoprotein complexes is essential in controlling various cellular functions including gene regulation. Diverse scaffolds containing proteins or nucleic acids could play key roles in stabilizing specific ribonucleoprotein complexes by enhancing protein-protein or RNA-protein interactions. On...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2007.00501.x

    authors： Chiu YL,Cao H,Rana TM

    更新日期：2007-04-01 00:00:00

  • Synthesis, molecular docking and biological evaluation of 1-phenylsulphonyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as novel potential tubulin assembling inhibitors.

    abstract：:A series of new 1-phenylsulphonyl-2-(1-methylindol-3-yl)-benzimidazole derivatives were designed, synthesized and evaluated as potential inhibitors of tubulin polymerization and anthropic cancer cell lines. Among them, compound 33 displayed the most potent tubulin polymerization inhibitory activity in vitro (IC50  = 1...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.12932

    authors： Wang YT,Cai XC,Shi TQ,Zhang YL,Wang ZC,Liu CH,Zhu HL

    更新日期：2017-07-01 00:00:00

  • Induction of cell death by a novel naphthoquinone containing a modified anthracycline ring system.

    abstract：:The novel naphthoquinone adduct 12,13-Dihydro-N-methyl-6,11,13-trioxo-5H-benzo[4,5]cyclohepta[1,2-b]naphthalen-5,12-imine (hereafter called TU100) was synthesized as a potential chemotherapeutic agent. TU100 arrests tissue culture cells in S and G2/M phases of the cell cycle, followed by rapid induction of apoptosis. ...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2011.01214.x

    authors： Carvajal D,Kennedy S,Boustani A,Lazar M,Nguyen S,DiCesare JC,Sheaff RJ

    更新日期：2011-11-01 00:00:00

  • Synthesis and biological evaluation of [1,2,4]triazolo[3,4-a]phthalazine and tetrazolo[5,1-a]phthalazine derivatives bearing substituted benzylpiperazine moieties as positive inotropic agents.

    abstract：:Two series of [1,2,4]triazolo[3,4-a]phthalazine and tetrazolo[5,1-a]phthalazine derivatives bearing substituted benzylpiperazine moieties have been synthesized and evaluated for their positive inotropic activity by measuring left atrium stroke volume on isolated rabbit heart preparations. The majority of the derivativ...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.12101

    authors： Wu Y,Sun LP,Ma LX,Che J,Song MX,Cui X,Piao HR

    更新日期：2013-05-01 00:00:00

  • Structural basis of non-steroidal anti-inflammatory drug diclofenac binding to human serum albumin.

    abstract：:Human serum albumin (HSA) is the most abundant protein in plasma, which plays a central role in drug pharmacokinetics because most compounds bound to HSA in blood circulation. To understand binding characterization of non-steroidal anti-inflammatory drugs to HSA, we resolved the structure of diclofenac and HSA complex...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.12583

    authors： Zhang Y,Lee P,Liang S,Zhou Z,Wu X,Yang F,Liang H

    更新日期：2015-11-01 00:00:00

  • Tumor suppressive activities of solvatochromic 3,3'-azadimethylene dinaphthospiropyran in colon cancer model.

    abstract：:Spiropyrans have been extensively investigated because of their thermo- and photochromic characteristics, but their biotherapeutic properties have not been explored much. We report anti-proliferative properties of a novel 3,3'-azadimethylene dinaphthospiropyran 11. Dibenzospiropyrans and dinaphthospiropyrans were synt...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.13785

    authors： Lagisetty P,Eeda V,Yadav VR,Nimmo SL,Subramaniam D,Powell DR,Awasthi V

    更新日期：2021-02-01 00:00:00

  • Design, synthesis, and biological evaluation of chrysin derivatives as potential FabH inhibitors.

    abstract：:New series of chrysin derivatives (4a-4t) were designed and synthesized by introducing different substituted piperazines at C-7 position. Their inhibitory effects on FabH were evaluated using two Gram-negative bacterial strains, Escherichia coli and Pseudomonas aeruginosa, and two Gram-positive bacterial strains, Baci...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.12839

    authors： Li HX,Wang ZC,Qian YM,Yan XQ,Lu YD,Zhu HL

    更新日期：2017-01-01 00:00:00

  • Design and synthesis of a novel peptide for selective detection of cancer cells.

    abstract：:Using a minimalist approach, an 11-residue peptide (Peptide 1) tagged with rhodamine fluorophore was designed and synthesized for selective detection of cancer cells. Peptide 1 contains RGD and NGR motifs to bind, respectively, integrins and aminopeptidase CD13, which are over expressed in cancer cells. Surface tensio...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.13675

    authors： Rajavenkatesh K,Padmaja M,Janani I,Aishwarya S,Purna Sai K,Thennarasu S

    更新日期：2020-06-01 00:00:00

  • Design of (99m) Tc-DTPA-CLP and preliminary evaluation in rats.

    abstract：:Radiopharmaceuticals are localized in (malignant) tumor tissues by different mechanisms. One of these mechanisms, gelatinase enzyme activity, is associated with poor prognosis in cancer patients and potential targets for tumor imaging. There are some gelatinases to be associated with metastatic potential for tumor ima...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.12253

    authors： Altıparmak B,Lambrecht FY,Er O

    更新日期：2014-03-01 00:00:00

  • The design, synthesis and potential utility of fluorescence probes that target DFG-out conformation of p38alpha for high throughput screening binding assay.

    abstract：:The design, synthesis and utility of fluorescence probes that bind to the DFG-out conformation of p38alpha kinase are described. Probes that demonstrate good affinity for p38alpha, have been identified and one of the probes, PF-04438255, has been successfully used in an high throughput screening (HTS) assay to identif...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2009.00884.x

    authors： Tecle H,Feru F,Liu H,Kuhn C,Rennie G,Morris M,Shao J,Cheng AC,Gikunju D,Miret J,Coli R,Xi SH,Clugston SL,Low S,Kazmirski S,Ding YH,Cao Q,Johnson TL,Deshmukh GD,DiNitto JP,Wu JC,English JM

    更新日期：2009-12-01 00:00:00

  • A natural language processing approach based on embedding deep learning from heterogeneous compounds for quantitative structure-activity relationship modeling.

    abstract：:Over the past decade, rapid development in biological and chemical technologies such as high-throughput screening, parallel synthesis, has been significantly increased the amount of data, which requires the creation and the integration of new analytical methods, especially deep learning models. Recently, there is an i...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.13742

    authors： Bouhedjar K,Boukelia A,Khorief Nacereddine A,Boucheham A,Belaidi A,Djerourou A

    更新日期：2020-09-01 00:00:00

  • On the origins of enzyme inhibitor selectivity and promiscuity: a case study of protein kinase binding to staurosporine.

    abstract：:Relationships between ligand binding and the shapes of the binding sites in families of homologous enzymes are investigated by comparing matrices of distances between key binding site atoms. Multiple linear regression is used to help identify key distances that influence ligand binding affinity. In order to illustrate...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2009.00832.x

    authors： Tanramluk D,Schreyer A,Pitt WR,Blundell TL

    更新日期：2009-07-01 00:00:00

  • Applications of machine-learning methods for the discovery of NDM-1 inhibitors.

    abstract：:The emergence of New Delhi metal beta-lactamase (NDM-1)-producing bacteria and their worldwide spread pose great challenges for the treatment of drug-resistant bacterial infections. These bacteria can hydrolyze most β-lactam antibacterials. Unfortunately, there are no clinically useful NDM-1 inhibitors. In the current...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.13708

    authors： Shi C,Dong F,Zhao G,Zhu N,Lao X,Zheng H

    更新日期：2020-11-01 00:00:00

  • Structure and activity of CPNGRC: a modified CD13/APN peptidic homing motif.

    abstract：:Asn-Gly-Arg peptides have been designed as vehicles for the delivery of chemotherapeutics, magnetic resonance imaging contrast agents, and fluorescence labels to tumor cells, and cardiac angiogenic tissue. Specificity is derived via an interaction with aminopeptidase N, also known as CD13, a cell surface receptor that...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2010.00974.x

    authors： Plesniak LA,Salzameda B,Hinderberger H,Regan E,Kahn J,Mills SA,Teriete P,Yao Y,Jennings P,Marassi F,Adams JA

    更新日期：2010-06-01 00:00:00

  • Conformational movement of F251 contributes to the molecular mechanism of constitutive activation in the C5a receptor.

    abstract：:The activation mechanism of G-protein-coupled receptors triggered upon binding of a ligand represents a very important 'conformational switch' in the biological array of signal transduction. However, the molecular and functional details for this activation switch remain unknown. Random saturation mutagenesis data on t...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2008.00630.x

    authors： Sen S,Baranski TJ,Nikiforovich GV

    更新日期：2008-03-01 00:00:00

  • The Binding Mode Prediction and Similar Ligand Potency in the Active Site of Vitamin D Receptor with QM/MM Interaction, MESP, and MD Simulation.

    abstract：:Non-secosteroidal ligands are well-known vitamin D receptor (VDR) agonists. In this study, we described a combined QM/MM to define the protein-ligand interaction energy a strong positive correlation in both QM-MM interaction energy and binding free energy against the biological activity. The molecular dynamics simulat...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.12754

    authors： Selvaraman N,Selvam SK,Muthusamy K

    更新日期：2016-08-01 00:00:00

  • A light-activated beta-turn scaffold within a somatostatin analog: NMR structure and biological activity.

    abstract：:Somatostatin owes its biological activity to the presence of a well-defined beta-turn centered around the tetrapeptide Phe-Trp-Lys-Thr. We have developed a light-activated beta-turn scaffold, 1, with the ability to template a beta-turn conformation within the somatostatin tetrapeptide only upon photolysis. The three-d...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2005.00337.x

    authors： Ulysse LG Jr,Chmielewski J

    更新日期：2006-02-01 00:00:00

  • Antibacterial and antitubercular evaluation of dihydronaphthalenone-indole hybrid analogs.

    abstract：:A new series of indole appended dihydronaphthalenone hybrid analogs (5a-t) have been synthesized through the Lewis acid catalyzed Michael addition of indoles to the arylidene/hetero arylidene ketones. All the synthesized derivatives are well characterized through the 1 H-NMR, 13 C-NMR, HRMS spectroscopic techniques, c...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.12990

    authors： V PK,J R,C T FS,K T A,S Keri R,Varughese S,Balappa Somappa S

    更新日期：2017-11-01 00:00:00

  • Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.

    abstract：:Alzheimer's disease onset and progression are associated with the dysregulation of multiple and complex physiological processes, and a successful therapeutic approach should therefore address more than one target. In line with this modern paradigm, a series of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene analogs (4a-q) w...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/cbdd.12732

    authors： Shaik JB,Palaka BK,Penumala M,Eadlapalli S,Darla Mark M,Ampasala DR,Vadde R,Amooru Gangaiah D

    更新日期：2016-07-01 00:00:00

  • Interaction of a curcumin analogue dimethoxycurcumin with DNA.

    abstract：:Dimethoxycurcumin (Dimc), a synthetic analogue of curcumin, that has been reported to exhibit better in vivo stability and anti-tumour activity, was investigated for its interaction with DNA, employing spectroscopic methods based on absorption, fluorescence, circular dichroism (CD), ethidium bromide (EtBr) competitive...

    journal_title：Chemical biology & drug design

    pub_type： 杂志文章

    doi：10.1111/j.1747-0285.2011.01083.x

    authors： Kunwar A,Simon E,Singh U,Chittela RK,Sharma D,Sandur SK,Priyadarsini IK

    更新日期：2011-04-01 00:00:00