Chemical genomics: massively parallel technologies for rapid lead identification and target validation.


:Chemical genomics is a new research paradigm with importantapplications in drug discovery. It links genomic targets withsmall-molecule chemistries thereby allowing for efficient targetvalidation and lead compound identification. ACADIA'schemical-genomics platform consists of a large and diverse small-moleculelibrary (800,000), a reference drug library (2,000), druggablegenomic targets (>300) and a cell-based functional assaytechnology (R-SAT(TM); Receptor Selection and AmplificationTechnology) that allows for ultra-high throughput screening(>500,000 data points/week) as well as high throughputpharmacology and profiling over a wide range of targets. Twoexamples are presented that illustrate the success of ourchemical-genomics approach: (i) The validation of inverse agonismat serotonin 5-HT(2A) receptors as an antipsychotic mechanismand the subsequent discovery of potent and selectively acting 5-HT(2A) inverse agonists, currently in preclinical development,and (ii) the discovery of the first ectopically binding subtype-selective muscarinic m1 agonist.






Hacksell U,Nash N,Burstein ES,Piu F,Croston G,Brann MR




Has Abstract


2002-01-01 00:00:00












  • Evaluation of monitoring approaches and effects of culture conditions on recombinant protein production in baculovirus-infected insect cells.

    abstract::The baculovirus infection process of Spodoptera frugiperda (Sf9) insect cells in oxygen-controlled bioreactors in serum-free medium was investigated using a recombinant Autographa californica (AcNPV) virus expressing beta-galactosidase enzyme as a model system. A variety of monitoring techniques including trypan blue ...


    pub_type: 杂志文章


    authors: Hensler WT,Agathos SN

    更新日期:1994-01-01 00:00:00

  • The influence of drinking-water pollution with heavy metal on the expression of IL-4 and IFN-γ in mice by real-time polymerase chain reaction.

    abstract::In recent years, water pollution has been converted to a challenging discussion in health area of human being. Heavy elements are one of the most important water pollutants and their negative adverse effects on body systems have been confirmed. In this study, investigation of effects of two heavy elements including le...


    pub_type: 杂志文章


    authors: Radbin R,Vahedi F,Chamani J

    更新日期:2014-10-01 00:00:00

  • Effect of purine supplementation on the growth of salmonid cell lines in different mammalian sera.

    abstract::The Chinook salmon embryo cell line, CHSE-214, grew well in fetal bovine serum (FBS) but poorly in dialyzed (d) FBS. Purines restored most but not all growth-promoting activity to dFBS, which suggests that purines account for a large portion of the dialyzable fraction's growth-promoting activity. CHSE-214 died in newb...


    pub_type: 杂志文章


    authors: Ganassin RC,Bols NC

    更新日期:1992-01-01 00:00:00

  • MicroRNAs: recently discovered key regulators of proliferation and apoptosis in animal cells : Identification of miRNAs regulating growth and survival.

    abstract::The relatively recent discovery of miRNAs has added a completely new dimension to the study of the regulation of gene expression. The mechanism of action of miRNAs, the conservation between diverse species and the fact that each miRNA can regulate a number of targets and phenotypes clearly indicates the importance of ...


    pub_type: 杂志文章


    authors: Gammell P

    更新日期:2007-04-01 00:00:00

  • Expression of anchorin CII mRNA by cultured chondrocytes.

    abstract::The establishment of a cell culture system promoting chondrocyte differentiation has been utilized to better characterize phenotypic stages of chondrogenesis at the cellular level. Although the expression of the type II collagen gene has been studied during "in vitro" chondrocyte differentiation, little is known about...


    pub_type: 杂志文章


    authors: Castagnola P,Cancedda R

    更新日期:1991-02-01 00:00:00

  • Erythropoietin processing in erythropoietic system and central nervous system.

    abstract::We describe possible functions of carbohydrates attached to growth factors and strategies to examine the functions, concentrating on erythropoietin, a major regulator of erythropoiesis. Erythropoietin in erythropoiesis functions as an endocrine hormone; it is produced by kidney cells and transferred into the circulati...


    pub_type: 杂志文章


    authors: Nagao M,Masuda S,Ueda M,Sasaki R

    更新日期:1995-01-01 00:00:00

  • A modification of tooth germ cultivation in vitro and in ovo.

    abstract::Mandibular molar anlages excised from 17-day mouse foetuses were cultured in vitro or in ovo (on the chorioallantoic membrane). In both cases, the explants were underlain either with a Millipore filter or with a piece of fibrin foam. Tooth germs were harvested after 7 days of cultivation and processed histologically. ...


    pub_type: 杂志文章


    authors: Peterka M,Mandys V,Peterková R

    更新日期:1991-09-01 00:00:00

  • A simple method for in situ freezing of anchorage-dependent cells including rat liver parenchymal cells.

    abstract::We developed a simple method for freezing anchorage-dependent cells, including primary cultured rat liver parenchymal cells, without detaching the cells from the culture dish. The method consists of preculture of the cells to confluence, changing the growth medium to a conventional freezing medium, packaging in a cont...


    pub_type: 杂志文章


    authors: Ohno T,Saijo-Kurita K,Miyamoto-Eimori N,Kurose T,Aoki Y,Yosimura S

    更新日期:1991-03-01 00:00:00

  • Neurite outgrowth promoting activity of marine algae from Japan against rat adrenal medulla pheochromocytoma cell line, PC12D.

    abstract::We screened for biological activity which induces neurite outgrowth in vitro from 300 species of marine algae from along the Japan coast for possible use as a treatment for the lack of neurotrophic factor which is considered to be a cause of Alzheimer's disease. In this study, we evaluated the neurite outgrowth promot...


    pub_type: 杂志文章


    authors: Kamei Y,Sagara A

    更新日期:2002-11-01 00:00:00

  • Modeling of cell culture processes.

    abstract::Models of cell processes can be particularly useful in simulating, optimizing and controlling cell culture systems. Models reported in the literature are of various degrees of biological structure and mathematical complexity and describe cell growth, death, metabolism, and product formation, alone or in combination wi...


    pub_type: 杂志文章,评审


    authors: Tziampazis E,Sambanis A

    更新日期:1994-01-01 00:00:00

  • Osteogenic differentiation of human placenta-derived mesenchymal stem cells (PMSCs) on electrospun nanofiber meshes.

    abstract::Numerous challenges remain in the successful clinical translation of cell-based therapeutic studies for skeletal tissue repair, including appropriate cell sources and viable cell delivery systems. Poly(ethylene glycol)-poly(ε-caprolactone) (PEG-PCL) amphiphilic block copolymers have been extensively explored in micros...


    pub_type: 杂志文章


    authors: Zhang D,Tong A,Zhou L,Fang F,Guo G

    更新日期:2012-12-01 00:00:00

  • Cytogenetic effects of nine Helichrysum taxa in human lymphocytes culture.

    abstract::Helichrysum Mill. (Asteraceae) species have been used in folk medicine for thousands of years in the world. The in vitro cytogenetic effects in human lymphocytes of nine Helichrysum taxa used in Turkey folk medicine were investigated. Blood samples were obtained from healthy donors, non-smoking volunteers, which were ...


    pub_type: 杂志文章


    authors: Eroğlu HE,Aksoy A,Hamzaoğlu E,Budak U,Albayrak S

    更新日期:2009-01-01 00:00:00

  • Molecular mechanisms of Bombyx batryticatus ethanol extract inducing gastric cancer SGC-7901 cells apoptosis.

    abstract::Bombyx batryticatus is a traditional Chinese medicine. To understand apoptotic effect of B. batryticatus ethanol extract (BBE), we investigated the role of BBE in inducing apoptosis of human gastric cancer cells SGC-7901. Cells treated with BBE and apoptosis was assessed by methyl thiazolyl tetrazolium (MTT) assay, mo...


    pub_type: 杂志文章


    authors: Wu JY,Sheikho A,Ma H,Li TC,Zhao YQ,Zhang YL,Wang D

    更新日期:2017-12-01 00:00:00

  • Genotypic and phenotypic changes of BHK-21 cells grown in suspension cultures.

    abstract::The propagation of foot-and-mouth disease virus on BHK-21 suspension cells, although economically convenient, may yield a scarcely immunizing antigen. Helpful insights were obtained by investigating a few genotypic and phenotypic features of the cell cultures. The appearance of polyploid populations, higher cell conce...


    pub_type: 杂志文章


    authors: Amadori M,Berneri C

    更新日期:1993-01-01 00:00:00

  • Use of cell cultures, nuclear and radioanalytical techniques for metallotoxicological studies at the JRC-Ispra.

    abstract::This paper reviews the JRC-Ispra research activity on toxicological studies related to the environmental and occupational exposure of trace metals, as carried out by a combination of cell culture methodologies with nuclear and radioanalytical techniques.Applications concern the setting of uptake-effect relationships a...


    pub_type: 杂志文章


    authors: Sabbioni E,Pozzi G,Fischbach M,Bahbouth E

    更新日期:1993-01-01 00:00:00

  • Endogenous synthesis of prostacyclin was positively regulated during the maturation phase of cultured adipocytes.

    abstract::Prostacyclin alternatively called prostaglandin (PG) I2 is an unstable metabolite synthesized by the arachidonate cyclooxygenase pathway. Earlier studies have suggested that prostacyclin analogues can act as a potent effector of adipose differentiation. However, biosynthesis of PGI2 has not been determined comprehensi...


    pub_type: 杂志文章


    authors: Rahman MS,Khan F,Syeda PK,Nishimura K,Jisaka M,Nagaya T,Shono F,Yokota K

    更新日期:2014-08-01 00:00:00

  • High level expression of a frog alpha-amidating enzyme, AE-II, in cultured cells and silkworm larvae using a Bombyx mori nuclear polyhedrosis virus expression vector.

    abstract::A Xenopus laevis peptidyl C-terminal alpha-amidating enzyme (AE-II) gene, modified by deletion of a region encoding the putative membrane-spanning domain and the putative C-terminal cytosolic tail, was expressed in BoMo-15 AIIc insect cells and silkworm larvae using a Bombyx mori baculovirus expression vector system. ...


    pub_type: 杂志文章


    authors: Kobayashi J,Imanishi S,Inoue H,Ohsuye K,Yamaichi K,Tsuruoka N,Tanaka S

    更新日期:1992-01-01 00:00:00

  • Effects of passage number on growth and productivity of hybridoma secreting MRSA anti-PBP2a monoclonal antibodies.

    abstract::Monoclonal antibodies (mAb) are high added value glycoproteins recommended for immunotherapy, diagnosis, and also for the treatment of bacterial infections resistant to multiple drugs such as Methicillin Resistant Staphylococcus aureus (MRSA). In addition to environmental conditions related to cell cultures, the intri...


    pub_type: 杂志文章


    authors: Corrêa AL,Senna JP,de Sousa ÁP

    更新日期:2016-05-01 00:00:00

  • Synthesis, characterization and cytotoxicity of boron nitride nanoparticles: emphasis on toxicogenomics.

    abstract::Nanotechnology is increasingly developing area including more than 700 commercial products such as clothing, food preparation, cosmetics, mechanics, electronics and also health industry. People generally contact with nanoparticles by inhaling from air. Thus, it is becoming important issue to understand harmful effects...


    pub_type: 杂志文章


    authors: Türkez H,Arslan ME,Sönmez E,Açikyildiz M,Tatar A,Geyikoğlu F

    更新日期:2019-02-01 00:00:00

  • Formation of monoclonal antibody against a major ginseng component, ginsenoside Rb1 and its characterization.

    abstract::The ratio of hapten and bovine serum albumin in an antigen conjugate was determined by matrix-assisted laser desorption/ionization mass spectrometry. A hybridoma secreting monoclonal antibody against ginsenoside Rb1 was produced by fusing splenocytes immunized with a ginsenoside Rb1- bovine serum albumin conjugate wit...


    pub_type: 杂志文章


    authors: Tanaka H,Fukuda N,Shoyama Y

    更新日期:1999-03-01 00:00:00

  • Isolation, culture and differentiation of duck (Anas platyrhynchos) preadipocytes.

    abstract::In the present study, we isolated preadipocytes from the adipose tissue of Peking duck and subsequently cultured them in vitro. Cell counting kit-8 assay was employed to establish the growth curve of duck primary preadipocytes. Meanwhile, after the cells reaching full confluency, they were induced to differentiate int...


    pub_type: 杂志文章


    authors: Ding F,Li QQ,Li L,Gan C,Yuan X,Gou H,He H,Han CC,Wang JW

    更新日期:2015-10-01 00:00:00

  • Cell Culture Derived AgMNPV Bioinsecticide: Biological Constraints and Bioprocess Issues.

    abstract::We have studied parameters for optimizing the Spodoptera frugiperda (Sf9) cell culture and viral infection for the production of Anticarsia gemmatalis multiple nucleopolyhedrosis virus (AgMNPV) polyhedra inclusion bodies (PIBs) in shaker-Schott or spinner bottles and bioreactors. We have assayed the k(L)a of the syste...


    pub_type: 杂志文章


    authors: Rodas VM,Marques FH,Honda MT,Soares DM,Jorge SA,Antoniazzi MM,Medugno C,Castro ME,Ribeiro BM,Souza ML,Tonso A,Pereira CA

    更新日期:2005-06-01 00:00:00

  • Promoting effect of rapeseed proteins and peptides on Sf9 insect cell growth.

    abstract::The Baculovirus Expression Vector System has become widely used for the production of recombinant proteins for research and diagnostics. Serum-free culture media able to support high cell densities have been developed for the large scale culture of insect cells. While serum elimination aims at avoiding the risks assoc...


    pub_type: 杂志文章


    authors: Deparis V,Durrieu C,Schweizer M,Marc I,Goergen JL,Chevalot I,Marc A

    更新日期:2003-07-01 00:00:00

  • (-) Epigallocatechin gallate suppresses the differentiation of 3T3-L1 preadipocytes through transcription factors FoxO1 and SREBP1c.

    abstract::Tea catechin is one of the compounds that are closely related to obesity and insulin sensitivity. In order to determine the effect of catechin on adipocyte differentiation, we treated 3T3-L1 preadipocytes with different kinds of catechins. Our results showed that catechins, especially epigallocatechin gallate (EGCG), ...


    pub_type: 杂志文章


    authors: Kim H,Hiraishi A,Tsuchiya K,Sakamoto K

    更新日期:2010-07-01 00:00:00

  • Pig testis extract augments adiponectin expression and secretion through the peroxisome proliferator-activated receptor signaling pathway in 3T3-L1 adipocytes.

    abstract::Adiponectin is a key molecule whose upregulation may ameliorate symptoms of type 2 diabetes mellitus and disorders of lipid metabolism. Several plant-derived components have been shown to enhance adiponectin secretion; however, there have been no reports on the effects of animal-derived products. Therefore, in the cur...


    pub_type: 杂志文章


    authors: Kadooka K,Sato M,Matsumoto T,Kuhara S,Katakura Y,Fujimura T

    更新日期:2018-06-01 00:00:00

  • Anti-proliferative and apoptotic effects of oleuropein and hydroxytyrosol on human breast cancer MCF-7 cells.

    abstract::Olive oil intake has been shown to induce significant levels of apoptosis in various cancer cells. These anti-cancer properties are thought to be mediated by phenolic compounds present in olive. These beneficial health effects of olive have been attributed, at least in part, to the presence of oleuropein and hydroxyty...


    pub_type: 杂志文章


    authors: Han J,Talorete TP,Yamada P,Isoda H

    更新日期:2009-01-01 00:00:00

  • Effect of new rotenoid glycoside from the fruits of Amorpha fruticosa LINNE on the growth of human immune cells.

    abstract::A new compound, rotenoid isoflavone glycoside named, 6'-O-beta-D: -glucopyranosyl-12a-hydroxydalpanol was isolated from the methanolic (MeOH) fruit extract of Amorpha fruticosa LINNE by means of multi-stage column chromatography. Immuno-modulatory activities of this new glycoside were compared with the partitioned fra...


    pub_type: 杂志文章


    authors: Lee HJ,Kang HY,Kim CH,Kim HS,Kwon MC,Kim SM,Shin IS,Lee HY

    更新日期:2006-11-01 00:00:00

  • The isolation and characterization of putative mesenchymal stem cells from the spiny mouse.

    abstract::The bone marrow represents the most common source from which to isolate mesenchymal stem cells (MSCs). MSCs are capable of differentiating into tissues of the three primary lineages and have the potential to enhance repair in damaged organs through the principals of regenerative medicine. Given the ease with which MSC...


    pub_type: 杂志文章


    authors: Dickinson H,Milton P,Jenkin G

    更新日期:2012-10-01 00:00:00

  • Dielectric spectroscopy of mammalian cells. 2. Simultaneous in situ evaluation by aperture impedance pulse spectroscopy and low frequency dielectric spectroscopy of the biomass of HTC cells on Cytodex 3.

    abstract::Low-frequency dielectric spectroscopy has been used in situ, i.e. while the cells are still attached to their microsupport, to monitor the changes of biomass accompanying the growth of anchorage-dependent cells. This method, when compared to Aperture Impedance Pulse Spectroscopy (also called electronic sizing), is cha...


    pub_type: 杂志文章


    authors: Degouys V,Cerckel I,Garcia A,Harfield J,Dubois D,Fabry L,Miller AO

    更新日期:1993-01-01 00:00:00

  • Immunophenotypic comparison of heterogenous non-sorted versus sorted mononuclear cells from human umbilical cord blood: a novel cell enrichment approach.

    abstract::Human umbilical cord blood (hUCB) has been the preferred source of stem cells for the treatment of haematological malignancies and genetic disorders. This is primarily due to its non-invasiveness, high accessibility with relative ease of isolation. Still failures do prevail due to its heterogeneity and lesser frequenc...


    pub_type: 杂志文章


    authors: Indumathi S,Harikrishnan R,Rajkumar JS,Dhanasekaran M

    更新日期:2015-01-01 00:00:00