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2013 | 60 | 4 |

Tytuł artykułu

Development of novel cellular model for affinity studies of histamine H4 receptor ligands

Warianty tytułu

Języki publikacji

EN

Abstrakty

EN
The G protein-coupled histamine H4 receptor (H4R) is the last member of histamine receptors family discovered so far. Its expression pattern, together with postulated involvement in a wide variety of immunological and inflammatory processes make histamine H4 receptor an interesting target for drug development. Potential H4R ligands may provide an innovative therapies for different immuno-based diseases, including allergy, asthma, pruritus associated with allergy or autoimmune skin conditions, rheumatoid arthritis and pain. However, none of successfully developed selective and potent histamine H4 receptor ligands have been introduced to the market up to date. For that reason there is still a strong demand for pharmacological models to be used in studies on potent H4R ligands. In current work we present the development of novel mammalian cell line, stably expressing human histamine H4 receptor, with use of retroviral transduction approach. Obtained cell line was pharmacologically characterized in radioligand binding studies and its utility for affinity testing of potent receptor ligands was confirmed in comparative studies with the use of relevant insect cells expression model. Obtained results allow for statement that developed cellular model may be successfully employed in search for new compounds active at histamine H4 receptor.

Słowa kluczowe

Wydawca

-

Rocznik

Tom

60

Numer

4

Opis fizyczny

p.823-827,fig.,ref.

Twórcy

autor
  • Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Krakow, Poland
  • Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Krakow, Poland

Bibliografia

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  • Hermans E (2004) Generation of model cell lines expressing recombinant G-protein-coupled receptors. Methods Mol Biol 259: 137-153. 
  • Jablonowski J, Carruthers N, Thurmond R (2004) The histamine H4 receptor and potential therapeutic uses for H4 ligands. Mini Rev Med Chem 4: 993-1000. 
  • Karcz T, Handzlik J, Łażewska D, Kottke T, Seifert R, Kieć-Kononowicz K (2010) Search for histamine H4 receptor ligands in the group of 4-methylpiperazino amide derivatives. Inflamm Res 49: 243-245. 
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  • Leurs R, Chazot PL, Shenton FC, Lim HD, de Esch IJ (2009) Molecular and biochemical pharmacology of the histamine H4 receptor. Br J Pharmacol 157: 14-23. 
  • Markowitz D, Goff S, Bank A (1988) Construction and use of a safe and efficient amphotropic packaging cell line. Virology 167: 400-406. 
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  • Nguyen T, Shapiro DA, George SR, Setola V, Lee DK, Cheng R, Rauser L, Lee SP, Lynch KR, Roth BL, O'Dowd BF (2001) Discovery of a novel member of the histamine receptor family. Mol Pharmacol 59: 427-433. 
  • Sarramegna V, Talmont F, Demange P, Milon A (2003) Heterologous expression of G-protein-coupled receptors: comparison of expression systems from the standpoint of large-scale production and purification. Cell Mol Life Sci 60: 1529-1546. 
  • Schneider EH, Schnell D, Papa D, Seifert R (2009) High constitutive activity and a G-protein-independent high-affinity state of the human histamine H4 receptor. Biochemistry 48: 1424-1438. 
  • Siehler S (2008) Cell-based assays in GPCR drug discovery. Biotechnol J 3: 471-483. 
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Typ dokumentu

Bibliografia

Identyfikatory

Identyfikator YADDA

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