PL EN


Preferencje help
Widoczny [Schowaj] Abstrakt
Liczba wyników
2013 | 60 | 4 |
Tytuł artykułu

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

Treść / Zawartość
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
  • Baldi L, Hacker DL, Adam M, Wurm FM (2007) Recombinant protein production by large-scale transient gene expression in mammalian cells: state of the art and future perspectives. Biotechnol Lett 29: 677-684. 
  • Benson DA, Cavanaugh M, Clark K, Karsch-Mizrachi I, Lipman DJ, Ostell J, Sayers EW (2013) GenBank. Nucleic Acids Res 41: D36-D42. 
  • Cepko C, Pear W (2001) Overview of the retrovirus transduction system. Curr Protoc Mol Biol 36: 9.9.1-9.9.16. 
  • Cheng YC, Prusoff WH (1973) Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22: 3099-3108. 
  • Gazi L, Bobirnac I, Danzeisen M, Schüpbach E, Langenegger D, Sommer B, Hoyer D, Tricklebank M, Schoeffter P (1999) Receptor density as a factor governing the efficacy of the dopamine D4 receptor ligands, L-745,870 and U-101958 at human recombinant D4.4 receptors expressed in CHO cells. Br J Pharmacol 128: 613-620. 
  • Haack KKV, McCarty NA (2011) Functional consequences of GPCR heterodimerization: GPCRs as allosteric modulators. Pharmaceuticals 4: 509-523.
  • 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. 
  • Kenakin T (1996) The classification of seven transmembrane receptors in recombinant expression systems. Pharmacol Rev 48: 413-463. 
  • Kenakin T (1997) Differences between natural and recombinant G protein-coupled receptor systems with varying receptor/G protein stoichiometry. Trends Pharmacol Sci 18: 456-464. 
  • Kottke T, Sander K, Weizel L, Schneider EH, Seifert R, Stark H (2011) Receptor-specific functional efficacies of alkyl imidazoles as dual histamine H3/H4 receptor ligands. Eur J Pharmacol 654: 200-208. 
  • 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. 
  • Morgenstern JP, Land H (1990) Advanced mammalian gene transfer: high titer retroviral vectors with multiple drug selection markers and a complementary helper-free packaging cell line. Nucleic Acids Res 18: 3587-3590.  
  • Nash MS, Selkirk JV, Gaymer CE, Challiss RA, Nahorski SR (2001) Enhanced inducible mGlu1alpha receptor expression in Chinese hamster ovary cells. J Neurochem 77: 1664-1667. 
  • 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. 
  • Smits R, Leurs R, de Esch IJ (2009) Major advances in the development of histamine H4 receptor ligands. Drug Discov Today 14: 745-753. 
  • Tiligada E, Zampeli E, Sander K, Stark H (2009) Histamine H3 and H4 receptors as novel drug targets. Expert Opin Investig Drugs 18: 1519-1531. 
  • Zampeli E, Tiligada E (2009) The role of histamine H4 receptor in immune and inflammatory disorders. Br J Pharmacol 157: 24-33. 
Typ dokumentu
Bibliografia
Identyfikatory
Identyfikator YADDA
bwmeta1.element.agro-5bd0849a-e8cf-4918-b921-e712cedd1322
JavaScript jest wyłączony w Twojej przeglądarce internetowej. Włącz go, a następnie odśwież stronę, aby móc w pełni z niej korzystać.