Abstract：
:Thermodynamic parameters DeltaG degrees , DeltaH degrees and DeltaS degrees of the binding equilibrium of 12 ligands (six agonists and six antagonists) to the A(2B) adenosine receptor subtype have been determined by affinity measurements carried out on HEK 293 cells stably transfected with human A(2B) adenosine receptors at six different temperatures (4, 10, 15, 20, 25, 30 degrees C) and van't Hoff plot analysis have been performed. Affinity constants were obtained from saturation experiments of [(3)H]MRE 2029-F20 or by its displacement in inhibition assays for the other compounds. van't Hoff plots were essentially linear in the temperature range investigated, showing that the DeltaC(p) degrees of the binding equilibrium is nearly zero. Thermodynamic parameters are in the range 7< or =DeltaH degrees < or =23 kJ mol(-1)and 123< or =DeltaS degrees < or =219 JK(-1)mol(-1) for agonists and -40 < or =DeltaH degrees < or =-20 kJ mol(-1) and 10< or =DeltaS degrees < or =91 JK(-1)mol(-1) for antagonists indicating that agonistic binding is always totally entropy-driven while antagonistic binding is enthalpy and entropy-driven. In the -TDeltaS degrees versus DeltaH degrees plot the thermodynamic data are clearly arranged in separate clusters for agonists and antagonists, which, therefore, turn out to be thermodynamically discriminated.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Gessi S,Fogli E,Sacchetto V,Varani K,Merighi S,Leung E,Lennan SM,Borea PAdoi
10.1016/j.bcp.2007.09.003subject
Has Abstractpub_date
2008-01-15 00:00:00pages
562-9issue
2eissn
0006-2952issn
1873-2968pii
S0006-2952(07)00609-0journal_volume
75pub_type
杂志文章abstract：:The hypoxia-inducible factor-1 (HIF-1) is primarily involved in the sensing and adapting of cells to changes in the O2 level, which is essential for their viability. It is important that this critical transcription factor be tightly regulated in order for cells to respond to a wide range of O2 concentrations. HIF-1 re...
journal_title：Biochemical pharmacology
pub_type： 杂志文章,评审
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journal_title：Biochemical pharmacology
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pub_type： 杂志文章
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pub_type： 杂志文章
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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pub_type： 杂志文章
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更新日期：1991-07-15 00:00:00
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pub_type： 杂志文章
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