Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.

R M Campbell; C Cartwright; W Chen; Y Chen; E Duzic; J M Fu; M Loveland; R Manning; B McKibben; C M Pleiman; L Silverman; J Trueheart; D R Webb; V Wilkinson; D J Witter; X Xie; A L Castelhano

doi:10.1016/s0960-894x(99)00398-4

PubMed · 10476879

Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.

R M Campbell·C Cartwright·W Chen·Y Chen·E Duzic·J M Fu·M Loveland·R Manning·B McKibben·C M Pleiman·L Silverman·J Trueheart·D R Webb·V Wilkinson·D J Witter·X Xie·A L Castelhano

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Abstract

Evaluation of a biased "library" of pyrrolo[2,3-d]pyrimidines using yeast-based functional assays expressing human A1- and A2a-adenosine receptors, led to the A1 selective antagonist 4b. A direct correlation between yeast functional activity and binding data was established. Practical compounds with polar residues at C-4 of the pyrrolopyrimidine system required H-bond donor functionality for high potency.

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Binding, Competitive Cell Line Humans Hydrogen Bonding Purinergic P1 Receptor Antagonists Pyrimidines Radioligand Assay Receptors, Purinergic P1 Recombinant Proteins Saccharomyces cerevisiae Journal Article

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R M Campbell, C Cartwright, W Chen, Y Chen, E Duzic, J M Fu, M Loveland, R Manning, B McKibben, C M Pleiman, L Silverman, J Trueheart, D R Webb, V Wilkinson, D J Witter, X Xie, A L Castelhano. 1999-08-16. Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.. https://doi.org/10.1016/s0960-894x(99)00398-4

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