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Biotech / Medical : KDUS, who knows this company? -- Ignore unavailable to you. Want to Upgrade?

To: scaram(o)uche who wrote (108)	9/16/1999 12:59:00 PM
From: scaram(o)uche	Respond to of 117

Bioorg Med Chem Lett 1999 Aug 16;9(16):2413-8 Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays. Campbell RM, Cartwright C, Chen W, Chen Y, Duzic E, Fu JM, Loveland M, Manning R, McKibben B, Pleiman CM, Silverman L, Trueheart J, Webb DR, Wilkinson V, Witter DJ, Xie X, Castelhano AL Cadus Pharmaceutical Corporation, Tarrytown, NY 10591, USA. [Medline record in process] 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.

To: scaram(o)uche who wrote (108)	9/16/1999 1:03:00 PM
From: scaram(o)uche	Read Replies (1) \| Respond to of 117

Nat Biotechnol 1999 Sep;17(9):878-83 Genetic screens in yeast to identify mammalian nonreceptor modulators of G-protein signaling. Cismowski MJ, Takesono A, Ma C, Lizano JS, Xie X, Fuernkranz H, Lanier SM, Duzic E Department of Pharmacology, Medical University of South Carolina, 171 Ashley Ave., Charleston, SC 29425, USA. [Medline record in process] We describe genetic screens in Saccharomyces cerevisiae designed to identify mammalian nonreceptor modulators of G-protein signaling pathways. Strains lacking a pheromone-responsive G-protein coupled receptor and expressing a mammalian-yeast Galpha hybrid protein were made conditional for growth upon either pheromone pathway activation (activator screen) or pheromone pathway inactivation (inhibitor screen). Mammalian cDNAs that conferred plasmid-dependent growth under restrictive conditions were identified. One of the cDNAs identified from the activator screen, a human Ras-related G protein that we term AGS1 (for activator of G-protein signaling), appears to function by facilitating guanosine triphosphate (GTP) exchange on the heterotrimeric Galpha. A cDNA product identified from the inhibitor screen encodes a previously identified regulator of G-protein signaling, human RGS5.