Two drug candidates were tested in a cell-based assay. Addition of drug candidate 1 resulted in an increase in intracellular cAMP. Addition of drug candidate 2 also resulted in an increase in cAMP Chemical and structural analysis indicated that both drug candidates have a doubly hydroxylated benzene ring that is connected to a linear -C(OHH)-C(H2)-NH-CH3 tail. Interestingly, drug candidate 1 produced even more dramatic increases in cAMP levels when co-administered with a cyclic nucleotide phosphodiesterase inhibitor. This effect was not observed for drug candidate 2. Addition of drug candidate 1 also increased the phosphorylation status of key cellular signaling proteins. This effect was not observed for drug candidate 2. Based on this data and material presented in lecture, what receptor do you think drug candidate 1 is acting on? Do you think drug candidate 2 is acting on the same receptor. Assuming satisfaction of the Lipinski rules reliably predicts oral bio-availability, would you predict drug candidate 1 to be orally active? Please support your answers with facts and logical arguments. subject: computitional biochemistry
Two drug candidates were tested in a cell-based assay. Addition of drug candidate 1 resulted in an increase in intracellular cAMP. Addition of drug candidate 2 also resulted in an increase in cAMP Chemical and structural analysis indicated that both drug candidates have a doubly hydroxylated benzene ring that is connected to a linear -C(OHH)-C(H2)-NH-CH3 tail. Interestingly, drug candidate 1 produced even more dramatic increases in cAMP levels when co-administered with a cyclic nucleotide phosphodiesterase inhibitor. This effect was not observed for drug candidate 2. Addition of drug candidate 1 also increased the phosphorylation status of key cellular signaling proteins. This effect was not observed for drug candidate 2. Based on this data and material presented in lecture, what receptor do you think drug candidate 1 is acting on? Do you think drug candidate 2 is acting on the same receptor. Assuming satisfaction of the Lipinski rules reliably predicts oral bio-availability, would you predict drug candidate 1 to be orally active? Please support your answers with facts and logical arguments. subject: computitional biochemistry
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