Ariel S. Gross

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Exploring human adenosine A3 receptor complementarity and activity for adenosine analogues modified in the ribose and purine moiety

Philippe Van Rompaey, Kenneth A. Jacobson, Ariel S. Gross, Zhan-Guo Gao, more

Bioorganic & Medicinal Chemistry > 2005 > 13 > 4 > 973-983

In this paper we investigated the influence on affinity, selectivity and intrinsic activity upon modification of the adenosine agonist scaffold at the 3′- and 5′-positions of the ribofuranosyl moiety and the 2- and N ⁶ -positions of the purine base. This resulted in the synthesis of various analogues, that is, 3–12 and 24–33, with good hA ₃ AR selectivity and moderate-to-high affinities...

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2,2'-Pyridylisatogen tosylate antagonizes P2Y ₁ receptor signaling without affecting nucleotide binding

Zhan-Guo Gao, Liaman Mamedova, Susanna Tchilibon, Ariel S. Gross, more

Biochemical Pharmacology > 2004 > 68 > 2 > 231-237

The effect of 2,2'-pyridylisatogen tosylate (PIT) on the human P2Y ₁ receptor and on other recombinant P2Y receptors has been studied. We first examined the modulation by PIT of the agonist-induced accumulation of inositol phosphates. PIT blocked 2-methylthio-ADP (2-MeSADP)-induced accumulation of inositol phosphates in 1321N1 astrocytoma cells stably expressing human P2Y ₁ receptors...

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Modulation of adenosine receptor affinity and intrinsic efficacy in adenine nucleosides substituted at the 2-position

Michihiro Ohno, Zhan-Guo Gao, Philippe Van Rompaey, Susanna Tchilibon, more

Bioorganic & Medicinal Chemistry > 2004 > 12 > 11 > 2995-3007

We studied the structural determinants of binding affinity and efficacy of adenosine receptor (AR) agonists. Substituents at the 2-position of adenosine were combined with N ⁶ -substitutions known to enhance human A ₃ AR affinity. Selectivity of binding of the analogues and their functional effects on cAMP production were studied using recombinant human A ₁ , A ₂ _A...

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Effects of the allosteric modulator SCH-202676 on adenosine and P2Y receptors

Zhan-Guo Gao, Ariel S. Gross, Kenneth A. Jacobson

Life Sciences > 2004 > 74 > 25 > 3173-3180

The G protein-coupled receptor allosteric modulator SCH-202676 (N-(2,3-diphenyl-1,2,4-thiadiazol-5-(2H)-ylidene)methanamine), which affects a wide range of structurally unrelated G protein-coupled receptors, has highly divergent effects on purine receptors. SCH-202676 inhibited radioligand binding to human adenosine A ₁ , A ₂ _A , and A ₃ receptors (IC ₅ ₀ =...

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Exploring distal regions of the A ₃ adenosine receptor binding site: sterically constrained N ⁶ -(2-phenylethyl)adenosine derivatives as potent ligands

Susanna Tchilibon, Soo-Kyung Kim, Zhan-Guo Gao, Brian A. Harris, more

Bioorganic & Medicinal Chemistry > 2004 > 12 > 9 > 2021-2034

We synthesized phenyl ring-substituted analogues of N ⁶ -(1S,2R)-(2-phenyl-1-cyclopropyl)adenosine, which is highly potent in binding to the human A ₃ AR with a K _i value of 0.63nM. The effects of these structural changes on affinity at human and rat adenosine receptors and on intrinsic efficacy at the hA ₃ AR were measured. A 3-nitrophenyl analogue was resolved chromatographically...

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Structural determinants of efficacy at A ₃ adenosine receptors: modification of the ribose moiety

Zhan-Guo Gao, Lak Shin Jeong, Hyung Ryong Moon, Hea Ok Kim, more

Biochemical Pharmacology > 2004 > 67 > 5 > 893-901

We have found previously that structural features of adenosine derivatives, particularly at the N ⁶ - and 2-positions of adenine, determine the intrinsic efficacy as A ₃ adenosine receptor (AR) agonists. Here, we have probed this phenomenon with respect to the ribose moiety using a series of ribose-modified adenosine derivatives, examining binding affinity and activation of the human...

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Structure-activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A ₃ receptor antagonists

Kwan-Young Jung, Soo-Kyung Kim, Zhan-Guo Gao, Ariel S. Gross, more

Bioorganic & Medicinal Chemistry > 2004 > 12 > 3 > 613-623

4-(4-Methoxyphenyl)-2-aminothiazole and 3-(4-methoxyphenyl)-5-aminothiadiazole derivatives have been synthesized and evaluated as selective antagonists for human adenosine A ₃ receptors. A methoxy group in the 4-position of the phenyl ring and N-acetyl or propionyl substitutions of the aminothiazole and aminothiadiazole templates displayed great increases of binding affinity and selectivity...

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Modeling the Adenosine Receptors: Comparison of the Binding Domains of A _2A Agonists and Antagonists

Soo-Kyung Kim, Zhan-Guo Gao, Philippe Van Rompaey, Ariel S. Gross, more

Journal of Medicinal Chemistry > 2003 > 46 > 23 > 4847 - 4859

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N ⁶ -Substituted adenosine derivatives: selectivity, efficacy, and species differences at A ₃ adenosine receptors

Zhan-Guo Gao, Joshua B. Blaustein, Ariel S. Gross, Neli Melman, more

Biochemical Pharmacology > 2003 > 65 > 10 > 1675-1684

The activation of the human A ₃ adenosine receptor (AR) by a wide range of N ⁶ -substituted adenosine derivatives was studied in intact CHO cells stably expressing this receptor. Selectivity of binding at rat and human ARs was also determined. Among N ⁶ -alkyl substitutions, small N ⁶ -alkyl groups were associated with selectivity for human A ₃ ARs vs. rat A...

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Search results for: Ariel S. Gross

Exploring human adenosine A3 receptor complementarity and activity for adenosine analogues modified in the ribose and purine moiety

2,2'-Pyridylisatogen tosylate antagonizes P2Y ₁ receptor signaling without affecting nucleotide binding

Modulation of adenosine receptor affinity and intrinsic efficacy in adenine nucleosides substituted at the 2-position

Effects of the allosteric modulator SCH-202676 on adenosine and P2Y receptors

Exploring distal regions of the A ₃ adenosine receptor binding site: sterically constrained N ⁶ -(2-phenylethyl)adenosine derivatives as potent ligands

Structural determinants of efficacy at A ₃ adenosine receptors: modification of the ribose moiety

Structure-activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A ₃ receptor antagonists

Modeling the Adenosine Receptors: Comparison of the Binding Domains of A _2A Agonists and Antagonists

N ⁶ -Substituted adenosine derivatives: selectivity, efficacy, and species differences at A ₃ adenosine receptors

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