Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Ariel S. Gross"'
Publikováno v:
Biochemical Pharmacology. 68:231-237
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-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::243e36c67d265147a7b1367aad486e58
https://doi.org/10.1016/j.bcp.2004.02.039
https://doi.org/10.1016/j.bcp.2004.02.039
Autor:
Philippe Van Rompaey, Brian A Harris, Michihiro Ohno, Susanna Tchilibon, Ariel S. Gross, Zhan-Guo Gao, Heng T. Duong, Serge Van Calenbergh, Kenneth A. Jacobson, Soo-Kyung Kim
Publikováno v:
Bioorganic & Medicinal Chemistry. 12:2995-3007
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 bind
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::46f967c152b57e1c4e2de9c8365b1329
https://doi.org/10.1016/j.bmc.2004.03.031
https://doi.org/10.1016/j.bmc.2004.03.031
Publikováno v:
Biochemical Pharmacology. 65:1675-1684
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5298b7edc90048220b528172e6b512e4
https://doi.org/10.1016/s0006-2952(03)00153-9
https://doi.org/10.1016/s0006-2952(03)00153-9
Autor:
Kenneth A. Jacobson, Joshua B. Blaustein, Zhan-Guo Gao, Aishe Chen, Soo-Kyung Kim, Ariel S. Gross
Publikováno v:
Molecular Pharmacology. 63:1021-1031
We examined the effects on allosteric modulation and ligand binding of the mutation of amino acid residues of the human A(3) adenosine receptor (A(3)AR) that are hypothesized to be near one of three loci: the putative sodium binding site, the putativ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::19f4fc792c8b3df977328e916d8e0cfd
https://doi.org/10.1124/mol.63.5.1021
https://doi.org/10.1124/mol.63.5.1021
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 rec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31875794138fdc6f3395f529e0dadd45
https://europepmc.org/articles/PMC4367543/
https://europepmc.org/articles/PMC4367543/
Autor:
Juan B. Rodriguez, Hyung Ryong Moon, Zhan-Guo Gao, Liaman K. Mamedova, Won Jun Choi, Eleonora Elhalem, Maria Julieta Comin, Dae Hong Shin, Kenneth A. Jacobson, Lak Shin Jeong, Ariel S. Gross, Hea Ok Kim, Neli Melman
We have found previously that structural features of adenosine derivatives, particularly at the N6- and 2-positions of adenine, determine the intrinsic efficacy as A3 adenosine receptor (AR) agonists. Here, we have probed this phenomenon with respect
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0faaa40214da4d5e33c6332716e0be3b
https://www.sciencedirect.com/science/article/pii/S0006295203008190
https://www.sciencedirect.com/science/article/pii/S0006295203008190
Autor:
Susanna Tchilibon, Joshua B. Blaustein, Zhan-Guo Gao, Kenneth A. Jacobson, Heng T. Duong, Brian A Harris, Soo-Kyung Kim, Ariel S. Gross, Neli Melman
Publikováno v:
Bioorganicmedicinal chemistry. 12(9)
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 Ki value of 0.63 nM. The effects of these structural changes on affinity at human and rat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b88fb8c4c9321d37e566c6479c1ae38e
https://pubmed.ncbi.nlm.nih.gov/15080906
https://pubmed.ncbi.nlm.nih.gov/15080906
Autor:
Zhan-Guo Gao, Serge Van Calenbergh, Philippe Van Rompaey, Kenneth A. Jacobson, Soo-Kyung Kim, Aishe Chen, Ariel S. Gross
Publikováno v:
Journal of medicinal chemistry. 46(23)
A three-dimensional model of the human A(2A) adenosine receptor (AR) and its docked ligands was built by homology to rhodopsin and validated with site-directed mutagenesis and the synthesis of chemically complementary agonists. Different binding mode
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b80ae9525d14502bfa1c116e7302792c
https://pubmed.ncbi.nlm.nih.gov/14584936
https://pubmed.ncbi.nlm.nih.gov/14584936