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10 results on '"Ahn, Sang Yeop"'

1. Structural Modification and Biological Evaluation of 2,8-Disubstituted Adenine and Its Nucleosides as A2A Adenosine Receptor Antagonists: Exploring the Roles of Ribose at Adenosine Receptors

Author

Kim, Gibae, primary, Jarhad, Dnyandev B., additional, Lee, Grim, additional, Kim, Gyudong, additional, Hou, Xiyan, additional, Yu, Jinha, additional, Lee, Chang Soo, additional, Warnick, Eugene, additional, Gao, Zhan-Guo, additional, Ahn, Sang Yeop, additional, Kwak, Dongik, additional, Park, Kichul, additional, Lee, Summer Dabin, additional, Park, Tae-uk, additional, Jung, So-young, additional, Lee, Jong Hyun, additional, Choi, Jong-Ryoul, additional, Kim, Myeongjoong, additional, Kim, Donghyun, additional, Kim, Bongtae, additional, Jacobson, Kenneth A., additional, and Jeong, Lak Shin, additional

Published
2024
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2. Structural Modification and Biological Evaluation of 2,8-Disubstituted Adenine and Its Nucleosides as A2A Adenosine Receptor Antagonists: Exploring the Roles of Ribose at Adenosine Receptors.

Author

Kim, Gibae, Jarhad, Dnyandev B., Lee, Grim, Kim, Gyudong, Hou, Xiyan, Yu, Jinha, Lee, Chang Soo, Warnick, Eugene, Gao, Zhan-Guo, Ahn, Sang Yeop, Kwak, Dongik, Park, Kichul, Lee, Summer Dabin, Park, Tae-uk, Jung, So-young, Lee, Jong Hyun, Choi, Jong-Ryoul, Kim, Myeongjoong, Kim, Donghyun, and Kim, Bongtae

Published
2024
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5. Structural Modification and Biological Evaluation of 2,8-Disubstituted Adenine and Its Nucleosides as A2AAdenosine Receptor Antagonists: Exploring the Roles of Ribose at Adenosine Receptors

Author

Kim, Gibae, Jarhad, Dnyandev B., Lee, Grim, Kim, Gyudong, Hou, Xiyan, Yu, Jinha, Lee, Chang Soo, Warnick, Eugene, Gao, Zhan-Guo, Ahn, Sang Yeop, Kwak, Dongik, Park, Kichul, Lee, Summer Dabin, Park, Tae-uk, Jung, So-young, Lee, Jong Hyun, Choi, Jong-Ryoul, Kim, Myeongjoong, Kim, Donghyun, Kim, Bongtae, Jacobson, Kenneth A., and Jeong, Lak Shin

Abstract

Building on the preceding structural analysis and a structure–activity relationship (SAR) of 8-aryl-2-hexynyl nucleoside hA2AAR antagonist 2a, we strategically inverted C2/C8 substituents and eliminated the ribose moiety. These modifications aimed to mitigate potential steric interactions between ribose and adenosine receptors. The SAR findings indicated that such inversions significantly modulated hA3AR binding affinities depending on the type of ribose, whereas removal of ribose altered the functional efficacy via hA2AAR. Among the synthesized derivatives, 2-aryl-8-hexynyl adenine 4ademonstrated the highest selectivity for hA2AAR (Ki,hA2A= 5.0 ± 0.5 nM, Ki,hA3/Ki,hA2A= 86) and effectively blocked cAMP production and restored IL-2 secretion in PBMCs. Favorable pharmacokinetic properties and a notable enhancement of anticancer effects in combination with an mAb immune checkpoint blockade were observed upon oral administration of 4a. These findings establish 4aas a viable immune-oncology therapeutic candidate.

Published
2024
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10. Structural Modification and Biological Evaluation of 2,8-Disubstituted Adenine and Its Nucleosides as A 2A Adenosine Receptor Antagonists: Exploring the Roles of Ribose at Adenosine Receptors.

Author

Kim G, Jarhad DB, Lee G, Kim G, Hou X, Yu J, Lee CS, Warnick E, Gao ZG, Ahn SY, Kwak D, Park K, Lee SD, Park TU, Jung SY, Lee JH, Choi JR, Kim M, Kim D, Kim B, Jacobson KA, and Jeong LS

Subjects
Humans, Structure-Activity Relationship, Animals, Mice, Molecular Structure, Rats, Female, Cell Line, Tumor, Adenine pharmacology, Adenine chemistry, Adenine analogs & derivatives, Adenosine A2 Receptor Antagonists pharmacology, Adenosine A2 Receptor Antagonists chemistry, Adenosine A2 Receptor Antagonists chemical synthesis, Nucleosides chemistry, Nucleosides pharmacology, Nucleosides chemical synthesis, Ribose chemistry, Ribose metabolism, Receptor, Adenosine A2A metabolism
Abstract

Building on the preceding structural analysis and a structure-activity relationship (SAR) of 8-aryl-2-hexynyl nucleoside hA 2A AR antagonist 2a , we strategically inverted C2/C8 substituents and eliminated the ribose moiety. These modifications aimed to mitigate potential steric interactions between ribose and adenosine receptors. The SAR findings indicated that such inversions significantly modulated hA 3 AR binding affinities depending on the type of ribose, whereas removal of ribose altered the functional efficacy via hA 2A AR. Among the synthesized derivatives, 2-aryl-8-hexynyl adenine 4a demonstrated the highest selectivity for hA 2A AR ( K i ,hA2A = 5.0 ± 0.5 nM, K i ,hA3 / K i ,hA2A = 86) and effectively blocked cAMP production and restored IL-2 secretion in PBMCs. Favorable pharmacokinetic properties and a notable enhancement of anticancer effects in combination with an mAb immune checkpoint blockade were observed upon oral administration of 4a . These findings establish 4a as a viable immune-oncology therapeutic candidate.

Published
2024
Full Text
View/download PDF

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