Pub. Date : 2019 Dec 27
PMID : 31809044
7 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Synthesis and PTP Inhibitory Activity of Illudalic Acid and Its Methyl Ether, with Insights into Selectivity for LAR PTP over Other Tyrosine Phosphatases under Physiologically Relevant Conditions. | illudalic acid | protein tyrosine phosphatase receptor type F | Homo sapiens |
| 2 | Synthesis and PTP inhibitory activity of illudalic acid and its methyl ether are described, with a focus on selective inhibition of LAR PTP relative to a small collection of other representative PTPs. | illudalic acid | protein tyrosine phosphatase receptor type F | Homo sapiens |
| 3 | Illudalic acid dose-dependently (measured IC50 = 2.1 +- 0.2 muM) and time-dependently inhibits LAR consistent with previous reports of covalent binding. | illudalic acid | protein tyrosine phosphatase receptor type F | Homo sapiens |
| 4 | The kinetics of LAR inhibition by illudalic acid are consistent with a two-step mechanism in which the inhibitor and enzyme first interact noncovalently (KI = 130 +- 50 muM), followed by covalent ligation at a rate kinact = 1.3 +- 0.4 min-1. | illudalic acid | protein tyrosine phosphatase receptor type F | Homo sapiens |
| 5 | The phenol methyl ether of illudalic acid was found to be less potent in our dose-response assays (measured IC50 = 55 +- 6 muM) but more selective for LAR, with a weaker initial noncovalent interaction and faster covalent ligation of LAR as compared to illudalic acid itself. | illudalic acid | protein tyrosine phosphatase receptor type F | Homo sapiens |
| 6 | The phenol methyl ether of illudalic acid was found to be less potent in our dose-response assays (measured IC50 = 55 +- 6 muM) but more selective for LAR, with a weaker initial noncovalent interaction and faster covalent ligation of LAR as compared to illudalic acid itself. | illudalic acid | protein tyrosine phosphatase receptor type F | Homo sapiens |
| 7 | These observations collectively help inform further development of illudalic acid analogues as potent and selective inhibitors of the LAR subfamily of tyrosine phosphatases. | illudalic acid | protein tyrosine phosphatase receptor type F | Homo sapiens |