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KAHA ligation as a platform for the rapid discovery of Protein Tyrosine phosphatase 1B (PTP1B) inhibitors
We have successfully designed and assembled a 66-member library of protein tyrosine phosphatases (PTP) inhibitor candidates using α-ketoacid-hydroxylamine (KAHA) ligation. Subsequent in situ enzymatic screening revealed a potent hit (IC50 = 1.67 μM) against PTP1B, which displayed 6.8- to 50-fold selectivity over other phosphatases. © 2024 Elsevier Inc.
Authors : Tian J.; Tan S.; Gao L.; Rajamani L.; Srinivasan R.
Source : Academic Press Inc.
Article Information
| Year | 2025 |
| Type | Article |
| DOI | 10.1016/j.bioorg.2024.108028 |
| ISSN | 00452068 |
| Volume | 154 |
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