| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371453 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
Abstract
The human T cell lymphotropic/leukemia virus type 1 (HTLV-I) causes adult T cell lymphoma/leukemia. The virus is also responsible for chronic progressive myelopathy and several inflammatory diseases. To stop the manufacturing of new viral components, in our previous reports, we derived small tetrapeptidic HTLV-I protease inhibitors with an important amide-capping moiety at the P3 residue. In the current study, we removed the P3-cap moiety and, with great difficulty, optimized the P3 residue for HTLV-I protease inhibition potency. We discovered a very potent and small tetrapeptidic HTLV-I protease inhibitor (KNI-10774a, IC50Â =Â 13Â nM).
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Authors
Jeffrey-Tri Nguyen, Keiko Kato, Henri-Obadja Kumada, Koushi Hidaka, Tooru Kimura, Yoshiaki Kiso,