Academic Journal
1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2).
| العنوان: | 1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2). |
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| المؤلفون: | Röhrig, U.F., Majjigapu, S.R., Caldelari, D., Dilek, N., Reichenbach, P., Ascencao, K., Irving, M., Coukos, G., Vogel, P., Zoete, V., Michielin, O. |
| المصدر: | Bioorganic & medicinal chemistry letters, vol. 26, no. 17, pp. 4330-4333 |
| سنة النشر: | 2016 |
| المجموعة: | Université de Lausanne (UNIL): Serval - Serveur académique lausannois |
| مصطلحات موضوعية: | Cancer immunotherapy, Cellular assays, Indoleamine 2,3-dioxygenase, Molecular modeling, Tryptophan metabolism |
| الوصف: | Indoleamine 2,3-dioxygenase 2 (IDO2) is a potential therapeutic target for the treatment of diseases that involve immune escape such as cancer. In contrast to IDO1, only a very limited number of inhibitors have been described for IDO2 due to inherent difficulties in expressing and purifying a functionally active, soluble form of the enzyme. Starting from our previously discovered highly efficient 4-aryl-1,2,3-triazole IDO1 inhibitor scaffold, we used computational structure-based methods to design inhibitors of IDO2 which we then tested in cellular assays. Our approach yielded low molecular weight inhibitors of IDO2, the most active displaying an IC50 value of 51μM for mIDO2, and twofold selectivity over hIDO1. These compounds could be useful as molecular probes to investigate the biological role of IDO2, and could inspire the design of new IDO2 inhibitors. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| Relation: | info:eu-repo/semantics/altIdentifier/pmid/27469130; info:eu-repo/semantics/altIdentifier/eissn/1464-3405; https://serval.unil.ch/notice/serval:BIB_9DF2682ECDFF |
| DOI: | 10.1016/j.bmcl.2016.07.031 |
| الاتاحة: | https://serval.unil.ch/notice/serval:BIB_9DF2682ECDFF https://doi.org/10.1016/j.bmcl.2016.07.031 |
| رقم الانضمام: | edsbas.3BD237C0 |
| قاعدة البيانات: | BASE |
| DOI: | 10.1016/j.bmcl.2016.07.031 |
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