Academic Journal
Site-Selective Modification of Proteins with Oxetanes
| العنوان: | Site-Selective Modification of Proteins with Oxetanes |
|---|---|
| المؤلفون: | Boutureira, O., Martínez-Sáez, N., Brindle, K.M., Neves, A.A., Corzana, F., Bernardes, G.J.L. |
| سنة النشر: | 2017 |
| مصطلحات موضوعية: | antibodies, oxetanes, protein modifications, small oxygen heterocycles, sulfur |
| الوصف: | Oxetanes are four-membered ring oxygen heterocycles that are advantageously used in medicinal chemistry as modulators of physicochemical properties of small molecules. Herein, we present a simple method for the incorporation of oxetanes into proteins through chemoselective alkylation of cysteine. We demonstrate a broad substrate scope by reacting proteins used as apoptotic markers and in drug formulation, and a therapeutic antibody with a series of 3-oxetane bromides, enabling the identification of novel handles (S-to-S/N rigid, non-aromatic, and soluble linker) and reactivity modes (temporary cysteine protecting group), while maintaining their intrinsic activity. The possibility to conjugate oxetane motifs into full-length proteins has potential to identify novel drug candidates as the next-generation of peptide/protein therapeutics with improved physicochemical and biological properties. © 2017 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 0947-6539 |
| Relation: | info:eu-repo/semantics/altIdentifier/wos/WOS:000401160100002; info:eu-repo/semantics/altIdentifier/pissn/0947-6539; Site-Selective Modification of Proteins with Oxetanes, 2017, vol. 23, núm. 27, pág. 6483-6489; https://investigacion.unirioja.es/documentos/5bbc693bb750603269e81796; urn:issn:0947-6539 |
| DOI: | 10.1002/CHEM.201700745 |
| الاتاحة: | https://investigacion.unirioja.es/documentos/5bbc693bb750603269e81796 https://doi.org/10.1002/CHEM.201700745 |
| Rights: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.D14A3822 |
| قاعدة البيانات: | BASE |
| تدمد: | 09476539 |
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| DOI: | 10.1002/CHEM.201700745 |