Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale

Autor: Habeshian, Sevan, Merz, Manuel Leonardo, Sangouard, Gontran, Mothukuri, Ganesh Kumar, Schüttel, Mischa, Bognár, Zsolt, Díaz-Perlas, Cristina, Vesin, Jonathan, Bortoli Chapalay, Julien, Turcatti, Gerardo, Cendron, Laura, Angelini, Alessandro, Heinis, Christian

Macrocycles have excellent potential as therapeutics due to their ability to bind challenging targets. However, generating macrocycles against new targets is hindered by a lack of large macrocycle libraries for high-throughput screening. To overcome

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::048daad1467d5a487d6e7712be123622
http://hdl.handle.net/10278/3762388

Macrocycle synthesis strategy based on step-wise "adding and reacting" three components enables screening of large combinatorial libraries.

Autor: Mothukuri, Ganesh K., Kale, Sangram S., Stenbratt, Carl L., Zorzi, Alessandro, Vesin, Jonathan, Bortoli Chapalay, Julien, Deyle, Kaycie, Turcatti, Gerardo, Cendron, Laura, Angelini, Alessandro, Heinis, Christian

Publikováno v: Chemical Science; 8/14/2020, Vol. 11 Issue 30, p7858-7863, 6p

Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale.

Autor: Habeshian S; Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015, Lausanne, Switzerland., Merz ML; Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015, Lausanne, Switzerland., Sangouard G; Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015, Lausanne, Switzerland., Mothukuri GK; Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015, Lausanne, Switzerland., Schüttel M; Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015, Lausanne, Switzerland., Bognár Z; Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015, Lausanne, Switzerland., Díaz-Perlas C; Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015, Lausanne, Switzerland., Vesin J; Biomolecular Screening Facility, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland., Bortoli Chapalay J; Biomolecular Screening Facility, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland., Turcatti G; Biomolecular Screening Facility, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland., Cendron L; Department of Biology, University of Padova, 35131, Padova, Italy., Angelini A; Department of Molecular Sciences and Nanosystems, Ca' Foscari University of Venice, Via Torino 155, Venezia Mestre, Venice, 30172, Italy.; European Centre for Living Technologies (ECLT), Ca' Bottacin, Dorsoduro 3911, Calle Crosera, Venice, 30124, Italy., Heinis C; Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015, Lausanne, Switzerland. christian.heinis@epfl.ch.

Publikováno v: Nature communications [Nat Commun] 2022 Jul 02; Vol. 13 (1), pp. 3823. Date of Electronic Publication: 2022 Jul 02.