Kemp Eliminases of the AlleyCat Family Possess High Substrate Promiscuity.

TitleKemp Eliminases of the AlleyCat Family Possess High Substrate Promiscuity.
Publication TypeJournal Article
Year of Publication2019
AuthorsCaselle, E. A., J. H. Yoon, S. Bhattacharya, J. J. L. Rempillo, Z. Lengyel, A. D'Souza, Y. S. Moroz, P. L. Tolbert, A. N. Volkov, M. Forconi, C. A. CastaƱeda, O. V. Makhlynets, and I. V. Korendovych
JournalChemCatChem
Volume11
Issue5
Pagination1425-1430
Date Published2019 Mar 06
ISSN1867-3880
Abstract

Minimalist enzymes designed to catalyze model reactions provide useful starting points for creating catalysts for practically important chemical transformations. We have shown that Kemp eliminases of the AlleyCat family facilitate conversion of leflunomide (an immunosupressor pro-drug) to its active form teriflunomide with outstanding rate enhancement (nearly four orders of magnitude) and catalytic proficiency (more than seven orders of magnitude) without any additional optimization. This remarkable activity is achieved by properly positioning the substrate in close proximity to the catalytic glutamate with very high pK.

DOI10.1002/cctc.201801994
Alternate JournalChemCatChem
PubMed ID31788134
PubMed Central IDPMC6884320
Grant ListR35 GM119634 / GM / NIGMS NIH HHS / United States
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