Journal
CHEMCATCHEM
Volume 11, Issue 5, Pages 1425-1430Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cctc.201801994
Keywords
allostery; Kemp elimination; protein design; calmodulin; Nuclear Magnetic Resonance
Categories
Funding
- NIH [GM119634, RR016461, OD012254, GM103499]
- NSF [1332349, 1750462, 1229559]
- College of Charleston [Summer Undergraduate Research with Faculty grants]
- Howard Hughes Medical Institute [52007537]
- Ralph E. Powe Junior Enhancement Awards
- Nappi Family Award
- Alexander von Humboldt Foundation
- Direct For Biological Sciences
- Div Of Molecular and Cellular Bioscience [1750462] Funding Source: National Science Foundation
- Division Of Chemistry
- Direct For Mathematical & Physical Scien [1229559] Funding Source: National Science Foundation
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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 immunosuppressor 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(a).
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