|Title||Kemp Eliminases of the AlleyCat Family Possess High Substrate Promiscuity.|
|Publication Type||Journal Article|
|Year of Publication||2019|
|Authors||Caselle, 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. Castañeda, O. V. Makhlynets, and I. V. Korendovych|
|Date Published||2019 Mar 06|
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.
|PubMed Central ID||PMC6884320|
|Grant List||R35 GM119634 / GM / NIGMS NIH HHS / United States|
Kemp Eliminases of the AlleyCat Family Possess High Substrate Promiscuity.