Biocatalysts for ezetimibe synthesis
US-9644189-B2 · May 9, 2017 · US
US10544400B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10544400-B2 |
| Application number | US-201816032319-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 11, 2018 |
| Priority date | May 4, 2010 |
| Publication date | Jan 28, 2020 |
| Grant date | Jan 28, 2020 |
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The present disclosure relates to non-naturally occurring polypeptides useful for preparing Ezetimibe, polynucleotides encoding the polypeptides, and methods of using the polypeptides.
Opening claim text (preview).
What is claimed is: 1. A non-naturally occurring ketoreductase polypeptide having ketoreductase activity, comprising an amino acid sequence that has at least 95% sequence identity to SEQ ID NO: 168, wherein the residue at position 190 is alanine, the residue at position 40 is arginine and the residue at position 64 is valine. 2. The non-naturally occurring ketoreductase polypeptide of claim 1 , wherein the amino acid sequence of said non-naturally occurring ketoreductase polypeptide further comprises one or more of the features selected from: the residue at position X93 is A and the residue at position X94 is T; the residue at position X93 is A and the residue at position X94 is P; the residue at position X93 is A and the residue at position X94 is S; or the residue at position X93 is I and the residue at position X94 is S. 3. The non-naturally occurring ketoreductase of claim 1 , wherein the amino acid sequence of said non-naturally occurring ketoreductase polypeptide further comprises one or more of the features selected from: the residue at position X203 is G; the residue at position X202 is G and the residue at position X203 is G; or the residue at position X201 is A, the residue position X202 is G and the residue at position X203 is G. 4. The non-naturally occurring ketoreductase claim 1 , wherein the amino acid sequence of said non-naturally occurring ketoreductase polypeptide further comprises one or more of the features selected from: the residue at position X196 is T; and the residue at position X199 is F. 5. The non-naturally occurring ketoreductase of claim 1 , wherein the amino acid sequence of said non-naturally occurring ketoreductase polypeptide further comprises one or more of the features selected from: the residue at position X21 is R or F; the residue at position X25 is R, T, or N; the residue at position X93 is A; the residue at position X94 is T, S, or P; the residue at position X95 is M, or V; the residue at position X96 is V, G, A, N, S, P, or T; the residue at position X99 is L; the residue at position X108 is H or K; the residue at position X117 is G; the residue at position X127 is K, or Q; the residue at position X147 is M, or I; the residue at position X148 is I; the residue at position X150 is H; the residue at position X152 is F, or N; the residue at position X155 is C; the residue at position X163 is I; the residue at position X195 is M; the residue at position X201 is I, L, or A; the residue at position X202 is L, N, V, or G; the residue at position X203 is G; the residue at position X204 is V, or A; the residue at position X205 is V; the residue at position X206 is I; the residue at position X207 is T, C, I, or N; the residue at position X211 is K; the residue at position X221 is D; the residue at position X223 is I; or the residue at position X226 is V.
Oxidoreductases acting on the CH-OH group of donors (1.1) · CPC title
Nitrogen as only ring hetero atom · CPC title
Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) · CPC title
Carbonyl reductase (NADPH) (1.1.1.184) · CPC title
acting on CH-OH groups as donors (1.1) · CPC title
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