[EN] METHODS FOR SELECTIVELY MODIFYING AMINO ACIDS AND PRODUCTS MADE THEREBY<br/>[FR] PROCÉDÉS DE MODIFICATION SÉLECTIVE D'ACIDES AMINÉS ET PRODUITS FABRIQUÉS PAR CEUX-CI
申请人:UNIV CALIFORNIA
公开号:WO2021007127A1
公开(公告)日:2021-01-14
Disclosed herein are methods for the selective substitution of a hydrogen bonded to a carbon atom (e.g., a hydrogen of an aliphatic methylene group) of a compound, which comprise contacting the compound with a substituent in the presence of a BesD halogenase.
Fluorinated somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin and the Lys side chain is monofluorinated in the .gamma. or .delta. positions. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.
Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of hydrazine compounds of formula (I) wherein the variables R
1
-R
9
are defined herein.
A fully automated, user-independent method is described for computer-mediated interpretation of data derived by mass spectrometry of an experimental peptide to identify and characterize a corresponding peptide sequence in a peptide database. The method identifies the corresponding sequence if it is present in the database, without the need for a skilled observer to choose from amongst a list of possible matches. By using an automated back-read process, the present method can uniquely identify a corresponding peptide sequence in a database based on a single matching peptide sequence. The method also permits mapping of mass spectral data to sequences in peptide or nucleotide databases for unambiguous identification of exons; determining a correct reading frame; identifying artefacts and errors in sequences; identifying mutations and polymorphisms; identifying post-translational modifications; and identifying exon-intron boundaries.
The present invention provides: a protein having dipeptide-synthesizing activity or a protein for dipeptide synthesis; DNA encoding the protein having dipeptide-synthesizing activity or the protein for dipeptide synthesis; a recombinant DNA comprising the DNA; a transformant carrying the recombinant DNA; a process for producing the protein having dipeptide-synthesizing activity; an enzymatic process for producing a dipeptide using the protein having dipeptide-synthesizing activity or the protein for dipeptide synthesis; and a process for producing a dipeptide using, as an enzyme source, a culture of a microorganism or a transformant having the ability to produce the protein having dipeptide-synthesizing activity or the protein for dipeptide synthesis, or the like.