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1. WO2020107118 - GENETICALLY-ENCODED MACROCYCLIC PEPTIDE LIBRARIES BEARING A PHARMACOPHORE

Publication Number WO/2020/107118
Publication Date 04.06.2020
International Application No. PCT/CA2019/051703
International Filing Date 28.11.2019
IPC
C07K 7/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
7Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04Linear peptides containing only normal peptide links
06having 5 to 11 amino acids
C07K 1/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
C07K 1/107 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
107by chemical modification of precursor peptides
C12N 15/11 2006.01
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09Recombinant DNA-technology
11DNA or RNA fragments; Modified forms thereof
C40B 30/04 2006.01
CCHEMISTRY; METALLURGY
40COMBINATORIAL TECHNOLOGY
BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
30Methods of screening libraries
04by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
C40B 40/02 2006.01
CCHEMISTRY; METALLURGY
40COMBINATORIAL TECHNOLOGY
BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
40Libraries per se, e.g. arrays, mixtures
02Libraries contained in or displayed by microorganisms, e.g. bacteria or animal cells; Libraries contained in or displayed by vectors, e.g. plasmids; Libraries containing only microorganisms or vectors
CPC
C07K 1/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
C07K 1/107
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
107by chemical modification of precursor peptides
C07K 7/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
7Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04Linear peptides containing only normal peptide links
06having 5 to 11 amino acids
C12N 15/11
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09Recombinant DNA-technology
11DNA or RNA fragments; Modified forms thereof
C40B 30/04
CCHEMISTRY; METALLURGY
40COMBINATORIAL TECHNOLOGY
BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
30Methods of screening libraries
04by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
C40B 40/02
CCHEMISTRY; METALLURGY
40COMBINATORIAL TECHNOLOGY
BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
40Libraries per se, e.g. arrays, mixtures
02Libraries contained in or displayed by microorganisms, e.g. bacteria or animal cells; Libraries contained in or displayed by vectors, e.g. plasmids; Libraries containing only microorganisms or vectors
Applicants
  • THE GOVERNORS OF THE UNIVERSITY OF ALBERTA [CA]/[CA]
Inventors
  • DERDA, Ratmir
  • MUKHERJEE, Raja
  • EKANAYAKE, Arunika
Agents
  • BENNETT JONES LLP
  • YOO, Edward
Priority Data
62/772,33928.11.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) GENETICALLY-ENCODED MACROCYCLIC PEPTIDE LIBRARIES BEARING A PHARMACOPHORE
(FR) BANQUES PEPTIDIQUES MACROCYCLIQUES GÉNÉTIQUEMENT CODÉS PORTANT UN PHARMACOPHORE
Abstract
(EN)
The present invention relates to a method of forming a macrocyclic peptide bearing a pharmacophore and said produced macrocyclic peptide, wherein the method comprises the steps of: reacting a peptide with two thiol groups of cysteine side chains with the reactive compound 1,5 -dichloropentanedion-2,4. The reaction between the reactive compound and the peptide produces an 1,3 -diketone-containing macrocyclic polypeptide. The macrocycle with a 1,3 -diketone group is then modified by reaction of said macrocycle with an alkyl or aryl hydrazine group bearing a pharmacophore in benign aqueous conditions. The macrocycles may be displayed in a library, such as a phage display library, and used to biopan for affinity against a selected target.
(FR)
La présente invention concerne un procédé de formation d'un peptide macrocyclique portant un pharmacophore ainsi que ledit peptide macrocyclique produit, le procédé comprenant les étapes consistant à : faire réagir un peptide ayant deux groupes thiol à chaînes latérales de cystéine avec un composé réactif 1,5-dichloropentanedion-2,4. La réaction entre le composé réactif et le peptide produit un polypeptide macrocyclique contenant 1,3-dicétone. Le macrocycle ayant un groupe 1,3-dicétone est ensuite modifié par mise en réaction dudit macrocycle avec un groupe alkyle ou aryle hydrazine portant un pharmacophore dans des conditions aqueuses bénignes. Les macrocycles peuvent figurer dans une banque, telle qu'une banque à exposition sur phage, et utilisés pour effectuer une biopsie permettant une affinité vis-à-vis d'une cible sélectionnée.
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