US5438119A
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US
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Method of obtaining a peptide with desired target property
Assignee: University of California, San Diego
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Filing: 1992-11-25
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Granted: 1995-08-01
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Expires: 2012-11-25
Abstract
Abstract A method to obtain selected individual peptides or families thereof which have a target property and optionally to determine the amino acid sequence of a selected peptide or peptides to permit synthesis in practical quantities is disclosed. In general outline, the method of the invention comprises synthesizing a mixture of randomly or deliberately generated peptides using standard synthesis techniques, but adjusting the individual concentrations of the components of a mixture of sequentially added amino acids according to the coupling constants for each amino acid/amino acid coupling. The subgroup of peptides having the target property can then be selected, and either each peptide isolated and sequenced, or analysis performed on the mixture to permit its composition to be reproduced. Also included in the invention is an efficient method to determine the relevant coupling constants.
Inventors
- 👤 William J. Rutter
- 👤 Daniel V. Santi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 16:00
CPC Classifications
C; C07; C07K; C07K1/00; C07K1/04; C07K1/047; C07K1/14; C07K1/36; G; G01; G01N; G01N33/00; G01N33/48; G01N33/50; G01N33/68
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
112 words
A method of obtaining a peptide having a desired target property, comprising the steps of: providing a mixture of candidate peptides containing 8,000 or more different peptides of distinct, unique and different amino acid sequences, wherein the presence of each peptide in the mixture is predetermined, each peptide is present in the mixture in retrievable and analyzable amounts and the mixture includes at least one biologically active peptide in a retrievable and analyzable amount; and selecting from among the mixture of candidate peptides a peptide having a desired target property by exposing the mixture of candidate peptides to a substance to which the peptide having a desired target property will preferentially bind.
Claim 2
Independent Claim
112 words
A method of obtaining a peptide having a desired target property, comprising the steps of: providing a mixture of candidate peptides containing 8,000 or more different peptides of distinct, unique and different amino acid sequences, wherein the presence of each peptide in the mixture is predetermined, each peptide is present in the mixture in retrievable and analyzable amounts and the mixture includes at least one biologically active peptide in a retrievable and analyzable amount; and selecting from among the mixture of candidate peptides a peptide having a desired target property by exposing the mixture of candidate peptides to a substance to which the peptide having a desired target property will preferentially bind.
Claim 3
Dependent Claim
19 words
The method as claimed in claim 1, further comprising: isolating the selected candidate peptide having the desired target property.
Claim 4
Dependent Claim
19 words
The method as claimed in claim 2, further comprising: identifying the isolated candidate peptide having the desired target property.
Claim 5
Dependent Claim
45 words
The method as claimed in claim 1, wherein the mixture of candidate peptides contains 160,000 or more different peptides of distinct, unique and different amino acid sequences, each in retrievable and analyzable amounts, and wherein the presence of each peptide in the mixture is predetermined.
Claim 6
Dependent Claim
45 words
The method as claimed in claim 1, wherein the mixture of candidate peptides contains 3,200,000 or more different peptides of distinct, unique and different amino acid sequences, each in retrievable and analyzable amounts, and wherein the presence of each peptide in the mixture is predetermined.
Claim 7
Dependent Claim
45 words
The method as claimed in claim 1, wherein the mixture of candidate peptides contains 64,000,000 or more different peptides of distinct, unique and different amino acid sequences, each in retrievable and analyzable amounts, and wherein the presence of each peptide in the mixture is predetermined.
Claim 8
Independent Claim
98 words
A method of obtaining a peptide having a desired target property, comprising the steps of: providing a mixture of candidate peptides containing 8,000 or more different peptides of distinct, unique and different amino acid sequences, wherein the presence of each peptide in the mixture is predetermined and each peptide is present in an amount such that each peptide is analyzable; and selecting from among the mixture of candidate peptides a peptide having a desired target property by exposing the mixture of candidate peptides to a substance to which the peptide having a desired target property will preferentially bind.
Claim 9
Independent Claim
98 words
A method of obtaining a peptide having a desired target property, comprising the steps of: providing a mixture of candidate peptides containing 8,000 or more different peptides of distinct, unique and different amino acid sequences, wherein the presence of each peptide in the mixture is predetermined and each peptide is present in an amount such that each peptide is analyzable; and selecting from among the mixture of candidate peptides a peptide having a desired target property by exposing the mixture of candidate peptides to a substance to which the peptide having a desired target property will preferentially bind.
Claim 10
Dependent Claim
19 words
The method as claimed in claim 7, further comprising: isolating the selected candidate peptide having the desired target property.
Claim 11
Dependent Claim
19 words
The method as claimed in claim 8, further comprising: identifying the isolated candidate peptide having the desired target property.
Claim 12
Dependent Claim
19 words
The method as claimed in claim 7, wherein the mixture of candidate peptides contains 160,000 or more different peptides.
Claim 13
Dependent Claim
19 words
The method as claimed in claim 7, wherein the mixture of candidate peptides contains 3,200,000 or more different peptides.
Claim 14
Dependent Claim
19 words
The method as claimed in claim 7, wherein the mixture of candidate peptides contains 64,000,000 or more different peptides.
Claim 15
Independent Claim
118 words
A method of obtaining a peptide having a desired target property comprising: a) synthesizing a mixture of peptides by reacting a predetermined amount of an activated amino acid residue with an acceptor amino acid or peptide in a manner so as to obtain a mixture of peptides containing 8,000 or more different peptides of distinct, unique and different amino acid sequences wherein the presence of each peptide in the mixture is predetermined, each peptide is present in the mixture in retrievable and analyzable amounts; and b) selecting peptides having one or more desired target properties by exposing the mixture of peptides to a substance to which the peptides having one or more desired target properties will preferentially bind.
Claim 16
Independent Claim
118 words
A method of obtaining a peptide having a desired target property comprising: a) synthesizing a mixture of peptides by reacting a predetermined amount of an activated amino acid residue with an acceptor amino acid or peptide in a manner so as to obtain a mixture of peptides containing 8,000 or more different peptides of distinct, unique and different amino acid sequences wherein the presence of each peptide in the mixture is predetermined, each peptide is present in the mixture in retrievable and analyzable amounts; and b) selecting peptides having one or more desired target properties by exposing the mixture of peptides to a substance to which the peptides having one or more desired target properties will preferentially bind.
Claim 17
Dependent Claim
17 words
The method of claim 13 wherein the peptide mixture contains 160,000 or more peptides in known quantities.
Claim 18
Dependent Claim
17 words
The method of claim 14 wherein the peptide mixture contains 3,200,000 or more peptides in known quantities.
Claim 19
Dependent Claim
17 words
The method of claim 15 wherein the peptide mixture contains 64,000,000 or more peptides in known quantities.
Claim 20
Independent Claim
110 words
A method of obtaining a peptide having a desired target property comprising: a) combining and reacting activated amino acids with an acceptor amino acid or peptide, wherein the concentration of activated amino acid added is varied depending on its coupling constant so as to obtain a candidate mixture of peptides wherein each peptide of the candidate mixture is present in a predicted and analyzable amount; b) selecting peptides having one or more desired target properties by exposing the candidate mixture to a substance to which the peptide having one or more desired target properties will bind; and c) isolating peptides which selectively bind to the substance from the candidate mixture.
Claim 21
Independent Claim
110 words
A method of obtaining a peptide having a desired target property comprising: a) combining and reacting activated amino acids with an acceptor amino acid or peptide, wherein the concentration of activated amino acid added is varied depending on its coupling constant so as to obtain a candidate mixture of peptides wherein each peptide of the candidate mixture is present in a predicted and analyzable amount; b) selecting peptides having one or more desired target properties by exposing the candidate mixture to a substance to which the peptide having one or more desired target properties will bind; and c) isolating peptides which selectively bind to the substance from the candidate mixture.
Claim 22
Dependent Claim
32 words
The method of claim 17, wherein selecting step b) is further comprised of a second selection step, such that the resulting selected peptides exhibit a greater degree of the desired target property.
Claim 23
Independent Claim
104 words
A method of obtaining a peptide ligand from a candidate mixture of peptides, said peptide ligand being a ligand of a given target molecule, comprising: a) combining and reacting activated amino acids with an acceptor amino acid or peptide, wherein the concentration of activated amino acid added is varied depending on its coupling constant, such that each peptide of the candidate mixture is present in a predicted and analyzable amount; and b) isolating peptides having an increased affinity to the target molecule by exposing the candidate mixture to a substance to which peptides having an increased affinity to the target molecule will preferentially bind.
Claim 24
Independent Claim
104 words
A method of obtaining a peptide ligand from a candidate mixture of peptides, said peptide ligand being a ligand of a given target molecule, comprising: a) combining and reacting activated amino acids with an acceptor amino acid or peptide, wherein the concentration of activated amino acid added is varied depending on its coupling constant, such that each peptide of the candidate mixture is present in a predicted and analyzable amount; and b) isolating peptides having an increased affinity to the target molecule by exposing the candidate mixture to a substance to which peptides having an increased affinity to the target molecule will preferentially bind.
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