US2003228274A1PendingUtilityA1
Polyamide chains of precise length
Est. expiryAug 28, 2018(expired)· nominal 20-yr term from priority
Inventors:Keith Rose
C08G 69/06C07K 1/1077C08G 69/00C08G 69/10C08G 73/10
43
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Claims
Abstract
Provided are chains of precise length and methods for their preparation. These chains are formed by the reaction of a derivative of a diacid and a diamine in a stepwise manner on a support. One of the reactants contains a water soluble oligomer, preferably polyethylene glycol. These chains are then used to chemically modify target macromolecules such as biologically important polypeptides.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A water soluble organic polyamide-based chain having a precise number of repeating units, said chain having the formula:
—{NH—Y—NH—CO—X—CO} n —{NH—Y′—NH} n′ —
wherein:
n is an integer from 1-100;
n′ is 0 or 1;
X and Y are divalent organic radicals lacking reactive functional groups or are absent and are the same or different, and can vary independently with each of said repeating units; and
Y′ is a divalent organic radical lacking reactive functional groups or is absent.
2 . The chain of claim 1 wherein one or more of the X and Y substituents are symmetrical radicals.
3 . The chain of claim 1 wherein at least one of the X and Y substituents contains 1 to 5 —CH 2 CH 2 O— groups.
4 . The chain of claim 1 wherein said divalent organic radicals are selected from the group consisting of substituted, unsubstituted, branched and linear, aliphatic and aromatic groups, and may optionally contain heteroatoms.
5 . The chain of claim 4 wherein said divalent organic radicals are selected from the group consisting of phenyl, C 1 -C 10 alkylene moieties, C 1 -C 10 alkyl groups, optionally containing heteroatoms, or a combination thereof.
6 . The chain of claim 5 wherein said divalent organic radicals are selected from the group consisting of —(CH 2 ) 2 —, —(CH 2 ) 6 —, —(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —, —[(CH 2 ) 3 —O—(CH 2 ) 2 —(CH 2 ) 2 —O—(CH 2 ) 3 ]—, —CH 2 —O—CH 2 — and —CH 2 —N(CH 3 )—CH 2 —.
7 . The chain of claim 1 having the formula:
—{NH—Y—NH—CO—X—CO} n —{NH—Y′—NH}—
8 . The chain of claim 7 having the formula:
—{NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—CO—(CH 2 ) 2 —CO} n ——{NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH}—
9 . The chain of claim 7 having the formula:
—{NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO——NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—CO—(CH 2 ) 2 —CO} z ——NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO—NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—
wherein z is an integer from 1-49.
10 . The chain of claim 1 having the formula:
—{NH—Y—NH—CO—X—CO} n —
11 . The chain of claim 10 having the formula:
—{NH—CH 2 —(CH 2 CH 2 O) 3 —(CH 2 ) 3 —NH—CO—(CH 2 ) 2 —CO} n —
12 . The chain of claim 10 having the formula:
—{NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO} n —
13 . The chain of claim 10 having the formula:
—{NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO——NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—CO—(CH 2 ) 2 —CO} n —
14 . A water soluble organic polyamide-based composition having a precise number of repeating units, said composition having the formula:
[U—{NH—Y—NH—CO—X—CO} n —{NH—Y′—NH} n′ ] q —V
wherein:
n is an integer from 1-100;
n′ is 0 or 1;
q is an integer from 1 to 10;
X and Y are divalent organic radicals lacking reactive functional groups or are absent and are the same or different, and can vary independently with each of said repeating units;
Y′ is a divalent organic radical lacking reactive functional groups or is absent;
V is selected from the group consisting of: a monovalent or multivalent target molecule whose properties are being modified or enhanced and having an optional divalent spacer or linker; a reporter group having a multivalent linker; a reactive group; and a terminal group having a multivalent linker, said terminal group being selected from the group consisting of —OH, —NH 2 , —H, and -Z-Q-support, where Z is a divalent spacer such as —NH—, —O— or may be absent, Q is a linker or a target molecule, and the support is a solid phase, matrix or surface; and
U is selected from the group consisting of: a target molecule whose properties are being modified or enhanced and having an optional divalent spacer or linker; a terminal group; a peptide chain; a protecting group; a support; and a reactive group.
15 . The composition of claim 14 wherein one or more of the X and Y substituents are symmetrical radicals.
16 . The composition of claim 14 wherein at least one of the X and Y substituents contains 1 to 5 —CH 2 CH 2 O— groups.
17 . The composition of claim 14 wherein said divalent organic radicals are selected from the group consisting of substituted, unsubstituted, branched and linear, aliphatic and aromatic groups, and may optionally contain heteroatoms.
18 . The composition of claim 17 wherein said divalent organic radicals are selected from the group consisting of phenyl, C 1 -C 10 alkylene moieties, C 1 -C 10 alkyl groups, optionally containing heteroatoms, or a combination thereof.
19 . The composition of claim 18 wherein said divalent organic radicals are selected from the group consisting of —(CH 2 ) 2 —, —(CH 2 ) 6 —, —(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —, —[(CH 2 ) 3 —O—(CH 2 ) 2 —(CH 2 ) 2 —O—(CH 2 ) 3 ]—, —CH 2 —O—CH 2 — and —CH 2 —N(CH 3 )—CH 2 —.
20 . The composition of claim 14 having the formula:
[U—{NH—Y—NH—CO—X—CO} n —{NH—Y′—NH}] q —V
21 . The composition of claim 20 having the formula:
[U—{NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—CO—(CH 2 ) 2 —CO} n ——{NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH}] q —V
22 . The composition of claim 20 having the formula:
[U—{NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO——NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—CO—(CH 2 ) 2 —CO} z ——NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO—NH (CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH] q —V
wherein z is an integer from 1-49.
23 . The composition of claim 14 having the formula:
[U—{NH—Y—NH—CO—X—CO} n ] q —V
24 . The composition of claim 23 having the formula:
[U—{NH—CH 2 —(CH 2 CH 2 O) 3 —(CH 2 ) 3 —NH—CO—(CH 2 ) 2 —CO} n ] q —V
25 . The composition of claim 23 having the formula:
[U—{NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO} n ] q —V
26 . The composition of claim 23 having the formula:
[U—{NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO——NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—CO—(CH 2 ) 2 —CO} n ] q —V
27 . The composition of claim 14 wherein said target molecule is selected from the group consisting of proteins, polypeptides, peptides, nucleic acids, liposomes, and therapeutic agents.
28 . The composition of claim 14 wherein said target molecule is a peptide selected from the group consisting of -GGLYACHMGPMTWVCQPLRG- (SEQ ID NO:1); -SVWRWLPYDKYE- (SEQ ID NO:3); and -ADGACRNPWC- (SEQ ID NO:6).
29 . A water soluble organic polyamide-based homogeneous composition having a precise number of repeating units, said composition having the formula:
[U—{NH—Y—NH—CO—X—CO} n {NH—Y′—NH} n′ ] q —V
wherein:
n is an integer from 1-100;
n′ is 0 or 1;
q is an integer from 1 to 10;
X and Y are divalent organic radicals lacking reactive functional groups or are absent and are the same or different, and can vary independently with each of said repeating units;
Y′ is a divalent organic radical lacking reactive functional groups or is absent;
V is selected from the group consisting of. a target molecule which is a peptide of less than 50 amino acid residues and having an optional divalent spacer or linker; a reporter group having a multivalent linker; a reactive group; and a terminal group having a multivalent linker, said terminal group being selected from the group consisting of —OH, —NH 2 , —H, and -Z-Q-support, where Z is a divalent spacer such as —NH—, —O— or may be absent, Q is a linker or a target molecule, and the support is a solid phase, matrix or surface; and
U is selected from the group consisting of: a target molecule which is a peptide of less than 50 amino acid residues and having an optional divalent spacer or linker; a terminal group; a peptide chain; a protecting group; a support; and a reactive group;
wherein at least one of U or V is a target molecule.
30 . The composition of claim 29 wherein said divalent organic radicals are selected from the group consisting of —(CH 2 ) 2 —, —(CH 2 ) 6 —, —(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —, —[(CH 2 ) 3 —O—(CH 2 ) 2 —(CH 2 ) 2 —O—(CH 2 ) 3 ]—, —CH 2 —O—CH 2 — and —CH 2 —N(CH 3 )—CH 2 —.
31 . The composition of claim 29 wherein said optional divalent linker is —COCH 2 ON═CH—CO—.
32 . The composition of claim 29 wherein said target molecule is selected from the group consisting of -GGLYACHMGPMTWVCQPLRG- (SEQ ID NO:1); -SVWRWLPYDKYE- (SEQ ID NO:3); and -ADGACRNPWC- (SEQ ID NO:6).
33 . The composition of claim 29 which has the formula: (peptide)-oxime-(‘PEG’-succ)n-‘PEG’-oxime-(peptide), wherein said peptide has the sequence -GGLYACHMGPMTWVCQPLRG- (SEQ ID NO: 1); oxime is —COCH 2 ON═CHC(O)—; ‘PEG’ represents the formula —NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—; succ represents the formula —CO—(CH 2 ) 2 —CO—; and n is 12 or 16.
34 . The composition of claim 29 which has the formula: peptide-Lys(NH 2 OCH 2 CO-(‘PEG’-succ) 8 )-NH 2 , wherein said peptide has the sequence -SVWRWLPYDKYE- (SEQ ID NO:3); ‘PEG’ represents the formula —NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—; and succ represents the formula —CO—(CH 2 ) 2 —CO—.
35 . The composition of claim 29 which has the formula: (peptide)-oxime-(‘PEG’-succ) 2 -Lys((peptide)-oxime-(‘PEG’-succ) 2 )amide, wherein said peptide has the sequence -GGLYACHMGPMTWVCQPLRG- (SEQ ID NO:1); oxime is -COCH 2 ON═CHC(O)—; ‘PEG’ represents the formula —NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—; and succ represents the formula —CO—(CH 2 ) 2 —CO—.
36 . The composition of claim 29 which has the formula: (peptide)-(‘PEG’-succ) 8 -Lys(aminooxyacetyl)-amide, wherein said peptide has the sequence -ADGACRNPWC- (SEQ ID NO:6); ‘PEG’ represents the formula —NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—; and succ represents the formula —CO—(CH 2 ) 2 —CO—.
37 . The composition of claim 29 which has the formula: [peptide-(‘PEG’-succ) 8 -Lys(oxime)amide] 4 Lys 2 Lys-NHCH 2 CH 2 S—CH 2 C(O)NH-fluorescein, wherein said peptide has the sequence -ADGACRNPWC- (SEQ ID NO:6); oxime is —COCH 2 ON═CHC(O)—; ‘PEG’ represents the formula —NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—; and succ represents the formula —CO—(CH 2 ) 2 —CO—.
38 . A water soluble organic polyamide-based homogeneous composition having the formula: (peptide)-oxime-(‘PEG’-succ) n -‘PEG’-oxime-(peptide), wherein said peptide has the sequence -GGLYACHMGPMTWVCQPLRG- (SEQ ID NO:1); oxime is —COCH 2 ON═CHC(O)—; ‘PEG’ represents the formula —NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—; succ represents the formula —CO—(CH 2 ) 2 —CO—; and n is 12 or 16.
39 . A water soluble organic polyamide-based homogeneous composition having the formula: peptide-Lys(NH 2 OCH 2 CO-(‘PEG’-succ) 8 )-NH 2 , wherein said peptide has the sequence -SVWRWLPYDKYE- (SEQ ID NO:3); ‘PEG’ represents the formula —NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—; and succ represents the formula —CO—(CH 2 ) 2 —CO—.
40 . A water soluble organic polyamide-based homogeneous composition having the formula: (peptide)-oxime-(‘PEG’-SUCC) 2 -Lys((peptide)-oxime-(‘PEG’-SUCC) 2 )amide, wherein said peptide has the sequence -GGLYACHMGPMTWVCQPLRG- (SEQ ID NO:1); oxime is —COCH 2 ON═CHC(O)—; ‘PEG’ represents the formula —NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—; and succ represents the formula —CO—(CH 2 ) 2 —CO—.
41 . A water soluble organic polyamide-based homogeneous composition having the formula: (peptide)-(‘PEG’-succ) 8 -Lys(aminooxyacetyl)-amide, wherein said peptide has the sequence -ADGACRNPWC- (SEQ ID NO:6); ‘PEG’ represents the formula —NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—; and succ represents the formula —CO—(CH 2 ) 2 —CO—.
42 . A water soluble organic polyamide-based homogeneous composition having the formula: [peptide-(‘PEG’-succ) 8 -Lys(oxime)amide] 4 Lys 2 Lys-NHCH 2 CH 2 S—CH 2 C(O)NH-fluorescein, wherein said peptide has the sequence -ADGACRNPWC- (SEQ ID NO:6); oxime is —COCH 2 ON═CHC(O)—; ‘PEG’ represents the formula —NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—; and succ represents the formula —CO—(CH 2 ) 2 —CO—.
43 . A method of synthesizing water soluble organic polyamide-based chain having a precise number of repeating units, said chain having the formula:
—{NH—Y—NH—CO—X—CO} n —{NH—Y′—NH} n′ —
wherein:
n is an integer from 1-100;
n′ is 1;
X and Y are divalent organic radicals lacking reactive functional groups or are absent and are the same or different, and can vary independently with each of said repeating units; and
Y′ is a divalent organic radical lacking reactive functional groups or is absent; comprising the steps of:
(a) acylating the amino or hydroxyl group of a compound of the formula Z-Q-support, where Z is H 2 N— or HO—; Q is a linker or a target molecule; and the support is a solid phase, matrix or surface, with a molar excess of a reagent L—CO—L′, where L and L′ are leaving groups and are the same or different;
(b) aminolysing the product of step (a) with a molar excess of a diamine having the formula, NH 2 —Y′—NH 2 ;
(c) acylating the product of step (b) with a molar excess of a derivative of a diacid having the formula, HOOC—X—COOH;
(d) activating the free carboxyl group of the product of step (c);
(e) aminolysing the product of step (d) with a molar excess of a diamine having the formula, NH 2 —Y—NH 2 ; and
(f) optionally repeating steps (c)-(e) using a derivative of a diacid having formula HOOC—X—COOH and a diamine having formula NH 2 —Y—NH 2 , where said X and Y substituents are the same or different from the X and Y substituents used in any of said previous aminolysing and acylating steps.
44 . The method of claim 43 wherein Q is a linker containing a cleavable moiety or a target molecule bound to the support by a linker containing a cleavable moiety, said method further comprising: cleaving said cleavable moiety to release the water soluble organic polyamide-based chain of precise length from the support.
45 . The method of claim 43 wherein one or more of the X and Y substituents are symmetrical radicals.
46 . The method of claim 43 wherein at least one of the X and Y substituents contains 1 to 5 —CH 2 CH 2 O— groups.
47 . The method of claim 43 wherein said divalent organic radicals are selected from the group consisting of substituted, unsubstituted, branched and linear, aliphatic and aromatic groups, and may optionally contain heteroatoms.
48 . The method of claim 47 wherein said divalent organic radicals are selected from the group consisting of phenyl, C 1 -C 10 alkylene moieties, C 1 -C 10 alkyl groups, optionally containing heteroatoms, or a combination thereof.
49 . The method of claim 48 wherein said divalent organic radicals are selected from the group consisting of —(CH 2 ) 2 —, —(CH 2 ) 6 —, —(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —, —[(CH 2 ) 3 —O—(CH 2 ) 2 —(CH 2 ) 2 —O—(CH 2 ) 3 ]—, —CH 2 —O—CH 2 — and —CH 2 —N(CH 3 )—CH 2 —.
50 . The method of claim 43 wherein said chain has the formula:
—{NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—CO—(CH 2 ) 2 —CO} n ——{NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH}—
51 . The method of claim 43 wherein said chain has the formula:
—[{NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO}——{NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—CO—(CH 2 ) 2 —CO}] z ——NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO—NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—
wherein z is an integer from 1-49.
52 . The method of claim 43 wherein the free carboxyl group is activated with an activating agent selected from the group consisting of carbonyl diimidazole, disuccinimidyl carbonate and O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate.
53 . A method of synthesizing a water soluble organic polyamide-based chain having a precise number of repeating units, said chain having the formula:
—{NH—Y—NH—CO—X—CO} n —
wherein:
n is an integer from 1-100; and
X and Y are divalent organic radicals lacking reactive functional groups or are absent and are the same or different, and can vary independently with each of said repeating units;
comprising the steps of:
(a) acylating the amino or hydroxyl group of a compound of the formula Z-Q-support with a molar excess of a derivative of a diacid having the formula, HOOC—X—COOH, where Z is H 2 N— or HO—; Q is a linker or a target molecule; the support is a solid phase, matrix or surface;
(b) activating the free carboxyl group of the product of step (a);
(c) aminolysing the product of step (b) with a molar excess of a diamine having the formula, NH 2 —Y—NH 2 ; and
(d) optionally repeating steps (a)-(c) using HOOC—X—COOH and NH 2 —Y—NH 2 , where said X and Y substituents are the same or different from the X and Y substituents used in any of said previous acylating and aminolysing steps.
54 . The method of claim 53 wherein Q is a linker containing a cleavable moiety or a target molecule bound to the support by a linker containing a cleavable moiety, said method further comprising: cleaving said cleavable moiety to release the water soluble organic polyamide-based chain of precise length from the support.
55 . The method of claim 53 wherein one or more of the X and Y substituents are symmetrical radicals.
56 . The method of claim 53 wherein at least one of the X and Y substituents contains 1 to 5 —CH 2 CH 2 O— groups.
57 . The method of claim 53 wherein said divalent organic radicals are selected from the group consisting of substituted, unsubstituted, branched and linear, aliphatic and aromatic groups, and may optionally contain heteroatoms.
58 . The method of claim 57 wherein said divalent organic radicals are selected from the group consisting of phenyl, C 1 -C 10 alkylene moieties, C 1 -C 10 alkyl groups, optionally containing heteroatoms, or a combination thereof.
59 . The method of claim 58 wherein said divalent organic radicals are selected from the group consisting of —(CH 2 ) 2 —, —(CH 2 ) 6 —, —(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —, —[(CH 2 ) 3 —O—(CH 2 ) 2 —(CH 2 ) 2 —O—(CH 2 ) 3 ]—, —CH 2 —O—CH 2 — and —CH 2 —N(CH 3 )—CH 2 —.
60 . The method of claim 53 wherein said chain has the formula:
—{NH—CH 2 —(CH 2 CH 2 O) 3 —(CH 2 ) 3 —NH—CO—(CH 2 ) 2 —CO} n —
61 . The method of claim 53 wherein said chain has the formula:
—{NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO} n—
62 . The method of claim 53 wherein said chain has the formula:
—{NH—(CH 2 ) 6 —NH—CO—(CH 2 ) 2 —CO——NH—(CH 2 ) 3 —(OCH 2 CH 2 ) 3 —CH 2 —NH—CO—(CH 2 ) 2 —CO} n —
63 . The method of claim 53 wherein the free carboxyl group is activated with an activating agent selected from the group consisting of carbonyl diimidazole, disuccinimidyl carbonate and O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate.
64 . A kit for synthesizing a water soluble organic polyamide-based chain having a precise number of repeating units, said chain having the formula:
—{NH—Y—NH—CO—X—CO} n —{NH—Y′—NH} n′ —
wherein:
n is an integer from 1-100;
n′ is 0 or 1;
X and Y are divalent organic radicals lacking reactive functional groups or are absent and are the same or different, and can vary independently with each of said repeating units;
Y′ is a divalent organic radical lacking reactive functional groups or is absent;
comprising:
(a) Z-Q-support, where Z is H 2 N— or HO—; Q is a linker or a target molecule; and the support is a solid phase, matrix or surface;
(b) a diacid having the formula, HOOC—X—COOH, or a derivative thereof; and
(c) a diamine having the formula, NH 2 —Y—NH 2 .
65 . The kit of claim 64 further comprising at least one additional diacid having the formula, HOOC—X—COOH, wherein the X substituent is different from the X substituent in the first diacid, or derivative thereof.
66 . The kit of claim 64 further comprising at least one additional di amine having the formula, NH 2 —Y—NH 2 , wherein the Y substituent is different from the Y substituent in the first diamine.
67 . The kit of claim 64 further comprising an activating agent selected from the group consisting of carbonyl diimidazole, disuccinimidyl carbonate and O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate.
68 . A kit for enhancing or modifying a target molecule comprising:
(a) reagents for synthesizing a water soluble organic polyamide-based chain having a precise number of repeating units, said chain having the formula: —{NH—Y—NH—CO—X—CO} n —{NH—Y′—NH} n′ — wherein: n is an integer from 1-100; n′ is 0 or 1; X and Y are divalent organic radicals lacking reactive functional groups or are absent and are the same or different, and can vary independently with each of said repeating units; and Y′ is a divalent organic radical lacking reactive functional groups or is absent; comprising:
(i) Z-Q-support, where Z is H 2 N— or HO—; Q is a linker or a target molecule; and the support is a solid phase, matrix or surface;
(ii) a diacid having the formula, HOOC—X—COOH, where X is a divalent organic radical lacking reactive functional groups or is absent, or a derivative thereof; and
(iii) a diamine having the formula, NH 2 —Y—NH 2 , where Y is a divalent organic radical lacking reactive functional groups or is absent; and
(b) a target molecule whose properties are being modified or enhanced, and having an optional divalent spacer or linker.
69 . The kit of claim 68 further comprising at least one additional diacid having the formula, HOOC—X—COOH, wherein the X substituent is different from the X substituent in the first diacid, or derivative thereof.
70 . The kit of claim 68 further comprising at least one additional diamine having the formula, NH 2 —Y—NH 2 , wherein the Y substituent is different from the Y substituent in the first diamine.
71 . The kit of claim 68 further comprising an activating agent selected from the group consisting of carbonyl diimidazole, disuccinimidyl carbonate and O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate.
72 . The kit of claim 68 wherein said target molecule is selected from the group consisting of proteins, polypeptides, peptides, nucleic acids, liposomes, and therapeutic agents.
73 . The kit of claim 72 wherein said target molecule is a peptide selected from the group consisting of -GGLYACHMGPMTWVCQPLRG- (SEQ ID NO:1); -SVWRWLPYDKYE- (SEQ ID NO:3); and -ADGACRNPWC- (SEQ ID NO:6).
74 . A kit for enhancing or modifying a target molecule comprising:
(a) a water soluble organic polyamide-based chain having a precise number of repeating units, said chain having the formula: —{NH—Y—NH—CO—X—CO} n —{NH—Y′—NH} n′ — wherein:
n is an integer from 1-100;
n′ is 0 or 1;
X and Y are divalent organic radicals lacking reactive functional groups or are absent and are the same or different, and can vary independently with each of said repeating units; and
Y′ is a divalent organic radical lacking reactive functional groups or is absent.; and
(b) a target molecule whose properties are being modified or enhanced, and having an optional divalent spacer or linker.
75 . The kit of claim 74 wherein said target molecule is selected from the group consisting of proteins, polypeptides, peptides, nucleic acids, liposomes, and therapeutic agents.
76 . The kit of claim 75 wherein said target molecule is a peptide selected from the group consisting of -GGLYACHMGPMTWVCQPLRG- (SEQ ID NO:1); -SVWRWLPYDKYE- (SEQ ID NO:3); and -ADGACRNPWC- (SEQ ID NO:6).Cited by (0)
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