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Details for Patent: 5,788,960

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Details for Patent: 5,788,960

Title: Technetium-99M labeled polypeptides for imaging
Abstract:The invention relates to radiolabeled imaging of a mammalian body. The invention in particular provides for reagents labeled with technetium-99 m for such imaging. The invention provides peptides which bind technetium-99 m and which can be targeted to specific sites within a mammalian body.
Inventor(s): Dean; Richard T. (Bedford, NH)
Assignee: Diatech, Inc. (Londonderry, NH)
Filing Date:Jun 05, 1995
Application Number:08/463,052
Claims:1. A technetium-99 m labeled scintigraphic imaging agent comprising, in combination:

(a) a peptide of 3 to 100 amino acids that specifically binds to a target site to be imaged; and

(b) a technetium-99 m binding moiety of the formula

wherein C is a cysteine amino acid residue and (aa) is any primary .alpha.- or .beta.-amino acid, the technetium-99 m binding moiety being covalently bound to the peptide, wherein the peptide specifically binds to clots, tumors, sites of infection, atherosclerotic plaques, amyloid plaques or bone.

2. A technetium-99 m labeled scintigraphic imaging agent according to claim 1 wherein the peptide is selected from the group consisting of:

YRALVDTLK (SEQ ID No.1)

RALVDTLK (SEQ ID No.2)

RALVDTLKFVTQAEGAK (SEQ ID No.3)

YAKFRETLEDTRDRMY (SEQ ID No.4)

AKFRETLEDTRDRMY (SEQ ID No.5)

YAALDLNAVANKIADFEL (SEQ ID No.6)

AALDLNAVANKIADFEL (SEQ ID No.7)

YRALVDTLKFVTEQAKGA (SEQ ID No.8)

RALVDTLKFVTEQAKGA (SEQ ID No.9)

YRALVDTEFKVKQEAGAK (SEQ ID No.10)

RALVDTEFKVKQEAGAK (SEQ ID No.11)

YRALVDTLKFVTQAEGAK (SEQ ID No.12)

VGVAPGVGVAPGVGVAPG (SEQ ID No.13)

VPGVGVPGVGVPGVGVPGVG (SEQ ID No.14)

formyl.Nleu.LF.Nleu.YK (SEQ ID No.15)

formyl MIFL (SEQ ID No.16)

formyl MLFK (SEQ ID No.17)

formyl MLFI (SEQ ID No.18)

formyl MFIL (SEQ ID No.19)

formyl MFLI (SEQ ID No.20)

formyl MLIF (SEQ ID No.21)

formyl MILF (SEQ ID No.22)

TKPR (SEQ ID No.23)

VGVAPG (SEQ ID No.24)

formyl MLF (SEQ ID No.25)

NDGDFEEIPEEYLQ (SEQ ID No.26)

NDGDFEEIPEEY(SO.sub.3 Na)LQ (SEQ ID No.27)

GPRG (SEQ ID No.28)

D-Phe.PRPGGGGNGDFEEIPEEYL (SEQ ID No.29)

RRRRPRRRRGDV (SEQ ID No.30)

PLYKKIIKKLLES (SEQ ID No.31)

RGD (SEQ ID No.32)

RGDS (SEQ ID No.33)

YIGSR (SEQ ID No.34)

CH.sub.2 CO.YIGSRC (SEQ ID No.35)

and

EKPLQNFTLSFR (SEQ ID No.36).

3. The technetium-99 m labeled scintigraphic imaging agent of claim 1 produced from a reagent comprising a specific binding peptide covalently linked to a Cp(aa)Cp technetium-99 m binding moiety through from about one to about ninety amino acids.

4. The technetium-99 m labeled scintigraphic imaging agent of claim 1 produced from a reagent comprising a technetium-99 m binding moiety having a sidechain sulfur atom protected by a protecting group of the formula

wherein R is a lower alkyl having 1 to 6 carbon atoms, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, carboxy, or lower alkoxycarbonyl, or 2-,3-,4-pyridyl.

5. The technetium-99 m labeled scintigraphic imaging agent of claim 1 produced from a reagent comprising a technetium-99 m binding moiety having the formula: ##STR8##
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