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Calcitonin receptor-binding peptides

A calcitonin receptor and calcitonin technology, applied in the direction of calcitonin, hormone peptide, isotope introduction into organic compounds, etc., can solve the technical difficulties of coupling while maintaining compound receptor specificity

Inactive Publication Date: 2000-05-24
DIATECH PTY LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But conjugating peptides or small molecules to labels or cytotoxic reagents while maintaining compound receptor specificity is technically difficult

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0159] Synthesis of BAT chelating agent

[0160] BAT chelators, particularly S-cysteine-derived and ε-aminolysylamino-derived BAT chelators, were prepared according to the methods of commonly owned and co-pending U.S. Serial No. 08 / 414424, incorporated herein by reference .

Embodiment 2

[0162] Solid Phase Peptide Synthesis

[0163] Solid-phase peptide synthesis (SPPS) was performed on a 0.25 mmol scale using an Applied Biosystems Model 431A Peptide Synthesizer, using fluorenylmethoxycarbonyl (Fmoc) amino-terminal protection with dicyclohexylcarbodiimide / hydroxybenzo Triazole or 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate / hydroxybenzotriazole (HBTU / HOBT) coupling, and for carboxyl Use p-hydroxymethylphenoxymethyl-polystyrene (HMP) resin or Sasrin for terminal acid TM Either chlorotrityl free radical resin or Rink amide resin for carboxy-terminated amides.

[0164] Where appropriate, Fmoc-Cys(BAT) and Nα-Fmoc-Nε-(BAT)Lys were synthesized as described in commonly owned and co-pending US Serial No. 08 / 414424, incorporated herein by reference.

[0165] By using the appropriate 2-haloacid as the last residue of the coupling in SPPS, or by using 2-haloacid / diisopropylcarbodiimide / N-hydroxysuccinamide / NMP or 2-halogenated anhydride / diis...

Embodiment 3

[0181] General method for radiolabeling with technetium-99m

[0182] 0.1 mg of the peptide prepared in Example 2 was dissolved in 0.1 ml or 0.2 ml of water or 0.9% saline. Technetium-99m gluceptate was prepared by reconstituting Glucoscan vials (E.I. DuPont de Nemours, Inc., Wilmington, DE) with 0.25 ml technetium-99m sodium pertechnetate containing up to 200 mCi and left at room temperature 15 minutes. Then 25 μl technetium-99m gluconate was added to the peptide and the reaction was allowed to proceed for 15-60 minutes at room temperature or 10-30 minutes at 100° C. and then filtered through a 0.2 μm filter.

[0183] The purity of the technetium-99m-labeled peptides was determined by reverse-phase HPLC using the following conditions: Waters Delta Pak C18 column, 5 μ, 3.9 mm x 150 mm analytical column loaded with each labeled peptide at a solvent flow rate equal to 1 ml / min Eluting peptide (Delta-Pak). Gradient elution using a gradient of 20-50% solvent B / solvent A (solvent...

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Abstract

This invention relates to calcitonin receptor binding reagents comprising compounds which are covalently linked to a radiometal chelator. The invention is embodied as calcitonin receptor binding peptide derivatives and analogues of calcitonin which may be radiolabeled with a suitable isotope and used as radiodiagnostic or radiotherapeutic agents. Methods and kits for making, radiolabeling and using such reagents diagnostically and therapeutically in a mammalian body are also provided.

Description

[0001] The present invention relates to calcitonin receptor binding agents capable of complexing metal ions, including radioactive metal ions, and to the implementation of the labeling of such agents for use at imaging sites in mammals or in therapy, particularly in the treatment of cancer Program. Background of the invention [0002] Over the past 60 years, great strides have been made in reducing long-term mortality trends for some types of cancer, such as gastric cancer. But at the same time, the death trend of some other cancers still exists or rises. For example, lung cancer is the most common cancer worldwide and represents the leading cause of cancer mortality in both men and women. Breast cancer is the most common cancer in women and the second leading cause of cancer mortality in women, with ovarian cancer mortality rates increasing in some countries. Lymphocytic cancers such as leukemia and non-Hodgkin's lymphoma in children and adults also continue to represent a ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/00A61K38/00A61K38/23A61K49/00A61K51/08A61P35/00C07B59/00C07K14/585
CPCC07K14/585A61K38/00A61P35/00A61K38/23
Inventor 理查德·T·迪安拉里·R·布什丹尼尔·A·皮尔逊约翰·利斯特-詹姆斯
Owner DIATECH PTY LTD