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Imaging Agent Labeled Peptide Synthesis

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Modern imaging techniques increasingly rely on the use of radioactive isotopes of certain metal ions, often in combination with targeting peptides. CD Formulation offers custom imaging agent-labeled peptide synthesis and modification services for disease diagnostics, where chelators are covalently linked to the peptide. We have an excellent track record in the field of radiopharmaceuticals and synthetic precursors for radiolabeled peptides for a wide range of applications.

Introduction to Imaging Agent Labeled Peptides

The main goal of modern biomedicine is to develop specific diagnostic and therapeutic agents for different diseases. Especially in cancer research, tumor-targeting molecules are a key factor in the development of new anti-tumor drugs. In addition, early diagnosis of the disease is an important factor for successful treatment. The meteoric advancement of chemical modification techniques has unleashed a wave of innovation, permitting the intricate design and synthesis of imaging agents intricately linked to synthetic peptides, poised as the vanguard of next-generation diagnostic and therapeutic modalities. These agents boast an impressive arsenal of attributes: enhanced metabolic resilience, robust pharmacokinetics, superior binding affinity, and selectivity, alongside strikingly improved imaging capabilities and commendable biosafety profiles. Non-invasive in vivo imaging using radiolabeled peptides has become a modern method for pathological changes such as cancer diagnosis.

Fig. 1 Peptide-based imaging agents. Fig. 1 The general development process of peptide-based imaging agents for cancer detection. (Sun X, et al., 2017)

Explore Our Custom Imaging Agent Labeled Peptide Synthesis Services

At CD Formulation, we harness an extensive reservoir of expertise amassed over decades in the intricate art of peptide synthesis, enabling us to offer bespoke services for imaging agent-labeled peptide synthesis. Our capabilities flourish with the remarkable adaptability to seamlessly integrate metal chelators, intricately positioned either at the N-terminus or cleverly woven into the side chains of lysine residues throughout the sequence.

Below, we list some metal chelators that are commonly used for the conjugation of imaging agent-labeled peptides:

Bifunctional Chelating Agent (BFCA)	Code	Mass Difference
Mercaptoacetyltriglycine, diaminedithiol, 2-hydrazinonicotinic acid,	MAG3, DADT, HYNIC	Technetium-99m (99mTc)
N-succinimidyl-4-[18F]fluorobenzoate	SFB	Fluorine-18 (18F)
N-succinimidyl-3-iodobenzoate, N-succinimidyl-5-iodo-3-pyridinecarboxylate	SIB, SIPC	Iodine-123 (123I)
1,4,7-triazacyclononane-1,4,7-triacetic acid, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid	NOTA, DOTA	Gallium-68 (68Ga)
1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetraacetic acid, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid, 1,4,7-triazacyclononane-1,4,7-triacetic acid	TETA, DOTA, NOTA	Copper-64 (64Cu)
diethylenetriaminepentaacetic acid, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid	DTPA, DOTA	Indium-111 (111In)
1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid	DOTA	Lutetium-177 (177Lu)
1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid	DOTA	Yttrium-90 (90Y)
1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid	DOTA	Bismuth-213 (213Bi)
Desferrioxamine	DFO	Fe³⁺, Zr⁴⁺

Choose The Right Metal Chelator for Your Imaging Agent-Labeled Peptide

Chelators—those enigmatic chemical entities like DTPA, DOTA, NOTA, and the curious DOTA-GA—assert their dominance as MRI contrast agents and cold metal conduits in the realm of Gd(III) and Y(III) for scintillating PET and CT imaging. These metal helatorshave excellent affinity and can effortlessly bind to a range of commonly used multivalent radiometals, including Lu-177 (177Lu), the mysterious Ga-67 (67Ga), the versatile In-111 (111In), and the bold Y-90 (90Y).
DFO, or Desferrioxamine, emerges as a fascinating iron chelator, exhibiting a remarkable affinity for Fe3+ alongside an array of other metal cations, including the elusive Zr4+. Intriguingly, this versatile compound can also be artfully integrated into peptide structures, opening up a myriad of possibilities in biochemistry and therapeutic applications.
Mercaptoacetyltriglycine (MAG3) can be easily incorporated into peptides for site-specific labeling with Tc-99m (99mTc).
Radioiodine label (125I) can be easily introduced into any tyrosine residue (or its derivative) in the sequence by iodination.

Fig. 2 DTPA and DOTA structures. Fig. 2 Schematic diagram of DTPA (a) and DOTA (b) structures. (Huhtala T, et al., 2014)

Applications of Imaging Agent-Labeled Peptide

Molecular imaging in cells in basic research.
Medical imaging in disease diagnosis.
Targeted drug delivery in disease treatment.

Peptide Manufacturing & Analytical Services

In addition to peptide synthesis capabilities, CD Formulation combines flexible GMP manufacturing facilities with cutting-edge peptide analytical knowledge to provide a full range of quality control testing services to accelerate the commercialization of your products, including:

Peptide identification (ESI-MS).
Peptide Molecular weight determination.
Peptide sequencing.
Peptide quantification/peptide content determination.
Peptide purity and impurity analysis (HPLC/UV).
Amino acid sequence.
Amino acid composition determination.
Net peptide content.

Enantiomeric purity testing (GC/MS; LC).
Residual counterion testing (e.g. TFA).
Elemental analysis.
Residual solvent testing.
Water content testing (GC or KF).
Peptide solubility testing.
Peptide stability testing.

Optical rotation determination.
Bioburden testing(TAMC/TYMC).
Bacterial endotoxin testing.
Sterility testing.
Cytotoxicity testing.
Process/product related impurity testing.
Other pharmacopoeia testing.

Publication

Published Data

Technology: Imaging Agent Labeled Peptide Synthesis

Journal: Nat Protoc.

IF: 10.032

Published: 2012

Results:

The authors describe a method for labeling peptides with the positron-emitting radioisotope fluorine-18 ((18)F) using a silicon fluoride acceptor (SiFA) labeling approach. In this method, N-terminally SiFA-modified peptides can be labeled with (18)F(-) in a single step at room temperature (20-25°C) or lower without the formation of byproducts. The protocol allows for a facile cartridge-based purification completely without HPLC implementation, yielding peptides with specific activities between 44.4 and 62.9 GBq μmol(-1) in 25 minutes.

Fig. 3 18F-Labeling of peptides using SiFA. (Wängler C, et al., 2012)

CD Formulation is a trusted partner for peptide synthesis. Please don't hesitate to contact us if you are considering using imaging agent labeled peptides in your project. We look forward to cooperating with you.

References

Sun X, Li Y, Liu T, et al. Peptide-based imaging agents for cancer detection. Adv Drug Deliv Rev. 2017;110-111:38-51.
Huhtala T, Weisell J, Rytkönen J, et al. Peptide labelling strategies for imaging agents. Methods Mol Biol. 2014;1088:171-83.
Wängler C, Niedermoser S, Chin J, et al. One-step (18)F-labeling of peptides for positron emission tomography imaging using the SiFA methodology. Nat Protoc. 2012 Nov;7(11):1946-55.

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