Peptide Conjugation for Disease Diagnosis
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Peptide conjugation is an important tool in the field of modern biomedicine, which links peptides with other molecules (such as dyes, drugs, proteins, etc.) through chemical bonds, thus enhancing the application potential of peptides in disease diagnosis. The following are examples of the use of peptide conjugation is used in the diagnosis of several common diseases.
Cancer diagnosis
In today's society, the incidence of malignant tumors is getting higher and higher, and it has become the number one killer that threatens human life. With the advent of the era of precision medicine, the use of tumor molecular markers for early screening and molecularly targeted therapy has become the focus of research. In 2018, the National Center for Nanoscience and Technology of China, in collaboration with a research team from the Department of Chemistry at Stanford University, developed a tumor-targeted molecular diagnostic technology using peptide molecular probes, which greatly promoted the progress in this field. The research team first successfully obtained a novel targeted peptide CP targeting the cancer stem cell marker CD133 through high-throughput screening of microarrays. Subsequently, they developed a novel water-soluble NIR-II fluorescent small molecule IRT and conjugated it to the CP peptide through a Click reaction to achieve tail vein injection and in vivo tumor scintigraphy. Compared to traditional untargeted molecules, CP-IRT has demonstrated significant advantages in reaching signal peaks in as little as 2 hours. This targeted molecular diagnostic method based on peptide conjugation technology not only shows excellent performance in cancer diagnosis, but even has the potential to replace traditional antibody diagnosis and treatment reagents, bringing new hope and possibilities for tumor treatment.
Fig.1 Fluorescent small molecule IRT is conjugated to CP peptides by a Click reaction. (Temma Takashi, et al., 2018)
Cardiovascular Disease diagnosis
Myocardial infarction (MI) is an acute cardiovascular event due to myocardial ischemia and necrosis due to blockage of the coronary arteries. Early diagnosis of myocardial infarction is essential for the care of patients. Peptide conjugation technology has shown significant advantages in the early diagnosis of myocardial infarction. For example, researchers have developed a peptide probe conjugated to a radioisotope that can specifically recognize and bind troponin I (cTnI) on cardiomyocytes, a marker of myocardial injury. Through radiological imaging technology, the occurrence of myocardial infarction can be detected early, helping clinicians to make rapid treatment decisions.
Table 1. Peptide conjugation service at Creative Peptides
Infectious diseases diagnosis
The early diagnosis of HIV infection is of great significance to prevent the spread of AIDS and improve the quality of life for patients. Traditional HIV diagnostic methods include ELISA and PCR, but these methods have certain limitations. Using peptide conjugation technology, the researchers developed a peptide probe conjugated to nanoparticles that can specifically recognize the envelope protein p24 of HIV. Nanoparticles enhance the signal intensity of the probe, enabling accurate detection of HIV infection even at low viral loads, providing a new avenue for early diagnosis.
Neurological Diseases diagnosis
Until now, early diagnosis of Alzheimer's disease (AD) has been challenging. Recent studies have shown that high expression of connective tissue growth factor (CTGF) in the brain of AD regulates the occurrence of amyloid (Aβ) plaques β, so CTGF may be an earlier biomarker for AD diagnosis than Aβ plaques. In June 2024, Gao's team at the Beijing University of Technology jointly published a research paper online in Nature Communications, in which the research team developed a peptide-coated gold nanocluster (DGC) with high affinity (KD~21.9 nM) that can specifically target CTGF. The nanoclusters can emit NIR-II and red fluorescence at the same time, and can be quantified in vitro by inductively conjugated plasma mass spectrometry (ICP-MS) for the ex vivo quantitative analysis of CTGC in brain sections of AD patients.
Fig.2 Schematic diagram of DGC preparation specifically targeting CTGF in Alzheimer's disease. (Lu Cao, et al., 2024)
Inflammatory diseases diagnosis
Peptides can be designed to specifically bind to inflammation-related molecules or cellular receptors. For example, certain peptides can recognize and bind to receptors for specific immune proteins, which can help with imaging diagnosis or therapeutic monitoring in areas of inflammation. Granulases (GZMS) are a family of serine proteases that are expressed by immune and non-immune cells and are involved in the pathophysiology of different inflammatory diseases. A peptide probe based on fluorescence energy resonance transfer linked in the order of the fluorophore FAM-peptide-quencher DABCYL was developed for the specific detection of GzmA activity in tissue samples and biological fluids in mouse and human samples during inflammatory diseases. Experiments have confirmed that the probe shows very good specificity and sensitivity for human and mouse GzmA.
Fig.3 Diagram of the mode of action of the fluorophore FAM-peptide-quencher DABCYL. (Senan-Salinas Ana, et al., 2024)
Summary
Peptide conjugation technology has shown significant advantages in the detection of cancer, cardiovascular disease, and infectious diseases, especially in terms of improving the sensitivity and specificity of the assay. This technology enables early diagnosis and precise treatment through the development of specific probes, greatly improving the efficiency and effectiveness of disease management. Therefore, peptide conjugation is of great significance in modern medicine and has become a key tool in the diagnosis and treatment of diseases.
References
- Wang, Weizhi, et al., Molecular cancer imaging in the second near‐infrared window using a renal‐excreted NIR‐II fluorophore‐peptide probe. Advanced Materials 30.22 (2018): 1800106.
- Temma, Takashi, et al., Radiolabelled probes for imaging of atherosclerotic plaques. American Journal of Nuclear Medicine and Molecular Imaging 2.4 (2012): 432.
- Mozhgani, Sayed-Hamidreza, et al., Nanotechnology based strategies for HIV-1 and HTLV-1 retroviruses gene detection. Heliyon 6.5 (2020).
- Lu, Cao, et al., A probe for NIR-II imaging and multimodal analysis of early Alzheimer's disease by targeting CTGF. Nature Communications 15.1 (2024): 5000.
- Senan-Salinas, Ana, et al., Selective Detection of Active Extracellular Granzyme A by Using a Novel Fluorescent Immunoprobe with Application to Inflammatory Diseases. ACS Pharmacology & Translational Science 7.5 (2024): 1474-1484.
