Targeting the chemokine receptor CXCR4 for cancer therapies
Ariana Rueda1,2,3, Naroa Serna2,4, Ramon Mangues5,6,7
1Institut de Recerca Sant Pau (IR SANT PAU), Sant Quintí 77 - 79, Barcelona, 08041, Spain.
Abstract:
The C-X-C chemokine receptor type 4 (CXCR4) has emerged as a key molecular biomarker for cancer therapies due to its critical role in tumor progression and metastases by displaying a stem cells phenotype. Its overexpression has been observed in more than 20 types of cancers, including solid tumors and hematological malignancies, and it is often associated with tumor aggressiveness and poor prognosis. Being initially recognized as a co-receptor involved in HIV infection, numerous CXCR4-targeting ligands and antagonists, including small molecules, peptides and biologics have been identified over the past decades. While only few of them have been used in the context of cancer therapies, recent biotechnological advancements using CXCR4 as a molecular target are showing significant potential to revolutionize future cancer therapies. Therefore, this review highlights the biotechnological innovations developed for cancer therapy and diagnosis by targeting the chemokine receptor CXCR4. It also discusses future perspectives on emerging therapeutic strategies, ranging from the use of small molecule inhibitors that block receptor signaling to cutting-edge nanocarriers designed for the targeted delivery of innovative drugs and proteins into cancer stem cells, aiming at cell-selective precision nanomedicines.
Insights
The C-X-C chemokine receptor type 4 (CXCR4) is a key biomarker in cancer, driving tumor progression and metastasis. Biotechnological innovations targeting CXCR4 show promise for revolutionizing cancer therapy and diagnosis.
Area of Science:
- Oncology
- Molecular Biology
- Biotechnology
Background:
- C-X-C chemokine receptor type 4 (CXCR4) is overexpressed in over 20 cancer types, correlating with aggressiveness and poor prognosis.
- CXCR4 plays a critical role in tumor progression, metastasis, and stem cell phenotype.
- Initially identified as an HIV co-receptor, CXCR4 is now a significant target for cancer therapies.
Purpose of the Study:
- To review biotechnological innovations for cancer therapy and diagnosis targeting CXCR4.
- To discuss emerging therapeutic strategies involving CXCR4 inhibition and targeted drug delivery.
Main Methods:
- Literature review of CXCR4-targeting ligands and antagonists.
- Analysis of recent biotechnological advancements in cancer therapy and diagnosis.
- Exploration of novel therapeutic strategies including small molecule inhibitors and nanocarriers.
Main Results:
- Numerous CXCR4-targeting agents (small molecules, peptides, biologics) have been developed.
- Biotechnological advancements offer significant potential for future cancer therapies.
- Targeted delivery systems, like nanocarriers, show promise for precision nanomedicine.
Conclusions:
- CXCR4 is a crucial molecular target with significant therapeutic and diagnostic potential in oncology.
- Emerging strategies focus on blocking CXCR4 signaling and targeted drug delivery to cancer stem cells.
- Biotechnology-driven innovations are poised to revolutionize cancer treatment paradigms.
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