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The challenges and opportunities of αvβ3-based therapeutics in cancer: From bench to clinical trials
Yanlun Gu1, Bingqi Dong2, Xu He3
1Department of Pharmacy, Peking University First Hospital, Xishiku Street, Xicheng District, 100034 Beijing, China; Institute of Clinical Pharmacology, Peking University First Hospital, Xueyuan Road 38, Haidian District, 100191 Beijing, China; Department of Pharmacy Administration and Clinical Pharmacy, School of Pharmaceutical Sciences, Peking University, Xueyuan Road 38, Haidian District, 100191 Beijing, China.
Abstract:
Integrins are main cell adhesion receptors serving as linker attaching cells to extracellular matrix (ECM) and bidirectional hubs transmitting biochemical and mechanical signals between cells and their environment. Integrin αvβ3 is a critical family member of integrins and interacts with ECM proteins containing RGD tripeptide sequence. Accumulating evidence indicated that the abnormal expression of integrin αvβ3 was associated with various tumor progressions, including tumor initiation, sustained tumor growth, distant metastasis, drug resistance development, maintenance of stemness in cancer cells. Therefore, αvβ3 has been explored as a therapeutic target in various types of cancers, but there is no αvβ3 antagonist approved for human therapy. Targeting-integrin αvβ3 therapeutics has been a challenge, but lessons from the past are valuable to the development of innovative targeting approaches. This review systematically summarized the structure, signal transduction, regulatory role in cancer, and drug development history of integrin αvβ3, and also provided new insights into αvβ3-based therapeutics in cancer from bench to clinical trials, which would contribute to developing effective targeting αvβ3 agents for cancer treatment.
Insights
Integrin αvβ3, a key cell adhesion receptor, is linked to cancer progression. This review explores αvβ3
Area of Science:
- Cell Biology
- Molecular Biology
- Oncology
Background:
- Integrins are crucial cell adhesion receptors mediating cell-extracellular matrix (ECM) interactions and signal transduction.
- Integrin αvβ3 specifically binds ECM proteins with an RGD sequence and is implicated in various cancer hallmarks.
- Abnormal αvβ3 expression correlates with tumor initiation, growth, metastasis, drug resistance, and cancer stemness.
Purpose of the Study:
- To systematically review the structure, signaling, and cancer-regulatory roles of integrin αvβ3.
- To analyze the drug development history and challenges of targeting αvβ3 in cancer.
- To provide insights for developing novel αvβ3-based cancer therapeutics.
Main Methods:
- Literature review of integrin αvβ3 structure and function.
- Analysis of preclinical and clinical studies on αvβ3 antagonists.
- Synthesis of information on αvβ3's role in cancer progression and therapeutic targeting.
Main Results:
- Integrin αvβ3 plays a multifaceted role in promoting tumor progression and resistance.
- Despite extensive research, no αvβ3 antagonist is currently approved for human cancer therapy.
- Past therapeutic development efforts offer valuable lessons for future strategies.
Conclusions:
- Integrin αvβ3 is a significant therapeutic target in oncology.
- Overcoming challenges in αvβ3 antagonist development is critical for effective cancer treatment.
- Further research into innovative αvβ3-targeting approaches is warranted to translate bench discoveries to clinical success.
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