生物活性

• 描述Integrins are a large family of cell surface receptors that mediate cell adhesion and influence migration, signal transduction, and gene expression^[3]. Integrin-mediated cell adhesion is important for development, immune responses, hemostasis and wound healing. Integrins also function as signal transducing receptors that can control intracellular pathways that regulate cell survival, proliferation, and cell fate. Conversely, cells can modulate the affinity of integrins for their ligands a process operationally defined as integrin activation^[4].Arg-Gly-Asp(RGD) is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; binds to integrins. RGD is the most effective and most often employed peptide sequence for stimulated cell adhesion on synthetic surfaces. There are 24 integrins binding to ECM molecules in a RGD dependent manner: α3β1, α5β1, α8β1, αIIbβ3, αvβ1, αvβ3, αvβ5, αvβ6, αvβ8, and to some extent α2β1 and α4β1^[5].The RGD sequence is the cell attachment site of a large number of adhesive extracellular matrix, blood, and cell surface proteins, and nearly half of the over 20 known integrins recognize this sequence in their adhesion protein ligands. The RGD peptides and mimics can be used to probe integrin functions in various biological systems. Drug design based on the RGD structure may provide new treatments for diseases such as thrombosis, osteoporosis, and cancer^[6].RGD peptide acts as an inhibitor of integrin-ligand interactions and can induce apoptosis in the absence of signals and integrin-mediated cell clustering. Research demonstrates that RGD peptides promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing^[7].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01806675	Adult Giant Cell Glioblastoma ... more >> Adult Glioblastoma Adult Gliosarcoma Male Breast Cancer Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma Recurrent Adenoid Cystic Carcinoma of the Oral Cavity Recurrent Adult Brain Tumor Recurrent Basal Cell Carcinoma of the Lip Recurrent Breast Cancer Recurrent Colon Cancer Recurrent Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity Recurrent Hypopharyngeal Cancer Recurrent Inverted Papilloma of the Paranasal Sinus and Nasal Cavity Recurrent Laryngeal Cancer Recurrent Lip and Oral Cavity Cancer Recurrent Lymphoepithelioma of the Nasopharynx Recurrent Lymphoepithelioma of the Oropharynx Recurrent Metastatic Squamous Neck Cancer With Occult Primary Recurrent Midline Lethal Granuloma of the Paranasal Sinus and Nasal Cavity Recurrent Mucoepidermoid Carcinoma of the Oral Cavity Recurrent Nasopharyngeal Cancer Recurrent Non-small Cell Lung Cancer Recurrent Oropharyngeal Cancer Recurrent Pancreatic Cancer Recurrent Paranasal Sinus and Nasal Cavity Cancer Recurrent Rectal Cancer Recurrent Renal Cell Cancer Recurrent Salivary Gland Cancer Stage IIIA Breast Cancer Stage IIIA Non-small Cell Lung Cancer Stage IIIB Breast Cancer Stage IIIB Non-small Cell Lung Cancer Stage IIIC Breast Cancer Stage IV Breast Cancer Stage IV Non-small Cell Lung Cancer Stage IV Pancreatic Cancer Stage IV Renal Cell Cancer Stage IVA Colon Cancer Stage IVA Rectal Cancer Stage IVA Salivary Gland Cancer Stage IVB Colon Cancer Stage IVB Salivary Gland Cancer Stage IVC Salivary Gland Cancer Tongue Cancer Unspecified Adult Solid Tumor, Protocol Specific Collapse <<	Phase 1 Phase 2	Active, not recruiting	March 2019	United States, California ... more >> Stanford University, School of Medicine Stanford, California, United States, 94305 Collapse <<
  NCT01492192	Carcinoma, Renal Cell	Phase 2	Terminated	-	United Kingdom ... more >> Department of Radiology, Oxford University Hospitals NHS Trust Oxford, Oxfordshire, United Kingdom, OX3 7LJ Collapse <<
  NCT02995642	Aortic Aneurysm, Abdominal ... more >> Carotid Atherosclerosis Collapse <<	Phase 2	Not yet recruiting	December 2019	United States, California ... more >> Stanford University Not yet recruiting Stanford, California, United States, 94305 Contact: Andrea Otte    650-736-4183    anotte@stanford.edu    Contact: Lacey Greene, MS, CNMT    6507254712    lacey.greene@stanford.edu    Principal Investigator: Guido Davidzon, MD          Sub-Investigator: Andrei Iagaru, MD Collapse <<

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• 参考文献

• [1] Buckley CD, Pilling D, et al. RGD peptides induce apoptosis by direct caspase-3 activation. Nature. 1999 Feb 11;397(6719):534-9.

  [2] Ruoslahti E. RGD and other recognition sequences for integrins. Annu Rev Cell Dev Biol. 1996;12:697-715.

  [3] S Liu,et al. Integrin cytoplasmic domain-binding proteins. J Cell Sci. 2000 Oct;113 ( Pt 20):3563-71.

  [4] Mark H Ginsberg. Integrin activation. BMB Rep.2014 Dec;47(12):655-9.

  [5] Hersel U, et al. RGD modified polymers: biomaterials for stimulated cell adhesion and beyond. Biomaterials. 2003 Nov;24(24):4385-415.

  [6] E Ruoslahti. RGD and other recognition sequences for integrins. Annu Rev Cell Dev Biol. 1996;12:697-715.

  [7] C D Buckley,et al. RGD peptides induce apoptosis by direct caspase-3 activation. Nature. 1999 Feb 11;397(6719):534-9.

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