Vascular-homing peptides for targeted drug delivery and molecular imaging: meeting the clinical challenges.
The vasculature of each organ expresses distinct molecular signatures critically influenced by the pathological status. The heterogeneous profile of the vascular beds has been successfully unveiled by the in vivo phage display, a high-throughput tool for mapping normal, diseased, and tumor vasculature. Specific challenges of this growing field are targeted therapies against cancer and cardiovascular diseases, as well as novel bioimaging diagnostic tools. Tumor vasculature-homing peptides have been extensively evaluated in several preclinical and clinical studies both as targeted-therapy and diagnosis. To date, results from several Phase I and II trials have been reported and many other trials are currently ongoing or recruiting patients. In this review, advances in the identification of novel peptide ligands and their corresponding receptors on tumor endothelium through the in vivo phage display technology are discussed. Emphasis is given to recent findings in the clinical setting of vascular-homing peptides selected by in vivo phage display for the treatment of advanced malignancies and their altered vascular beds.
Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, via L. de Crecchio 7, 80138 Naples, Italy.
Nunzia
N
D'Onofrio
Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, via L. de Crecchio 7, 80138 Naples, Italy.
Michele
M
Caraglia
Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, via L. de Crecchio 7, 80138 Naples, Italy.
Anna
A
Grimaldi
Department of Geriatrics and Metabolic Diseases, Second University of Naples, Piazza Miraglia 2, 80138 Naples, Italy.
Raffaele
R
Marfella
Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, via L. de Crecchio 7, 80138 Naples, Italy.
Luigi
L
Servillo
Department of Geriatrics and Metabolic Diseases, Second University of Naples, Piazza Miraglia 2, 80138 Naples, Italy.
Giuseppe
G
Paolisso
Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, via L. de Crecchio 7, 80138 Naples, Italy. Electronic address: marialuisa.balestrieri@unina2.it.
Maria Luisa
ML
Balestrieri
D020533:Angiogenesis Inhibitors / Q000008:administration & dosage / Q000302:isolation & purification; D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods*; D055808:Drug Discovery; D004730:Endothelium, Vascular / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D057054:Molecular Imaging / Q000379:methods*; D058990:Molecular Targeted Therapy; D009389:Neovascularization, Pathologic / Q000175:diagnosis* / Q000188:drug therapy*; D019151:Peptide Library; D010455:Peptides / Q000008:administration & dosage*
D020533:Angiogenesis Inhibitors; D019151:Peptide Library; D010455:Peptides
Cancer; Endothelium; Peptides; Phage display