Integrin αvβ3 is a molecular marker for the estimation of tumor angiogenesis and is an imaging target for radiolabeled Arg-Gly-Asp (RGD) peptides. In this study, the authors investigated the clinical efficacy and safety of a novel radiolabeled RGD peptide, 99mTc-IDA-D-[c(RGDfK)]2, for the imaging of integrin αvβ3 expression, as a measure of tumor angiogenesis in lung cancers and brain tumors. F...

imaging of infection and inflammation is an important issue in nuclear medicine as it may have relevant implication for the management of patients with infections or inflammatory diseases. in this regard the synthesis of human polyclonal immunoglobuline g (igg) radiolabeled with technetium-99m (99mtc) by a novel method, via a nicotinamide hydrazine derivative, was performed. the biological beha...

The v 3 integrin is expressed on proliferating endothelial cells such as those present in growing tumors, as well as on tumor cells of various origin. Tumor-induced angiogenesis can be blocked in vivo by antagonizing the v 3 integrin with small peptides containing the Arg-Gly-Asp (RGD) amino acid sequence. This tripeptidic sequence, naturally present in extracellular matrix proteins, is the pri...

The alpha(v)beta(3) integrin is expressed on proliferating endothelial cells such as those present in growing tumors, as well as on tumor cells of various origin. Tumor-induced angiogenesis can be blocked in vivo by antagonizing the alpha(v)beta(3) integrin with small peptides containing the Arg-Gly-Asp (RGD) amino acid sequence. This tripeptidic sequence, naturally present in extracellular mat...

Abstract Dual functionalization of targeting vectors, such as peptides and antibodies, is still synthetically challenging despite the increasing demand for molecules serving multiple purposes (i.e., optical nuclear imaging). Our strategy was to synthesize a versatile building block via orthogonal incorporation chemical entities (e.g., radionuclide chelator, fluorescent dye, cytotoxic drugs, cli...

BACKGROUND Polybasic helical peptides, such as peptide p5, bind human amyloid extracts and synthetic amyloid fibrils. When radiolabeled, peptide p5 has been shown to specifically bind amyloid in vivo thereby allowing imaging of the disease. Structural requirements for heparin and amyloid binding have been studied using analogs of p5 that modify helicity and chirality. METHODS Peptide-ligand i...

BACKGROUND Uroguanylin is an endogenous peptide agonist that binds to the guanylate cyclase C receptor (GC-C). GC-C is overexpressed in human colorectal cancer (CRC), and exposure of GC-C-expressing cells to GC-C agonists results in cell cycle arrest and/or apoptosis, highlighting the therapeutic potential of such compounds. This study describes the first use of radiolabeled uroguanylin analogs...

This article reviews the results of somatostatin receptor imaging (SRI) in patients with somatostatin receptor–positive neuroendocrine tumors, such as pituitary tumors, endocrine pancreatic tumors, carcinoids, gastrinomas, and paragangliomas, or other diseases in which somatostatin receptors may also be expressed, like sarcoidosis and autoimmune diseases. [111InDTPA0]octreotide is a radiopharma...

Agouti-related protein (AgRP) is a 4-kDa cystine-knot peptide of human origin with four disulfide bonds and four solvent-exposed loops. The cell adhesion receptor integrin α(v)β(3) is an important tumor angiogenesis factor that determines the invasiveness and metastatic ability of many malignant tumors. AgRP mutants have been engineered to bind to integrin α(v)β(3) with high affinity and specif...

Metastatic melanoma remains an incurable disease, and there is a great need for novel therapeutic modalities. We have recently identified melanin as a target for radionuclide therapy of melanoma and demonstrated the feasibility of this approach using a 188-rhenium ( (188)Re)-radiolabeled melanin-binding decapeptide to fungal melanin known as 4B4. Although the results indicated that radiolabeled...