2013
DOI: 10.1016/j.nucmedbio.2012.09.006
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[68Ga]NS3-RGD and [68Ga] Oxo-DO3A-RGD for imaging αvβ3 integrin expression: synthesis, evaluation, and comparison

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Cited by 18 publications
(16 citation statements)
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“…35 The fully protected, open peptide was cyclized using diphenylphosphorylazide (DPPA) and NaHCO 3 . 36 A mixture of the crude protected acyclic peptide (1 equiv, 90 μ mol, 100 mg), NaHCO 3 (5 equiv, 450 μ mol, 36 mg), DMF (100 mL), and DPPA (3 equiv, 270 μ mol, 80 mg) was stirred overnight. Upon confirming the completion of cyclization by ESI-MS, the solvent was evaporated under vacuum and deprotection was performed without purification using a mixture of TFA, H 2 O, and TES (95:2.5:2.5).…”
Section: Methodsmentioning
confidence: 99%
“…35 The fully protected, open peptide was cyclized using diphenylphosphorylazide (DPPA) and NaHCO 3 . 36 A mixture of the crude protected acyclic peptide (1 equiv, 90 μ mol, 100 mg), NaHCO 3 (5 equiv, 450 μ mol, 36 mg), DMF (100 mL), and DPPA (3 equiv, 270 μ mol, 80 mg) was stirred overnight. Upon confirming the completion of cyclization by ESI-MS, the solvent was evaporated under vacuum and deprotection was performed without purification using a mixture of TFA, H 2 O, and TES (95:2.5:2.5).…”
Section: Methodsmentioning
confidence: 99%
“…Although showing similar complexation characteristics, the oxo derivative did not inherit the advantage of kinetic inertness from the parent DOTA; however, p‐NO 2 ‐Bn‐PCTA shows both high kinetic inertness and favourable in vivo biodistribution characteristics. A study of the oxo derivative also shows inferior in vivo characteristics when conjugated to Arginylglycylaspartic acid (RGD) peptides . p‐NO 2 ‐Bn‐PCTA has subsequently been compared with a 1,4,7‐triazacyclononane‐1,4,7‐triacetic acid (NOTA) derivative for small peptide in vivo imaging and has been shown to have very similar properties, adding to the library of BFCs suitable for in vivo 68 Ga imaging …”
Section: Macrocyclic Chelatorsmentioning
confidence: 99%
“…Integrins a V b 3 have been shown to play an important role in a series of pathologic processes including angiogenesis and tumor cell metastasis (2,(13)(14)(15)(16)(17)(18). Given the high affinity of RGD-based peptides for a V b 3 integrin receptors, a variety of cyclic RGD peptide conjugates have been used to target tumors overexpressing these receptors (9)(10)(11)(12)(14)(15)(16)19,20). However, it has been demonstrated that the dimeric conjugate is more suitable, for both imaging and therapeutic applications, than the monomeric conjugate.…”
mentioning
confidence: 99%
“…Somatostatin analogs have been in use the longest, have led to the accumulation of a vast amount of data, and have proven useful for the management of patients with neuroendocrine tumors (4)(5)(6)(7)(8). Several other peptide receptorbinding compounds have been synthesized within the past few years and are currently in various research stages-in vitro, in vivo, and preclinical studies-but have not yet been approved for clinical use (9)(10)(11). These new and rapidly expanding peptide-based radiopharmaceuticals deserve close attention.…”
mentioning
confidence: 99%
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