2003
DOI: 10.1021/jm030789z
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A New Biotin Derivative−DOTA Conjugate as a Candidate for Pretargeted Diagnosis and Therapy of Tumors

Abstract: The synthesis of a new biotin derivative, the (CO) reduced N-aminohexyl biotinamido derivative, designed to be serum biotinidase resistant, and its conjugation to the chelator DOTA through an amide bond at one of the four carboxymethyl chains are described. The (90)Y-labeled conjugate was able to bind avidin at different Av/conjugate molar ratios with good results. The preclinical results indicate that this new biotin-DOTA conjugate is a good candidate for pretargeted diagnosis and therapy of tumors.

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Cited by 44 publications
(50 citation statements)
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(28 reference statements)
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“…One possible problem in in vivo circumstances is the biotinidase enzyme (especially in plasma), which is capable of cleaving biotin-conjugates [80] and thereby lowering the targeting efficacy of the system. The development of biotin derivatives that are resistant to biotinidase, however, reduces the severity of this problem [81]. baculoviruses are taken up by a variety of cells, it would be useful to restrict viral transduction to the target cells.…”
Section: The Potential Of Novel Avidin Fusion Proteins In Medical Tarmentioning
confidence: 99%
“…One possible problem in in vivo circumstances is the biotinidase enzyme (especially in plasma), which is capable of cleaving biotin-conjugates [80] and thereby lowering the targeting efficacy of the system. The development of biotin derivatives that are resistant to biotinidase, however, reduces the severity of this problem [81]. baculoviruses are taken up by a variety of cells, it would be useful to restrict viral transduction to the target cells.…”
Section: The Potential Of Novel Avidin Fusion Proteins In Medical Tarmentioning
confidence: 99%
“…The monomer units combine into the active form, 2,3 so each avidin unit is capable of binding four biotin molecules. 3,4 The avidin-biotin system has been used as a tool for various purposes, such as the diagnosis 5 of, for example, tumours 6 and for isolation (affinity chromatography). 7 The intention of the present work was to use the avidin-biotin system in combination with positron emission tomography (PET) imaging to follow the fate of the transplanted islets of Langerhans.…”
Section: Introductionmentioning
confidence: 99%
“…68 Ga-1,4,7,10-tetra-azacyclododecane-1,4,7,10-tetraacetic acidTyr3-octreotide (DOTA-TOC), 68 Ga-DOTA-1-Nal-octreotide (DOTA-NOC), 68 Ga-DOTA-bombesin, 68 Ga-1,4,7-triazacyclononanetriacetic acid (NOTA)-RGD, 68 Ga-DOTAalbumin, and 68 Ga-DOTA-human epidermal growth factor (hEGF) are examples of such agents (Fig. 1) [8,[10][11][12][13][14][15]. Similarly, some agents, such as 68 Ga-[(4,6-MeO 2 sal) 2-BAPEN] + and 68 Ga-N 2 S 2 , are chelates of radioactive gallium and used for myocardial imaging [16][17][18].…”
Section: Introductionmentioning
confidence: 99%