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Conjugation and Labeling Procedures for Isothiocyanato Derivatives

The preparation of DTPA coupled antibodies radiolabeled with metallic radionuclides: an improved method.

D. J. HNATOWICH, R. L. CHILDS, D. LANTEIGNE, A. NAJAFI, J. IMMUNOL. METHODS, 1983, 65, 147-157.
Abstract from www.NCBI.gov

Conjugation of antibodies with bifunctional chelating agents: isothiocyanate and bromoacetamido reagents, methods of analysis, and subsequent addition of metal ions.

Radiometal labeling of immunoproteins: covalent linkage of 2-(4-isothiocyanatobenzyl) diethylenetriaminepentaacetic acid ligands to immunoglobulin.

Macrocyclic chelates of radiometals for diagnosis and therapy.

An improved method for labeling monoclonal antibodies with samarium-153: use of the bifunctional chelate 2-(p-isothiocyanatobenzyl)-6-methyldiethylenetriaminepentaacetic acid.

A rapid, single vessel method for preparation of clinical grade ligand conjugated monoclonal antibodies.

Evaluation of a new DTPA-derivative chelator: comparative biodistribution and imaging studies of indium-111-labeled B3 monoclonal antibody in athymic mice bearing human epidermoid carcinoma xenographs.

Optimized conditions for chelation of yttrium-90-DOTA immunoconjugates.

Quantitative 89Zr immuno-PET for in vivo scouting of 90Y-labeled monoclonal antibodies in xenograft-bearing nude mice.

Comparative biodistribution of indium- and yttrium-labeled B3 monoclonal antibody conjugated to either 2-(p-SCN-Bz)-6-methyl-DTPA (1B4M-DTPA) or 2-(p-SCN-Bz)-1,4,7,10-tetraazacyclododecane tetraacetic acid (2B-DOTA).

Improved in vivo stability and tumor targeting of bismuth labeled antibody.

Quantitative 89Zr immuno-PET for in vivo scouting of 90Y-labeled monoclonal antibodies in xenograft bearing nude mice.

Specific localization, gamma camera imaging and intracellular trafficking of radiolabelled chimeric anti-G(D3) ganglioside monoclonal antibody KM871in SK-MEL-28 melanoma xenografts.

Targeting primary human Ph+ B-cell precursor leukemia-engrafted SCID mice usning radiolabeled anti-CD19 monoclonal antibodies.

Evaluation of the in vivo biodistribution of indium-111 and yttrium-88 labeled dendrimer-1B4M-DTPA and its conjugation with anti-Tac monoclonal antibody.

Pharmacokinetics, dosimetry and toxicity of the targetable atomic generator, 225Ac-HuM195, in nonhuman primates.

Comparison of 1,4,7,10-tetraazacyclododecane-N,N’,N”,N”’-tetraacetic acid (DOTA)-peptide-ChL6, a novel immunoconjugate with catabolizable linker, to 2-iminothiolane-2-p-(bromoacetamido)benzyl-DOTA-ChL6 in breast cancer xenografts.

Labeling anti-HER2/neu monoclonal antibodies with 111In and 90Y using a bifunctional DTPA chelating agent.

Alpha-emitting bismuth cyclohexylbenzyl DTPA constructs of recombinant humanized anti-CD33 antibodies: pharmacokinetics, bioactivity, toxicity and chemistry.

Pretargeted alpha-emitting radioimmunotherapy using 213Bi 1,4,7,10-tetraazacyclododecane-N,N’,N”,N”’-tetraacetic Acid-biotin.

Application of DOTA-tris(tert-Bu) in the Synthesis of DOTA-peptides

Solid-phase synthesis of DOTA-peptides.

L. M. DE LEON-RODRIGUEZ, Z. KOVACS, G. R. DIECKMANN, A. D. SHERRY, CHEM.EUR. J., 200410, 1149-1155.
Abstract from www.NCBI.gov

Magnetic resonance imaging detects a specific peptide-protein binding event.

Macrocyclic chelators with paramagnetic cations are internalized into mammalian cells via a HIV-Tat derived membrane translocation peptide.

Novel series of 111In-labeled bombesin analogs as potential radiopharmaceuticals for specific targeting of gastrin-releasing peptide receptors expressed on human prostate cancer cells.

Poly(L-glutamic acid) Gd(III)-DOTA conjugate with a degradable spacer for magnetic resonance imaging.

Chemical synthesis of Escherichia Coli ST h analogues by regioselectivedisulfide bond formation: biological evaluation of an 111In-DOTA-Phe 19-ST h analogue for specific targeting of human colon cancers.

Evaluation of cleavable (Tyr 3)-octreotate derivatives for longer intracellular probe residence.

Radiometal-labelled macrocyclic chelator-derivatised somatostatin analogue with superb tumour-targeting properties and potential for receptor-mediated internal radiotherapy.

Coupling with DOTA and Activated Esters of DOTA

An improved method for conjugating monoclonal antibodies with N-hydroxysulfosuccinidyl DOTA.

M. R. LEWIS, J. Y. KAO, A. L. ANDERSON, J. E. SHIVELY, A. RAUBITSCHEK, BIOCONJUGATE CHEM . 2001, 12, 320-324. Abstract from www.NCBI.gov

Vinyl sulfone bifunctional derivatives of DOTA allow sulfhydryl or amino-directed coupling to antibodies. Conjugates retain immunoreactivity and have similar biodistributions.

MicroPET and autoradiographic imaging of breast cancer a V-integrin expression using 18F- and 64Cu-labeled RGD peptide.

Conformation and structure of polymeric contrast agents for medical imaging.

Conjugation of DOTA using isolated phenolic active esters: the labeling and biodistribution of albumin as blood pool marker.

Direct synthesis of DOTA-DPhe 1-octreotide and DOTA-DPhe 1, Tyr 3-octreotide (SMT487): Two conjugates for systemic delivery of radiotherapeutical nuclides to somatostatin receptor positive tumors in man.

TmDOTP as an in vivo Temperature Probe

Brain temperature measured by 1H-NMR in conjunction with a lanthanide complex.

H. K. F. TRUBEL, P. K. MACIEJEWSKI, J. H. FARBER, F. HYDER J. APPL. PHYSIOL. 2003, 94, 1641-1649. Abstract from www.NCBI.gov

Simultaneous measurements of temperature and pH in Vivo using NMR in conjuction with TmDOTP5-.