Kreatech Biotechnology B.v.

Kreatech Diagnostics

Rijksuniversiteit Leiden

Stichting Klinische Research Academisch Medisch Centrum

Jan Reedijk

Tinka Jelsma

Robert Jochem Heetebrij

Herman Hendricus Volkers

Franciscus Michiel Van Den Berg

Hendrik Jan Houthoff

Remco Maria Van Es

Edwin Leo Lempers

Hendrick Jan Houthoff

Marieke Johanna Bloemink

Hendrik-Jan Houthoff

Marieke J Bloemink

Edwin L Lempers

Jan Hendrick Houthoff

The present invention provides improved methods for labeling nucleotides. The method of the invention for labeling nucleotides comprises the steps of: reacting a reactive moiety of a linker, which linker is a platinum compound having a stabilizing bridge and two reactive moieties, with an electron donating moiety of a spacer, which spacer comprises a chain having at least four atoms and at least one heteroatom in the chain, which spacer further comprises said electron donating moiety at one end of the chain and a reactive moiety at the other end of the chain; reacting the reactive moiety of said spacer with a label; reacting the other reactive moiety of said linker with a nucleotide. A major advantage of the invention is that all nucleotides can be labeled by the method of the invention, whereas until now the attachment of a label was mostly restricted to one or certain nucleotides.

Methods for labeling nucleotides, labeled nucleotides and useful intermediates

The present invention provides a labeled nucleoside having formula: where X represents an aliphatic diamine, and the labeling moiety comprises a label and a spacer, where the spacer is coupled at one end to a platinum atom and at the other end to the label, which spacer comprises a chain having at least four carbon atoms and at least one oxygen atom in the chain. The invention further provides a method for labeling a nucleoside, kits for labeling a nucleoside, and kits for producing a labeled nucleic acid.

Trans-platinum compound, and diagnostic kit

The invention provides platinum-based probe compounds having the structure: ##STR1## wherein: Pt is a platinum atom, PROBE is a probe biomolecule for associating to a target biomolecule, M is a detectable marker moiety, and X and Y are stabilizing substituents. Also provided are platinum-based labeling compounds having the structure: ##STR2## wherein: Pt is a platinum atom, M is a detectable marker moiety, A is a displaceable leaving group, and X and Y are stabilizing substituents. The invention further provides platinum-based linker compounds having the structure: ##STR3## wherein: Pt is a platinum atom, A and B are the same or different reactive moieties, and X and Y are stabilizing substituents. Other Pt.sup.II and Pt.sup.IV compounds are also provided. Moreover, the invention provides methods for the preparation and use of these compounds, as well as diagnostic kits which contain the compounds.

Platinum-containing compounds methods for their preparation and

Platinum-containing compounds, methods for their preparation and

Pt-containing compound, process for its preparation, and application of

Growing community of inventors

Leiden, Netherlands

Jan Reedijk