University of Massachusetts

Boston University

Immunomedics, Inc.

Univ. of Mass. Medical Center

Donald J Hnatowich

Mary Rusckowski

Charles Cantor

Takeshi Sano

Cassandra L Smith

Christof M Niemeyer

Guozheng Liu

Paul Winnard, Jr

George Mardirossian

Fengchun Chang

The present invention provides a kit and a method for targeting of a diagnostic or therapeutic agent to a target site in a mammal having a pathological condition. The kit comprises, in separate containers, (a) a first conjugate comprising a targeting moiety and a Morpholino oligomer, wherein the targeting moiety selectively binds to a primary, target-specific binding site of the target site or to a substance produced by or associated with the target site; (b) optionally, a clearing agent; and (c) a second conjugate comprising a complementary Morpholino oligomer and a diagnostic agent or therapeutic agent. The method comprises administering (a), optionally (b), and (c) to a mammal.

Morpholino imaging and therapy

Compositions of radiolabeled nucleic acids and methods for synthesis and use thereof are disclosed.

Chelator compositions and methods of synthesis thereof

The invention is directed to constructs and compositions containing multimeric forms of nucleic acid. Multimeric nucleic acids comprise single-stranded nucleic acids attached via biotin to streptavidin and bound with a functional group. These constructs can be utilized in vivo to treat or identify diseased tissue or cells. Repeated administrations of multimeric nucleic acid compositions produce a rapid and specific amplification of nucleic acid constructs and their attached functional groups. For treatment purposes, functional groups may be toxins, radioisotopes, genes or enzymes. Diagnostically, labeled multimeric constructs may be used to identify specific targets in vivo or in vitro. Multimeric nucleic acids may also be used in nanotechnology and to create self-assembling polymeric aggregates such as membranes of defined porosity, microcircuits and many other products.

Self-assembling multimeric nucleic acid constructs

Amines, including proteins and polypeptides covalently coupled with a chelating agent such as diethylenetriaminepentaacetic acid (DTPA) can be labeled with .sup.99m Tc in the presence of a stannous reducing agent at near neutral pH by maintaining the protein concentration at a low level and the DTPA concentration at a high level. The .sup.99m Tc is labeled to the protein through the DTPA sites linked to the protein. Utilizing .sup.111 In labeled proteins as controls, it is shown that the .sup.99m Tc labeled proteins are labeled at the DTPA sites and that they exhibit in vivo stabilities equal to that of the .sup.111 In labeled proteins.

Process for labeling amines with .sup.99m Tc

A dicyclic dianhydride rapidly and efficiently couples with a broad variety of amines such as polypeptides and proteins in non-aqueous or aqueous media and then may be chelated with a wide choice of radioisotope metallic cations to yield a radio-labeled product that is stable in vivo. A simple 1-step synthesis of the coupled amine in aqueous solution of neutral pH is described which requires only a few minutes time and with little accompanying hydrolysis.

Growing community of inventors

Brookline, MA, United States of America

Donald J Hnatowich