Pappanaicken Kumaresan

From One-Bead One-Compound Combinatorial Libraries to Chemical Microarrays

Screening chemical microarrays: methods and applications.

Published in Molecular BioSystems

Development of tissue plasminogen activator specific "on demand cleavable" (odc) linkers for radioimmunotherapy by scree...

Published in Bioconjugate Chemistry

New strategies are needed to protect normal organs from radiation in cancer radioimmunotherapy (RIT). This can be achieved by rapid clearance of radiometal in the circulation after accumulation of radioimmunoconjugates (RIC) in the tumor. Our strategy is to place highly efficient and specific cleavable linkers between radiometal chelates and the tu...

Evaluation of ketone-oxime method for developing therapeutic on-demand cleavable immunoconjugates.

Published in Bioconjugate Chemistry

The use of antibody molecules in immunoassay, molecular targeting, or detection techniques encompasses a broad variety of applications affecting nearly every field of medical science. In cancer therapy, monoclonal antibodies (mAb) have been used as vehicles to deliver radionuclides, toxins, or drugs to the target cancer cells. New conjugation metho...

Rainbow beads: a color coding method to facilitate high-throughput screening and optimization of one-bead one-compound c...

Published in Journal of Combinatorial Chemistry

We have developed a new color-encoding method that facilitates high-throughput screening of one-bead one-compound (OBOC) combinatorial libraries. Polymer beads displaying chemical compounds or families of compounds are stained with oil-based organic dyes that are used as coding tags. The color dyes do not affect cell binding to the compounds displa...

Synthesis and Characterization of a Novel Inhibitor of C-Reactive Protein–Mediated Proinflammatory Effects

Published in Metabolic Syndrome and Related Disorders

A novel peptide inhibitor attenuates C-reactive protein s pro-inflammatory effects in-vivo.

Published in International Journal of Cardiology

Development of TNKase-specific cleavable peptide-linked radioimmunoconjugates for radioimmunotherapy.

Published in Bioorganic & Medicinal Chemistry Letters

Radioimmunotherapy (RIT) is a method for selectively delivering radionuclides to cancer cells while reducing the radiation dose to normal tissues. However, because of slow clearance of MAbs, normal tissues also received radiotoxicity. One of the promising strategies is linking on-demand cleavable (ODC) peptides between radiometal chelates and the t...

On-demand cleavable linkers for radioimmunotherapy.

Published in Methods in Molecular Biology

Radioimmunotherapy (RIT) using radiolabeled antibodies or its fragments holds great promise for cancer therapy. However, its clinical potential is often limited by the undesirable radiation exposure to normal organs such as liver, kidney, and bone marrow. It is important to develop new strategies in RIT that enable protection of vital organs from r...

The use of one-bead one-compound combinatorial library technology to discover high-affinity αvβ3 integrin and cancer tar...

Published in Molecular Cancer Therapeutics

The αvβ3 integrin, expressed on the surface of various normal and cancer cells, is involved in numerous physiologic processes such as angiogenesis, apoptosis, and bone resorption. Because this integrin plays a key role in angiogenesis and metastasis of human tumors, αvβ3 integrin ligands are of great interest to advances in targeted therapy and can...

Rapid discovery of death ligands with one-bead-two-compound combinatorial library methods.

Published in ACS Combinatorial Science

The one-bead-one-compound (OBOC) technology enables one to generate thousands to millions of chemical molecules on resin beads (90 μm diameter) such that each bead displays 10(13) copies of the same chemical entity. Whole-cell binding assays have been developed to screen OBOC combinatorial libraries for ligands that bind to specific cell surface re...

Targeting Btk/Etk of prostate cancer cells by a novel dual inhibitor.

Published in Cell Death and Disease

Btk and Etk/BMX are Tec-family non-receptor tyrosine kinases. Btk has previously been reported to be expressed primarily in B cells and has an important role in immune responses and B-cell malignancies. Etk has been shown previously to provide a strong survival and metastasis signal in human prostate cancer cells, and to confer androgen independenc...

Design, synthesis, and application of OB2C combinatorial peptide and peptidomimetic libraries.

Published in Methods in Molecular Biology

The "one-bead two-compound" (OB2C) combinatorial library is constructed on topologically segregated trifunctional bilayer beads such that each bead has a fixed cell-capturing ligand and a random library compound co-displayed on its surface and a chemical coding tag (bar code) inside the bead. An OB2C library containing thousands to millions of comp...