The “One-Bead-One-Compound” Combinatorial Approach to Identifying Molecular Imaging Probes
Published in Cancer Biology & Therapy
Published in Journal of Nuclear Medicine
Published in Molecular Cancer Therapeutics
Published in Analytical Biochemistry
It is now routine using automatic Edman microsequencing to determine the primary structure of peptides or proteins containing natural amino acids; however, a deficiency in the ability to readily sequence peptides containing unnatural amino acids remains. With the advent of synthetic peptide chemistry, combinatorial chemistry, and the large number o...
Published in Genomics Proteomics & Therpaeutics
Published in Journal of Neurochemistry
Several small molecule ligands for amyloid-beta (Abeta) fibrils deposited in brain have been developed to facilitate radiological diagnosis of Alzheimer s disease (AD). Recently, the build-up of Abeta oligomers (AbetaO) in brain has been recognized as an additional hallmark of AD and may play a more significant role in early stages. Evidence sugges...
Published in Analytical Biochemistry
The search for small molecules that specifically recognize protein targets is a laborious process if conducted in a one protein-one compound manner. A high-throughput antibody-based screening of one bead-one compound (OBOC) combinatorial small molecule libraries is described here, whereby libraries containing thousands of different small molecule l...
Published in Molecular Cancer Therapeutics
Increasing literature suggests that cell adhesion molecule alpha4beta1 integrin plays a pivotal role in autoimmune diseases and cancer development. Noninvasive visualization of alpha4beta1 integrin in vivo will facilitate the understanding of its involvement in disease progression and development of targeted therapies. Due to the lack of high-affin...
Published in Biophysical Journal
Deposition of amyloid fibrils, consisting primarily of Aβ(40) and Aβ(42) peptides, in the extracellular space in the brain is a major characteristic of Alzheimer s disease (AD). We recently developed new (to our knowledge) drug candidates for AD that inhibit the fibril formation of Aβ peptides and eliminate their neurotoxicity. We performed all-ato...
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...
Published in Nature Medicine
Published in Journal of Nuclear Medicine
Published in Bioconjugate Chemistry
Nonspecific ligation methods have been traditionally used to chemically modify immunoglobulins. Site-specific ligation of compounds (toxins or ligands) to antibodies has become increasingly important in the fields of therapeutic antibody-drug conjugates and bispecific antibodies. In this present study, we took advantage of the reported nucleotide-b...