Ruiwu (Ray) Liu

The “One-Bead-One-Compound” Combinatorial Approach to Identifying Molecular Imaging Probes

High throughput screening of a small molecule one-bead-one-compound combinatorial library to identify attenuators of p21...

Published in Cancer Biology & Therapy

111In-LLP2A-DOTA Polyethylene Glycol–Targeting α4β1 Integrin: Comparative Pharmacokinetics for Imaging and Therapy of Ly...

Published in Journal of Nuclear Medicine

Peptide Combinatorial Libraries

Novel peptide ligands for a4b1 integrin over-expressed in bronchiolalveolar cancer cells

Published in Molecular Cancer Therapeutics

Automatic Edman microsequencing of peptides containing multiple unnatural amino acids.

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...

Designed amino acids that induce b-sheet folding and b-sheet interactions in peptides

Development of peptidomimetic substrates and inhibitors that bind to the peptide binding pocket of the catalytic site of...

Development and characterization of potent and specific peptide inhibitors of p60c-src protein tyrosine kinase using pse...

Published in Journal of Peptide Research

The cytoplasmic protein p60c-src, an ubiquitous non-receptor protein tyrosine kinase (PTK) is a potential anticancer target as it is over-expressed and/or constitutively active in several cancer types. In addition, the phenotype of c-src knock-out mice is consistent with osteopetrosis, which suggests that inhibitors against this enzyme may also be ...

An unnatural amino acid that induces beta-sheet folding and interaction in peptides.

Published in Journal of the American Chemical Society

This paper introduces a unique amino acid that can readily be incorporated into peptides to make them fold into beta-sheetlike structures that dimerize through beta-sheet interactions. This new amino acid, Orn(i-PrCO-Hao), consists of an ornithine residue with the beta-strand-mimicking amino acid Hao [J. Am. Chem. Soc. 2000, 122, 7654-7661] attache...

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

Applications of topologically segregated bilayer beads in one-bead one-compound combinatorial libraries.

Published in Journal of Peptide Research

We recently reported the use of a biphasic approach to generate topologically segregated bilayer beads. In generating one-bead one-compound (OBOC) combinatorial libraries, novel encoding methods have been applied to these beads such as the testing library compound and the coding tags residing on the outer layer and inner core of each bead, respec...

Partial alloc-deprotection approach for ladder synthesis of "one-bead one-compound" combinatorial libraries.

Published in Journal of Combinatorial Chemistry

The topologically segregated bilayer-bead concept has been applied to encoded "one-bead one-compound"(OBOC) combinatorial libraries to avoid the interference of coding tags with biological screening. In this paper, we report on the development of a novel partial Alloc-deprotection (PAD) approach and the use of this approach to establish a new ladde...

In vivo optical imaging of human lymphoma xenograft using a library-derived peptidomimetic against alpha4beta1 integrin....

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...

Near-infrared optical imaging in glioblastoma xenograft with ligand-targeting alpha 3 integrin.

Published in European Journal of Nuclear Medicine

Development of hydrogel TentaGel shell-core beads for ultrahigh throughput solution-phase screening of encoded OBOC comb...

Published in Journal of Combinatorial Chemistry

The one-bead one-compound (OBOC) combinatorial library method enables the rapid generation and screening of millions of discrete chemical compounds on beads. Most of the OBOC screening methods require the library compounds to remain tethered to the bead during screening process. Methods have also been developed to release library compounds from imm...

Directing mesenchymal stem cells to bone to augment bone formation and increase bone mass

Published in Nature Medicine

Molecular imaging of very late antigen-4 (α4β1 integrin) in the premetastatic niche.

Published in Journal of Nuclear Medicine

In-vivo biodistribution and safety of 99mTc-LLP2A-HYNIC in canine non-Hodgkin lymphoma.

Theranostic agents are critical for improving the diagnosis and treatment of non-Hodgkin Lymphoma (NHL). The peptidomimetic LLP2A is a novel peptide receptor radiotherapy candidate for treating NHL that expresses the activated α4β1 integrin. Tumor-bearing dogs are an excellent model of human NHL with similar clinical characteristics, behavior, and ...

Molecular characteristics of CTA056, a novel interleukin-2-inducible T-cell kinase inhibitor that selectively targets ma...

Published in Molecular Pharmacology

Interleukin-2-inducible T-cell kinase (Itk) is a member of the Btk (Bruton s tyrosine kinase) family of tyrosine kinases. Itk plays an important role in normal T-cell functions and in the pathophysiology of both autoimmune diseases and T-cell malignancies. Here, we describe the initial characterization of a selective inhibitor, 7-benzyl-1-(3-(piper...