Wenwu Xiao

Well-Defined, Reversible Boronate Crosslinked Nanocarriers for Targeted Drug Delivery in Response to Acidic pH Values an...

Published in Angewandte Chemie International Edition in English

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...

Discovery of high-affinity peptide ligands for vancomycin.

Published in Biopolymers

Vancomycin, an important antibiotic against medically relevant gram-positive bacteria such as methicillin-resistant Staphylococcus aureus, exerts its antibacterial effects by binding with moderate affinity to the C-terminal Lys-D-Ala-D-Ala motif (Kaa) of the bacterial cell wall peptide precursor. Essential for Kaa binding to vancomcyin is the free-...

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...

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

Published in European Journal of Nuclear Medicine

Structure-activity relationship studies of targeting ligands against breast cancer cells.

Published in Journal of Medicinal Chemistry

A series of LXY3 (1) analogues were designed and synthesized. Their binding affinity was demonstrated using MDA-MB-231 breast cancer cells adherence inhibition assay. Further structure-activity relationship was obtained. Analogue 29 was discovered to have 3.5-fold increase of the binding affinity. Fluorescent microscopy and in vivo and ex vivo imag...

Biodistribution and pharmacokinetics of a telodendrimer micellar paclitaxel nanoformulation in a mouse xenograft model o...

Published in International Journal of Nanomedicine

Discovery of specific ligands for oral squamous carcinoma to develop anti-cancer drug loaded precise targeting nanothera...

Published in Journal of the California Dental Association

Oral squamous cell carcinoma has a low five-year survival rate, which may be due to late detection and a lack of effective tumor-specific therapies. Using a high throughput drug discovery strategy termed one-bead one-compound combinatorial library, the authors identified six compounds with high binding affinity to different human oral squamous cell...

Discovery of targeting ligands for breast cancer cells using the one-bead one-compound combinatorial method.

Published in Journal of Medicinal Chemistry

Four "one-bead one-compound" (OBOC) combinatorial libraries were designed, synthesized, and screened against MDA-MB-231 breast cancer cells. A novel cyclic peptide 1 (LXY1) with high binding specificity to alpha3 integrin was identified. Molecular interactions between alpha3 integrin and 1 were characterized by using a series of K562 cells transfec...

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...

The effect of surface charge on in vivo biodistribution of PEG-oligocholic acid based micellar nanoparticles.

Published in Biomaterials

To systematically elucidate the effect of surface charge on the cellular uptake and in vivo fate of PEG-oligocholic acid based micellar nanoparticles (NPs), the distal PEG termini of monomeric PEG-oligocholic acid dendrimers (telodendrimers) are each derivatized with different number (n = 0, 1, 3 and 6) of anionic aspartic acids (negative charge) o...

Nanomicelle formulation modifies the pharmacokinetic profiles and cardiac toxicity of daunorubicin.

Published in Nanomedicine

Well-defined, reversible disulfide cross-linked micelles for on-demand paclitaxel delivery.

Published in Biomaterials

To minimize premature release of drugs from their carriers during circulation in the blood stream, we have recently developed reversible disulfide cross-linked micelles (DCMs) that can be triggered to release drug at the tumor site or in cancer cells. We designed and synthesized thiolated linear-dendritic polymers (telodendrimers) by introducing cy...

Probing of the assembly structure and dynamics within nanoparticles during interaction with blood proteins.

Published in ACS Nano

Fully understanding the influence of blood proteins on the assembly structure and dynamics within nanoparticles is difficult because of the complexity of the system and the difficulty in probing the diverse elements and milieus involved. Here we show the use of site-specific labeling with spin probes and fluorophores combined with electron paramagn...

Immobilized OBOC combinatorial bead array to facilitate multiplicative screening.

Published in Current Topics in Medicinal Chemistry

One-bead-one-compound (OBOC) combinatorial library screening has been broadly utilized for the last two decades to identify small molecules, peptides or peptidomimetics targeting variable screening probes such as cell surface receptors, bacteria, protein kinases, phosphatases, proteases etc. In previous screening methods, library beads were suspend...

Mechanochemotransduction during cardiomyocyte contraction is mediated by localized nitric oxide signaling.

Published in Science Signaling

Cardiomyocytes contract against a mechanical load during each heartbeat, and excessive mechanical stress leads to heart diseases. Using a cell-in-gel system that imposes an afterload during cardiomyocyte contraction, we found that nitric oxide synthase (NOS) was involved in transducing mechanical load to alter Ca(2+) dynamics. In mouse ventricular ...

A smart and versatile theranostic nanomedicine platform based on nanoporphyrin.

Published in Nature Communications

Multifunctional nanoparticles with combined diagnostic and therapeutic functions show great promise towards personalized nanomedicine. However, attaining consistently high performance of these functions in vivo in one single nanoconstruct remains extremely challenging. Here we demonstrate the use of one single polymer to develop a smart all-in-one...

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...

Microfluidic-Enabled Print-to-Screen Platform for High-Throughput Screening of Combinatorial Chemotherapy.

Published in Analytical Chemistry

Since the 1960s, combination chemotherapy has been widely utilized as a standard method to treat cancer. However, because of the potentially enormous number of drug candidates and combinations, conventional identification methods of the effective drug combinations are usually associated with significantly high operational costs, low throughput scre...

Optimization of RGD-Containing Cyclic Peptides against αvβ3 Integrin.

Published in Molecular Cancer Therapeutics

We have previously reported the use of one-bead-one-compound (OBOC) combinatorial technology to develop a disulfide cyclic, Arg-Gly-Asp-containing octapeptide LXW7 (cGRGDdvc), that targets αvβ3 integrin with high affinity and specificity. αvβ3 integrin is known to be overexpressed in many cancers and in tumor vasculature, and it has been establishe...