Wolf Wrasidlo

Wolf Wrasidlo
University of California, San Diego | UCSD · Moores Cancer Center/Oncology

About

17
Publications
1,733
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409
Citations
Citations since 2017
0 Research Items
190 Citations
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2017201820192020202120222023010203040
2017201820192020202120222023010203040

Publications

Publications (17)
Article
Full-text available
Transcription factors (TFs) are a major class of protein signaling molecules that play a critical role in most cancers. OLIG2 is a bHLH TF essential for survival and expansion of the highly aggressive brain cancer, glioblastoma (GBM), and represents an attractive therapeutic target. TFs including OLIG2 are typically activated by dimerization, and T...
Article
Full-text available
Staurosporine (STS) is a potent pan-kinase inhibitor with marked activity against several chemotherapy-resistant tumor types in vitro. The translational progress of this compound has been hindered by poor pharmacokinetics and toxicity. We sought to determine whether liposomal encapsulation of STS would enhance antitumor efficacy and reduce toxicity...
Data
Liposomal uptake and morphological changes in U87 cells stably expressing GFP (green). Panel A is a brightfield image of the cells incubated with empty liposomes conjugated with fluorescent dye (BODIPY – red). Panel B shows these cells confocal imaged in the green channel (upper) and the red channel (lower). Panel C is a merge of green and red acqu...
Data
Characterization of staurosporine liposomes by DLS and SEM. (A) Size (diameter, nm) of staurosporine liposomes measured by differential light scattering (DLS). (B) Representative scanning transmission electron microscope (SEM) images showing the structure of staurosporine liposomes.
Data
Graphs A–G depict staurosporine effects on viability (MTT assay) of the glioblastoma cell lines U118 (A), U251 (B), A172 (C), GBM4 (D), GBM8 (E) PC3 prostate tumor (F), and MDA-MB-231 breast tumor (G). Experiments were performed in triplicate and the mean ± standard error of the mean is indicated. Abbreviations: conc, concentration; Lipo, liposomal...
Article
Full-text available
The localized conversion of inactive doxorubicin prodrug chemotherapeutics to pharmacalogically active forms is difficult to quantify in mouse tumor models because it occurs only in small regions of tissue. The tumor tissue extraction protocol and LC-MS/MS analysis method described here were optimized to obtain a detection limit of 7.8 pg for the a...
Article
Full-text available
Sparing sensitive healthy tissue from chemotherapy exposure is a critical challenge in the treatment of cancer. The work described here demonstrates the localized in vivo photo-activation of a new chemotherapy prodrug of doxorubicin (DOX). The DOX prodrug (DOX-PCB) was 200 times less toxic to cells, but released pure DOX when exposed to 365 nm ligh...
Article
Dextran-coated superparamagnetic iron oxide nanoparticles (dextran-SPIO conjugates) offer the attractive possibility of enhancing MRI imaging sensitivity so that small or diffuse lesions can be detected. However, systemically injected SPIOs are rapidly removed by macrophages. We engineered embryonic cells (HEK293T) to express major macrophage scave...
Article
Quantum dots (QDs) are attracting intense interest as fluorescence labeling agents for biomedical imaging because biocompatible coatings and relatively nontoxic rare earth metal QDs have emerged as possible options. QD photoemissions are bright, of narrow wavelength range, and very stable. We sought to encapsulate QDs within targeted PEGylated lipo...
Article
We report here the in vivo combined-modality imaging of multifunctional drug delivery nanoparticles. These dextran core-based stealth liposomal nanoparticles (nanosomes) contained doxorubicin, iron oxide for magnetic resonance imaging (MRI) contrast, and BODIPY for fluorescence. The particles were long-lived in vivo because of surface decoration wi...
Article
Full-text available
We have developed a synthetic route for the preparation of a hybrid bisubstrate small molecule based on a nucleoside. A prototype compound was designed and docked into the catalytic domain of the AdSS enzyme bridging the region between the magnesium center of the protein to the nucleoside region. The synthesis involves coupling a brominated peptide...
Article
Full-text available
Screening for novel anticancer drugs in chemical libraries isolated from marine organisms, we identified the lipopeptide somocystinamide A (ScA) as a pluripotent inhibitor of angiogenesis and tumor cell proliferation. The antiproliferative activity was largely attributable to induction of programmed cell death. Sensitivity to ScA was significantly...
Article
Full-text available
Calicheamicin thetaII is a member of the enediyne class of antitumor antibiotics that bind to DNA and induce apoptosis. These compounds differ, however, from conventional anticancer drugs as they bind in a sequence-specific manner noncovalently to DNA and cause sequence-selective oxidation of deoxyriboses and bending of the DNA helix. Calicheamicin...
Article
Two 4'-propylcarbonoxy derivatives (2,3) of etoposide (1), a topoisomerase II inhibitor, were synthesized and evaluated as potential prodrugs for anticancer therapy. Their activation via hydrolysis mechanisms was determined as a function of pH in buffer solutions, in human serum and in the presence of carboxyl ester hydrolase. Cytotoxicity was dete...
Chapter
Completely aromatic polymers offer a unique opportunity for studying molecular motions responsible for transition and relaxation effects. In linear aliphatic polymers relaxation processes are believed to originate in rotations, either of whole chains, chain segments or individual moieties within a molecular unit (1,2). In fully aromatic polymers ro...

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