@article{govan_mciver_riggsbee_deiters_2012, title={Hydrogen Peroxide Induced Activation of Gene Expression in Mammalian Cells using Boronate Estrone Derivatives}, volume={51}, ISSN={["1521-3773"]}, DOI={10.1002/anie.201203222}, abstractNote={Keeping the boron out of the ER: A genetic switch was engineered that activates gene expression in the presence of H(2)O(2). The use of a boronate group on an estrone molecule allows for activation of gene expression through binding of the estrogen receptor only when the boron group is oxidized by H(2)O(2). This sensor is highly sensitive and specific for H(2)O(2).}, number={36}, journal={ANGEWANDTE CHEMIE-INTERNATIONAL EDITION}, author={Govan, Jeane M. and McIver, Andrew L. and Riggsbee, Chad and Deiters, Alexander}, year={2012}, pages={9066–9070} } @article{dush_mciver_parr_young_fisher_newman_sannes_hauck_deiters_nascone-yoder_2011, title={Heterotaxin: A TGF-beta Signaling Inhibitor Identified in a Multi-Phenotype Profiling Screen in Xenopus Embryos}, volume={18}, ISSN={["1879-1301"]}, DOI={10.1016/j.chembiol.2010.12.008}, abstractNote={Disruptions of anatomical left-right asymmetry result in life-threatening heterotaxic birth defects in vital organs. We performed a small molecule screen for left-right asymmetry phenotypes in Xenopus embryos and discovered a pyridine analog, heterotaxin, which disrupts both cardiovascular and digestive organ laterality and inhibits TGF-β-dependent left-right asymmetric gene expression. Heterotaxin analogs also perturb vascular development, melanogenesis, cell migration, and adhesion, and indirectly inhibit the phosphorylation of an intracellular mediator of TGF-β signaling. This combined phenotypic profile identifies these compounds as a class of TGF-β signaling inhibitors. Notably, heterotaxin analogs also possess highly desirable antitumor properties, inhibiting epithelial-mesenchymal transition, angiogenesis, and tumor cell proliferation in mammalian systems. Our results suggest that assessing multiple organ, tissue, cellular, and molecular parameters in a whole organism context is a valuable strategy for identifying the mechanism of action of bioactive compounds.}, number={2}, journal={CHEMISTRY & BIOLOGY}, author={Dush, Michael K. and McIver, Andrew L. and Parr, Meredith A. and Young, Douglas D. and Fisher, Julie and Newman, Donna R. and Sannes, Philip L. and Hauck, Marlene L. and Deiters, Alexander and Nascone-Yoder, Nanette}, year={2011}, month={Feb}, pages={252–263} } @article{govan_mciver_deiters_2011, title={Stabilization and Photochemical Regulation of Antisense Agents through PEGylation}, volume={22}, ISSN={["1520-4812"]}, DOI={10.1021/bc200411n}, abstractNote={Oligonucleotides are effective tools for the regulation of gene expression in cell culture and model organisms, most importantly through antisense mechanisms. Due to the inherent instability of DNA antisense agents, various modifications have been introduced to increase the efficacy of oligonucleotides, including phosphorothioate DNA, locked nucleic acids, peptide nucleic acids, and others. Here, we present antisense agent stabilization through conjugation of a poly(ethylene glycol) (PEG) group to a DNA oligonucleotide. By employing a photocleavable linker between the PEG group and the antisense agent, we were able to achieve light-induced deactivation of antisense activity. The bioconjugated PEG group provides stability to the DNA antisense agent without affecting its native function of silencing gene expression via RNase H-catalyzed mRNA degradation. Once irradiated with UV light of 365 nm, the PEG group is cleaved from the antisense agent leaving the DNA unprotected and open for degradation by endogenous nucleases, thereby restoring gene expression. By using a photocleavable PEG group (PhotoPEG), antisense activity can be regulated with high spatial and temporal resolution, paving the way for precise regulation of gene expression in biological systems.}, number={10}, journal={BIOCONJUGATE CHEMISTRY}, author={Govan, Jeane M. and McIver, Andrew L. and Deiters, Alexander}, year={2011}, month={Oct}, pages={2136–2142} } @article{georgianna_lusic_mclver_deiters_2010, title={Photocleavable Polyethylene Glycol for the Light-Regulation of Protein Function}, volume={21}, ISSN={["1043-1802"]}, DOI={10.1021/bc100084n}, abstractNote={PEGylation is commonly employed to enhance the pharmacokinetic properties of proteins, but it can interfere with natural protein function. Protein activity can thus be abrogated through PEGylation, and a controllable means to remove the polyethylene glycol (PEG) group from the protein is desirable. As such, light affords a unique control over biomolecules through the application of photosensitive groups. Herein, we report the synthesis of a photocleavable PEG reagent (PhotoPEG) and its application to the light-regulation of enzyme activity.}, number={8}, journal={BIOCONJUGATE CHEMISTRY}, author={Georgianna, Wesleigh E. and Lusic, Hrvoje and Mclver, Andrew L. and Deiters, Alexander}, year={2010}, month={Aug}, pages={1404–1407} } @article{mciver_deiters_2010, title={Tricyclic Alkaloid Core Structures Assembled by a Cyclotrimerization-Coupled Intramolecular Nucleophilic Substitution Reaction}, volume={12}, ISSN={["1523-7052"]}, DOI={10.1021/ol100177u}, abstractNote={A facile approach to tricyclic alkaloid core structures was developed by sequencing a pyridine-forming [2 + 2 + 2] cyclotrimerization reaction with an intramolecular nucleophilic substitution. This methodology enabled the facile assembly of the spiroindolinone framework of citrinadins A and B, and cyclopiamine B.}, number={6}, journal={ORGANIC LETTERS}, author={McIver, Andrew L. and Deiters, Alexander}, year={2010}, month={Mar}, pages={1288–1291} } @article{mciver_young_deiters_2008, title={A general approach to triphenylenes and azatriphenylenes: total synthesis of dehydrotylophorine and tylophorine}, ISSN={["1359-7345"]}, DOI={10.1039/b811068a}, abstractNote={A convergent and flexible synthesis of substituted triphenylenes, azatriphenylenes, and the cytotoxic alkaloids dehydrotylophorine and tylophorine has been developed.}, number={39}, journal={CHEMICAL COMMUNICATIONS}, author={McIver, Andrew and Young, Douglas D. and Deiters, Alexander}, year={2008}, pages={4750–4752} }