@article{enamorado_connelly_deiters_comins_2015, title={A concise synthesis of the Lycopodium alkaloid cermizine D}, volume={56}, ISSN={["0040-4039"]}, DOI={10.1016/j.tetlet.2015.04.013}, abstractNote={A racemic and asymmetric synthesis of cermizine D (1) was accomplished in six steps from 4-methoxypyridine or 4-methoxy-3-TIPS-pyridine in 12% and 13% overall yield, respectively. A key step is a stereoselective 1,4-addition of a 2-((trimethylsilyl)methyl)pyridine-derived cuprate to a bicyclic 2,3-dihydro-4-pyridone. Racemic and (−)-cermizine D failed to exhibit cytotoxicity against four different cell lines.}, number={23}, journal={TETRAHEDRON LETTERS}, author={Enamorado, Monica F. and Connelly, Colleen M. and Deiters, Alexander and Comins, Daniel L.}, year={2015}, month={Jun}, pages={3683–3685} }
 @article{naro_thomas_stephens_connelly_deiters_2015, title={Aryl amide small-molecule inhibitors of microRNA miR-21 function}, volume={25}, ISSN={["1464-3405"]}, DOI={10.1016/j.bmcl.2015.07.016}, abstractNote={MicroRNAs (miRNAs) are single stranded RNA molecules of ∼22 nucleotides that negatively regulate gene expression. MiRNAs are involved in fundamental cellular processes, such as development, differentiation, proliferation, and survival. MiRNA misregulation has been linked to various human diseases, most notably cancer. MicroRNA-21 (miR-21), a well-established oncomiR, is significantly overexpressed in many types of human cancers, thus rendering miR-21 a potential therapeutic target. Using a luciferase-based reporter assay under the control of miR-21 expression, a high-throughput screen of >300,000 compounds led to the discovery of a new aryl amide class of small-molecule miR-21 inhibitors. Structure–activity relationship (SAR) studies resulted in the development of four aryl amide derivatives as potent and selective miR-21 inhibitors. The intracellular levels of various miRNAs in HeLa cells were analyzed by qRT-PCR revealing specificity for miR-21 inhibition over other miRNAs. Additionally, preliminary mechanism of action studies propose a different mode of action compared to previously reported miR-21 inhibitors, thus affording a new chemical probe for future studies.}, number={21}, journal={BIOORGANIC & MEDICINAL CHEMISTRY LETTERS}, author={Naro, Yuta and Thomas, Meryl and Stephens, Matthew D. and Connelly, Colleen M. and Deiters, Alexander}, year={2015}, month={Nov}, pages={4793–4796} }
 @article{vonlanthen_connelly_deiters_linden_finney_2014, title={Thiourea-Based Fluorescent Chemosensors for Aqueous Metal Ion Detection and Cellular Imaging}, volume={79}, ISSN={["1520-6904"]}, DOI={10.1021/jo500710g}, abstractNote={We describe three significant advances in the use of thioureas as reporting elements for metal-responsive fluorescent chemosensors. First, on the basis of the crystal structure of a chemosensor analogue, we provide a deeper understanding of the details of the thiourea coordination environment. Second, we describe a new generation of chemosensors with higher affinities for Zn(2+) and Cd(2+) than were observed for earlier probes, expanding the scope of this type of probe beyond Hg(2+) detection. Third, we show that a thiourea-based chemosensor can be employed for fluorescence microscopy imaging of Hg(2+) ion concentrations in living mammalian cells.}, number={13}, journal={JOURNAL OF ORGANIC CHEMISTRY}, author={Vonlanthen, Mireille and Connelly, Colleen M. and Deiters, Alexander and Linden, Anthony and Finney, Nathaniel S.}, year={2014}, month={Jul}, pages={6054–6060} }
 @article{connelly_thomas_deiters_2012, title={High-Throughput Luciferase Reporter Assay for Small-Molecule Inhibitors of MicroRNA Function}, volume={17}, ISSN={["1087-0571"]}, DOI={10.1177/1087057112439606}, abstractNote={MicroRNAs (miRNAs) are endogenous, single-stranded, noncoding RNAs of 21 to 23 nucleotides that regulate gene expression, typically by binding the 3′ untranslated regions of target messenger RNAs. It is estimated that miRNAs are involved in the regulation of 30% of all genes and almost every genetic pathway. Recently, the misregulation of miRNAs has been linked to various human diseases including cancer and viral infections, identifying miRNAs as potential targets for drug discovery. Thus, small-molecule modifiers of miRNAs could serve as lead structures for the development of new therapeutic agents and be useful tools in the elucidation of detailed mechanisms of miRNA function. As a result, we have developed a high-throughput screen for potential small-molecule regulators of the liver-specific microRNA miR-122, which is involved in hepatocellular carcinoma development and hepatitis C virus infection. Our small-molecule screen employs a Huh7 human hepatoma cell line stably transfected with a Renilla luciferase sensor for endogenous miR-122. The assay was optimized and validated using an miR-122 antisense agent and a previously identified small-molecule miR-122 inhibitor. The described reporter assay will enable the high-throughput screening of small-molecule miR-122 inhibitors and can be readily extended to other miRNAs.}, number={6}, journal={JOURNAL OF BIOMOLECULAR SCREENING}, author={Connelly, Colleen M. and Thomas, Meryl and Deiters, Alexander}, year={2012}, month={Jul}, pages={822–828} }
 @article{connelly_uprety_hemphill_deiters_2012, title={Spatiotemporal control of microRNA function using light-activated antagomirs}, volume={8}, ISSN={["1742-206X"]}, DOI={10.1039/c2mb25175b}, abstractNote={MicroRNAs (miRNAs) are small non-coding RNAs that act as post-transcriptional gene regulators and have been shown to regulate many biological processes including embryonal development, cell differentiation, apoptosis, and proliferation. Variations in the expression of certain miRNAs have been linked to a wide range of human diseases - especially cancer - and the diversity of miRNA targets suggests that they are involved in various cellular networks. Several tools have been developed to control the function of individual miRNAs and have been applied to study their biogenesis, biological role, and therapeutic potential; however, common methods lack a precise level of control that allows for the study of miRNA function with high spatial and temporal resolution. Light-activated miRNA antagomirs for mature miR-122 and miR-21 were developed through the site-specific installation of caging groups on the bases of selected nucleotides. Installation of caged nucleotides led to complete inhibition of the antagomir-miRNA hybridization and thus inactivation of antagomir function. The miRNA-inhibitory activity of the caged antagomirs was fully restored upon decaging through a brief UV irradiation. The synthesized antagomirs were applied to the photochemical regulation of miRNA function in mammalian cells. Moreover, spatial control over antagomir activity was obtained in mammalian cells through localized UV exposure. The presented approach enables the precise regulation of miRNA function and miRNA networks with unprecedented spatial and temporal resolution using UV irradiation and can be extended to any miRNA of interest.}, number={11}, journal={MOLECULAR BIOSYSTEMS}, author={Connelly, Colleen M. and Uprety, Rajendra and Hemphill, James and Deiters, Alexander}, year={2012}, pages={2987–2993} }
 @article{young_connelly_grohmann_deiters_2010, title={Small Molecule Modifiers of MicroRNA miR-122 Function for the Treatment of Hepatitis C Virus Infection and Hepatocellular Carcinoma}, volume={132}, ISSN={["1520-5126"]}, DOI={10.1021/ja910275u}, abstractNote={MicroRNAs are a recently discovered new class of important endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation has the potential to provide new therapeutic approaches to such diseases. Here, we report the first small molecule inhibitors and activators of the liver-specific microRNA miR-122. This microRNA is the most abundant microRNA in the liver and is involved in hepatocellular carcinoma development and hepatitis C virus (HCV) infection. Our small molecule inhibitors reduce viral replication in liver cells and represent a new approach to the treatment of HCV infections. Moreover, small molecule activation of miR-122 in liver cancer cells selectively induced apoptosis through caspase activation, thus having implications in cancer chemotherapy. In addition to providing a new approach for the development of therapeutics, small molecule modifiers of miR-122 function are unique tools for exploring miR-122 biogenesis.}, number={23}, journal={JOURNAL OF THE AMERICAN CHEMICAL SOCIETY}, author={Young, Douglas D. and Connelly, Colleen M. and Grohmann, Christoph and Deiters, Alexander}, year={2010}, month={Jun}, pages={7976–7981} }