Publications

Publications
The Resazurin Reduction Assay Can Distinguish Cytotoxic from Cytostatic Compounds in Spheroid Screening Assays.
Journal of biomolecular screening

 Walzl A, Unger C, Kramer N, Unterleuthner D, Scherzer M, Hengstschläger M, Schwanzer-Pfeiffer D, Dolznig H
 Journal of biomolecular screening - vol. 19 1047-1059 (2014)

Spheroid-based cellular screening approaches represent a highly physiologic experimental setup to identify novel anticancer drugs and an innovative preclinical model to reduce the high failure rate of anticancer compounds in clinical trials. The resazurin reduction (RR) assay, known as the alamarBlue or CellTiter-Blue assay, is frequently used to determine cell viability/proliferation capacity in eukaryotic cells. […]

Publications
Anti-tumor activity of the beta-adrenergic receptor antagonist propranolol in neuroblastoma.
Oncotarget

 Wolter JK, Wolter NE, Blanch A, Partridge T, Cheng L, Morgenstern DA, Podkowa M, Kaplan DR, Irwin MS
 Oncotarget - vol. 5 161-172 (2014)

Neuroblastoma (NB) is a pediatric tumor of the sympathetic nervous system, which is often associated with elevated catecholamines. More than half of patients with metastatic NB relapse and survival is extremely poor with current therapies. In a high-throughput screen of FDA-approved drugs we identified anti-NB activity for the nonselective β-adrenergic receptor antagonist propranolol hydrochloride. Propranolol […]

Publications
A high throughput flow cytometric assay platform targeting transporter inhibition
Drug Discovery Today: Technologies

 Tegos GP, Evangelisti AM, Strouse JJ, Ursu O, Bologa C, Sklar LA
 Drug Discovery Today: Technologies - vol. 12 e95-e103 (2014)

This review highlights the concepts, recent applications and limitations of High Throughput Screening (HTS) flow cytometry-based efflux inhibitory assays. This platform has been employed in mammalian and yeast efflux systems leading to the identification of small molecules with transporter inhibitory capabilities. This technology offers the possibility of substrate multiplexing and may promote novel strategies targeting […]

Publications
Enzymatic Characterization of ER Stress-Dependent Kinase, PERK, and Development of a High-Throughput Assay for Identification of PERK Inhibitors
J Biomol screen

 Pytel D, Seyb K, Liu M, Ray SS, Concannon J, Huang M, Cuny GD, Diehl JA, Glicksman MA
 J Biomol screen - vol. 2 1024-1034 (2014)

PERK is serine/threonine kinase localized to the endoplasmic reticulum (ER) membrane. PERK is activated and contributes to cell survival in response to a variety of physiological stresses that affect protein quality control in the ER, such as hypoxia, glucose depravation, increased lipid biosynthesis, and increased protein translation. Pro-survival functions of PERK are triggered by such […]

Publications
Fishing for causes and cures of motor neuron disorders.
Disease models & mechanisms

 Patten SA, Armstrong GAB, Lissouba A, Kabashi E, Parker JA, Drapeau P
 Disease models & mechanisms - vol. 7 799-809 (2014)

Motor neuron disorders (MNDs) are a clinically heterogeneous group of neurological diseases characterized by progressive degeneration of motor neurons, and share some common pathological pathways. Despite remarkable advances in our understanding of these diseases, no curative treatment for MNDs exists. To better understand the pathogenesis of MNDs and to help develop new treatments, the establishment […]

Publications
Expanding the results of a high throughput screen against an isochorismate-pyruvate lyase to enzymes of a similar scaffold or mechanism
Bioorganic and Medicinal Chemistry

 Meneely KM, Luo Q, Riley AP, Taylor B, Roy A, Stein RL, Prisinzano TE, Lamb AL
 Bioorganic and Medicinal Chemistry - vol. 22 5961-5969 (2014)

Antibiotic resistance is a growing health concern, and new avenues of antimicrobial drug design are being actively sought. One suggested pathway to be targeted for inhibitor design is that of iron scavenging through siderophores. Here we present a high throughput screen to the isochorismate-pyruvate lyase of Pseudomonas aeruginosa, an enzyme required for the production of […]

Publications
Dystrophic muscle improvement in zebrafish via increased heme oxygenase signaling
Human molecular genetics

 Kawahara G, Gasperini MJ, Myers JA, Widrick JJ, Eran A, Serafini PR, Alexander MS, Pletcher MT, Morris CA, Kunkel LM
 Human molecular genetics - vol. 23 1869-1878 (2014)

Duchenne muscular dystrophy (DMD) is caused by a lack of the dystrophin protein and has no effective treatment at present. Zebrafish provide a powerful in vivo tool for high-throughput therapeutic drug screening for the improvement of muscle phenotypes caused by dystrophin deficiency. Using the dystrophin-deficient zebrafish, sapje, we have screened a total of 2640 compounds […]

Publications
Development of a Drosophila melanogaster spliceosensor system for in vivo high-throughput screening in myotonic dystrophy type 1.
Disease models & mechanisms

 García-Alcover I, Colonques-Bellmunt J, Garijo R, Tormo JR, Artero R, Álvarez-Abril MC, López Castel A, Pérez-Alonso M
 Disease models & mechanisms - vol. 7 1297-1306 (2014)

Alternative splicing of pre-mRNAs is an important mechanism that regulates cellular function in higher eukaryotes. A growing number of human genetic diseases involve splicing defects that are directly connected to their pathology. In myotonic dystrophy type 1 (DM1), several clinical manifestations have been proposed to be the consequence of tissue-specific missplicing of numerous genes. These […]

Publications
Induction of covalently crosslinked p62 oligomers with reduced binding to polyubiquitinated proteins by the autophagy inhibitor verteporfin
PLoS ONE

 Donohue E, Balgi AD, Komatsu M, Roberge M
 PLoS ONE - vol. 9 1-30 (2014)

Autophagy is a cellular catabolic process responsible for the degradation of cytoplasmic constituents, including organelles and long-lived proteins, that helps maintain cellular homeostasis and protect against various cellular stresses. Verteporfin is a benzoporphyrin derivative used clinically in photodynamic therapy to treat macular degeneration. Verteporfin was recently found to inhibit autophagosome formation by an unknown mechanism […]

Publications
Energetics-based methods for protein folding and stability measurements.
Annual review of analytical chemistry (Palo Alto, Calif.)

 Geer MA, Fitzgerald MC
 Annual review of analytical chemistry (Palo Alto, Calif.) - vol. 7 209-28 (2014)

Over the past 15 years, a series of energetics-based techniques have been developed for the thermodynamic analysis of protein folding and stability. These techniques include Stability of Unpurified Proteins from Rates of amide H/D Exchange (SUPREX), pulse proteolysis, Stability of Proteins from Rates of Oxidation (SPROX), slow histidine H/D exchange, lysine amidination, and quantitative cysteine […]

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