Publications

Publications
Chemical Genetic Identification of the Histamine H1 Receptor as a Stimulator of Insulin-Induced Adipogenesis
Chemistry & Biology

 Mech LD
 Chemistry & Biology - vol. 11 907-913 (2014)

Alarge collection of bioactivecompoundswith diverse biological effects can be used as probes to elucidate new biological mechanisms that influence a particular cellular process. Here we analyze the effects of 880 well-known small-molecule bioactives or drugs on the insulin-induced adipogenesis of 3T3-L1 fibroblasts, a cell-culturemodelof fat cell differentiation. Our screen identified 86 compounds as modulators of […]

Publications
Chemical con artists foil drug discovery
Nature

 Baell J, Walters MA
 Nature - vol. 513 481-483 (2014)

Naivety about promiscuous, assay-duping molecules is polluting the literature and wasting resources, warn Jonathan Baell and Michael A. Walters

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 […]

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