Neoclassic drug discovery: the case for lead generation using phenotypic and functional approaches

JA Lee, EL Berg - Journal of biomolecular screening, 2013 - journals.sagepub.com
Innovation and new molecular entity production by the pharmaceutical industry has been
below expectations. Surprisingly, more first-in-class small-molecule drugs approved by the …

Designing drugs that overcome antibacterial resistance: where do we stand and what should we do?

R Penchovsky, M Traykovska - Expert opinion on drug discovery, 2015 - Taylor & Francis
Introduction: In recent years, infections caused by multidrug-resistant bacterial pathogens
have become a huge issue to public healthcare systems. Indeed, the misuse of antibiotics …

T-probe: an integrated microscale device for online in situ single cell analysis and metabolic profiling using mass spectrometry

R Liu, N Pan, Y Zhu, Z Yang - Analytical chemistry, 2018 - ACS Publications
The exploration of single cells reveals cell heterogeneity and biological principle of cellular
metabolism. Although a number of mass spectrometry (MS) based single cell MS (SCMS) …

ITGB1-dependent upregulation of Caveolin-1 switches TGFβ signalling from tumour-suppressive to oncogenic in prostate cancer

T Pellinen, S Blom, S Sánchez, K Välimäki… - Scientific Reports, 2018 - nature.com
Abstract Caveolin-1 (CAV1) is over-expressed in prostate cancer (PCa) and is associated
with adverse prognosis, but the molecular mechanisms linking CAV1 expression to disease …

Tissue Phenomics for prognostic biomarker discovery in low-and intermediate-risk prostate cancer

N Harder, M Athelogou, H Hessel, N Brieu, M Yigitsoy… - Scientific reports, 2018 - nature.com
Tissue Phenomics is the discipline of mining tissue images to identify patterns that are
related to clinical outcome providing potential prognostic and predictive value. This involves …

Identifying and quantifying heterogeneity in high content analysis: application of heterogeneity indices to drug discovery

AH Gough, N Chen, TY Shun, TR Lezon, RC Boltz… - PloS one, 2014 - journals.plos.org
One of the greatest challenges in biomedical research, drug discovery and diagnostics is
understanding how seemingly identical cells can respond differently to perturbagens …

Flow cytometry: impact on early drug discovery

BS Edwards, LA Sklar - Journal of biomolecular screening, 2015 - journals.sagepub.com
Modern flow cytometers can make optical measurements of 10 or more parameters per cell
at tens of thousands of cells per second and more than five orders of magnitude dynamic …

A novel high-content analysis tool reveals Rab8-driven cytoskeletal reorganization through Rho GTPases, calpain and MT1-MMP

JJ Bravo-Cordero, M Cordani… - Journal of cell …, 2016 - journals.biologists.com
Rab8 is a small Ras-related GTPase that regulates polarized membrane transport to the
plasma membrane. Here, we developed a high-content analysis (HCA) tool to dissect Rab8 …

Adaptation of robust Z'factor for assay quality assessment in microelectrode array based screening using adult dorsal root ganglion neurons

R Atmaramani, JJ Pancrazio, BJ Black - Journal of Neuroscience Methods, 2020 - Elsevier
Background Cell-based assays comprising primary sensory neurons cultured in vitro are an
emerging tool for the screening and identification of potential analgesic compounds and …

Image analysis for tissue phenomics

J Zimmermann, KE Steele, B Laffin… - … cancer patients for …, 2018 - taylorfrancis.com
This chapter discusses the image analysis component of tissue phenomics studies, together
with the pre-analytical variables that are critical for the successful execution of these studies …