Opportunities and challenges in phenotypic drug discovery: an industry perspective

A disease model of diabetic nephropathy in a glomerulus-on-a-chip microdevice

(2017) Li Wang et al.   LAB ON A CHIP

Accelerating glioblastoma drug discovery: Convergence of patient-derived models, genome editing and phenotypic screening

(2017) Eoghan O'Duibhir et al.   MOLECULAR AND CELLULAR NEUROSCIENCE

Applications of chemogenomic library screening in drug discovery

(2017) Lyn H. Jones et al.   NATURE REVIEWS DRUG DISCOVERY

In vitro cardiotoxicity assessment of environmental chemicals using an organotypic human induced pluripotent stem cell-derived model

(2017) Oksana Sirenko et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Target identification for biologically active small molecules using chemical biology approaches

(2016) Heesu Lee et al.   ARCHIVES OF PHARMACAL RESEARCH

Transcriptional Characterization of Compounds: Lessons Learned from the Public LINCS Data

(2016) Hans De Wolf et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

The OncoArray Consortium: A Network for Understanding the Genetic Architecture of Common Cancers

(2016) Christopher I. Amos et al.   CANCER EPIDEMIOLOGY BIOMARKERS & PREVENTION

Defining Glomerular Disease in Mechanistic Terms: Implementing an Integrative Biology Approach in Nephrology

(2016) L. H. Mariani et al.   Clinical Journal of the American Society of Nephrology

Challenges and Hurdles to Business as Usual in Drug Development for Treatment of Rare Diseases

(2016) DC Swinney   CLINICAL PHARMACOLOGY & THERAPEUTICS

Polypharmacology in Drug Discovery: A Review from Systems Pharmacology Perspective

(2016) Wenjuan Zhang et al.   CURRENT PHARMACEUTICAL DESIGN

JAK inhibition in the treatment of diabetic kidney disease

(2016) Frank C. Brosius et al.   DIABETOLOGIA

Phenotypic screening: the future of antibody discovery

(2016) Andrea L. Gonzalez-Munoz et al.   DRUG DISCOVERY TODAY

Identifying compound efficacy targets in phenotypic drug discovery

(2016) Markus Schirle et al.   DRUG DISCOVERY TODAY

Identification of protein binding partners of small molecules using label-free methods

(2016) Chaitanya Saxena   Expert Opinion on Drug Discovery

Advances and challenges in hereditary cancer pharmacogenetics

(2016) Ingolf Cascorbi et al.   Expert Opinion on Drug Metabolism & Toxicology

Natural Products as Sources of New Drugs from 1981 to 2014

(2016) David J. Newman et al.   JOURNAL OF NATURAL PRODUCTS

Multiparametric Analysis of Oncology Drug Screening with Aqueous Two-Phase Tumor Spheroids

(2016) Pradip Shahi Thakuri et al.   MOLECULAR PHARMACEUTICS

Target identification by image analysis

(2016) V. Fetz et al.   NATURAL PRODUCT REPORTS

Proteome-wide covalent ligand discovery in native biological systems

(2016) Keriann M. Backus et al.   NATURE

Diversity-oriented synthesis yields novel multistage antimalarial inhibitors

(2016) Nobutaka Kato et al.   NATURE

Chemoproteomic profiling and discovery of protein electrophiles in human cells

(2016) Megan L. Matthews et al.   Nature Chemistry

Withaferin A is a leptin sensitizer with strong antidiabetic properties in mice

(2016) Jaemin Lee et al.   NATURE MEDICINE

Screening out irrelevant cell-based models of disease

(2016) Peter Horvath et al.   NATURE REVIEWS DRUG DISCOVERY

Cornerstones of CRISPR–Cas in drug discovery and therapy

(2016) Christof Fellmann et al.   NATURE REVIEWS DRUG DISCOVERY

Induced pluripotent stem cell technology: a decade of progress

(2016) Yanhong Shi et al.   NATURE REVIEWS DRUG DISCOVERY

A comprehensive map of molecular drug targets

(2016) Rita Santos et al.   NATURE REVIEWS DRUG DISCOVERY

Pluripotent stem cells in disease modelling and drug discovery

(2016) Yishai Avior et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Three-dimensional culture systems in cancer research: Focus on tumor spheroid model

(2016) Sritama Nath et al.   PHARMACOLOGY & THERAPEUTICS

Phenotypic Assessment and the Discovery of Topiramate

(2016) Bruce E. Maryanoff   ACS Medicinal Chemistry Letters

Targeting mutant RAS in patient-derived colorectal cancer organoids by combinatorial drug screening

(2016) Carla S Verissimo et al.   eLife

Microtissues in Cardiovascular Medicine: Regenerative Potential Based on a 3D Microenvironment

(2016) Julia Günter et al.   Stem Cells International

When Quality Beats Quantity: Decision Theory, Drug Discovery, and the Reproducibility Crisis

(2016) Jack W. Scannell et al.   PLoS One

Pathway reporter genes define molecular phenotypes of human cells

(2015) Jitao David Zhang et al.   BMC GENOMICS

Treatment of Obesity with Celastrol

(2015) Junli Liu et al.   CELL

Prospective Derivation of a Living Organoid Biobank of Colorectal Cancer Patients

(2015) Marc van de Wetering et al.   CELL

The impact of CRISPR–Cas9 on target identification and validation

(2015) Jonathan D. Moore   DRUG DISCOVERY TODAY

Losartan ameliorates dystrophic epidermolysis bullosa and uncovers new disease mechanisms

(2015) A. Nystrom et al.   EMBO Molecular Medicine

Related articles

(2015)   Expert Opinion on Drug Metabolism & Toxicology

Nintedanib: From Discovery to the Clinic

(2015) Gerald J. Roth et al.   JOURNAL OF MEDICINAL CHEMISTRY

Compound signature detection on LINCS L1000 big data

(2015) Chenglin Liu et al.   Molecular BioSystems

Tumor-Derived Cell Lines as Molecular Models of Cancer Pharmacogenomics

(2015) A. Goodspeed et al.   MOLECULAR CANCER RESEARCH

The DNA of a nation

(2015) Vivien Marx   NATURE

Functional genomics to uncover drug mechanism of action

(2015) Sebastian M B Nijman   Nature Chemical Biology

Dark chemical matter as a promising starting point for drug lead discovery

(2015) Anne Mai Wassermann et al.   Nature Chemical Biology

SMN2 splice modulators enhance U1–pre-mRNA association and rescue SMA mice

(2015) James Palacino et al.   Nature Chemical Biology

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

The phenotypic screening pendulum swings

(2015) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Preclinical target validation using patient-derived cells

(2015) Aled M. Edwards et al.   NATURE REVIEWS DRUG DISCOVERY

The re-emergence of natural products for drug discovery in the genomics era

(2015) Alan L. Harvey et al.   NATURE REVIEWS DRUG DISCOVERY

Organs-on-chips at the frontiers of drug discovery

(2015) Eric W. Esch et al.   NATURE REVIEWS DRUG DISCOVERY

Developing predictive assays: The phenotypic screening “rule of 3”

(2015) Fabien Vincent et al.   Science Translational Medicine

Tissue transcriptome-driven identification of epidermal growth factor as a chronic kidney disease biomarker

(2015) Wenjun Ju et al.   Science Translational Medicine

High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma

(2015) Christine E. Quartararo et al.   ACS Medicinal Chemistry Letters

Target (In)Validation: A Critical, Sometimes Unheralded, Role of Modern Medicinal Chemistry

(2015) Ramzi F. Sweis   ACS Medicinal Chemistry Letters

Spherical Cancer Models in Tumor Biology

(2015) Louis-Bastien Weiswald et al.   NEOPLASIA

Highly sensitive amplicon-based transcript quantification by semiconductor sequencing

(2014) Jitao Zhang et al.   BMC GENOMICS

The discovery of medicines for rare diseases

(2014) David C Swinney et al.   Future Medicinal Chemistry

Clinical development success rates for investigational drugs

(2014) Michael Hay et al.   NATURE BIOTECHNOLOGY

A comprehensive transcriptional portrait of human cancer cell lines

(2014) Christiaan Klijn et al.   NATURE BIOTECHNOLOGY

White-to-brown metabolic conversion of human adipocytes by JAK inhibition

(2014) Annie Moisan et al.   NATURE CELL BIOLOGY

The discovery of first-in-class drugs: origins and evolution

(2014) Jörg Eder et al.   NATURE REVIEWS DRUG DISCOVERY

Phenotypic screening in cancer drug discovery — past, present and future

(2014) John G. Moffat et al.   NATURE REVIEWS DRUG DISCOVERY

The South Asian Genome

(2014) John C. Chambers et al.   PLoS One

Toward performance-diverse small-molecule libraries for cell-based phenotypic screening using multiplexed high-dimensional profiling

(2014) M. J. Wawer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

SMN2 splicing modifiers improve motor function and longevity in mice with spinal muscular atrophy

(2014) N. A. Naryshkin et al.   SCIENCE

iPS cell derived neuronal cells for drug discovery

(2014) Ralf Heilker et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

The value of translational biomarkers to phenotypic assays

(2014) David C. Swinney   Frontiers in Pharmacology

Comparative genomics as a tool to understand evolution and disease

(2013) J. Alfoldi et al.   GENOME RESEARCH

Data mining reveals a network of early-response genes as a consensus signature of drug-induced in vitro and in vivo toxicity

(2013) J D Zhang et al.   PHARMACOGENOMICS JOURNAL

Bacterial cytological profiling rapidly identifies the cellular pathways targeted by antibacterial molecules

(2013) P. Nonejuie et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974

(2013) J. Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Power of Rare Diseases: Found in Translation

(2013) M. C. Fishman   Science Translational Medicine

Ivacaftor potentiation of multiple CFTR channels with gating mutations

(2012) Haihui Yu et al.   Journal of Cystic Fibrosis

Raise standards for preclinical cancer research

(2012) C. Glenn Begley et al.   NATURE

Large-scale screening using familial dysautonomia induced pluripotent stem cells identifies compounds that rescue IKBKAP expression

(2012) Gabsang Lee et al.   NATURE BIOTECHNOLOGY

Biology-Oriented Synthesis

(2011) Stefan Wetzel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival

(2011) Paul Morgan et al.   DRUG DISCOVERY TODAY

How were new medicines discovered?

(2011) David C. Swinney et al.   NATURE REVIEWS DRUG DISCOVERY

Believe it or not: how much can we rely on published data on potential drug targets?

(2011) Florian Prinz et al.   NATURE REVIEWS DRUG DISCOVERY

High-Content Phenotypic Profiling of Drug Response Signatures across Distinct Cancer Cells

(2010) P. D. Caie et al.   MOLECULAR CANCER THERAPEUTICS

Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect

(2010) Min Gao et al.   NATURE

Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis

(2010) Volker Brinkmann et al.   NATURE REVIEWS DRUG DISCOVERY

Spiroindolones, a Potent Compound Class for the Treatment of Malaria

(2010) M. Rottmann et al.   SCIENCE

Can Animal Models of Disease Reliably Inform Human Studies?

(2010) H. Bart van der Worp et al.   PLOS MEDICINE

Modern Approaches in the Search for New Lead Antiparasitic Compounds from Higher Plants

(2009) Emerson Queiroz et al.   CURRENT DRUG TARGETS

Spheroid-based drug screen: considerations and practical approach

(2009) Juergen Friedrich et al.   Nature Protocols

Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770

(2009) F. Van Goor et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Brivaracetam: a rational drug discovery success story

(2008) M A Rogawski   BRITISH JOURNAL OF PHARMACOLOGY

Characterization of Chemical Libraries for Luciferase Inhibitory Activity

(2008) Douglas S. Auld et al.   JOURNAL OF MEDICINAL CHEMISTRY

Genomics takes hold in Asia

(2008) David Cyranoski   NATURE

SV2A protein is a broad-spectrum anticonvulsant target: Functional correlation between protein binding and seizure protection in models of both partial and generalized epilepsy

(2007) Rafal M. Kaminski et al.   NEUROPHARMACOLOGY