4.8 Review

Mitigating risk in academic preclinical drug discovery

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Letter Education, Scientific Disciplines

The Innovation Forager: Stimulating Academic Innovation

Thomas Ungar et al.

ACADEMIC MEDICINE (2014)

Article Biochemistry & Molecular Biology

Genome Editing-Enabled HIS Assays Expand Drug Target Pathways for Charcot-Marie-Tooth Disease

James Inglese et al.

ACS CHEMICAL BIOLOGY (2014)

Article Biochemistry & Molecular Biology

Phytochemicals Perturb Membranes and Promiscuously Alter Protein Function

Helgi I. Ingolfsson et al.

ACS CHEMICAL BIOLOGY (2014)

Article Chemistry, Multidisciplinary

Pharmacophore Reassignment for Induction of the Immunosurveillance Cytokine TRAIL

Nicholas T. Jacob et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2014)

Article Chemistry, Medicinal

A biochemical screen for GroEL/GroES inhibitors

Steven M. Johnson et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2014)

Article Biochemical Research Methods

From HTS to Phase I: The Institute for Therapeutics Discovery and Development at the University of Minnesota

Peter I. Dosa et al.

COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING (2014)

Review Chemistry, Medicinal

A Unique Industrial - Academic Collaboration Towards the Next Generation of Schizophrenia Therapeutics

Gregor J. Macdonald et al.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2014)

Editorial Material Chemistry, Medicinal

To screen or not to screen: an impassioned plea for smarter chemical libraries to improve drug lead finding

Gerry Lushington et al.

FUTURE MEDICINAL CHEMISTRY (2014)

Article Chemistry, Medicinal

The essential roles of chemistry in high-throughput screening triage

Jayme L. Dahlin et al.

FUTURE MEDICINAL CHEMISTRY (2014)

Article Chemistry, Medicinal

Undecaprenyl Diphosphate Synthase Inhibitors: Antibacterial Drug Leads

William Sinko et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Article Oncology

A Novel Small-Molecule Inhibitor of Mcl-1 Blocks Pancreatic Cancer Growth In Vitro and In Vivo

Fardokht Abulwerdi et al.

MOLECULAR CANCER THERAPEUTICS (2014)

Editorial Material Multidisciplinary Sciences

Chemical con artists foil drug discovery

Jonathan Baell et al.

NATURE (2014)

Article Biochemical Research Methods

The cellular thermal shift assay for evaluating drug target interactions in cells

Rozbeh Jafari et al.

NATURE PROTOCOLS (2014)

Letter Biotechnology & Applied Microbiology

Can you trust your animal study data?

Ian S. Peers et al.

NATURE REVIEWS DRUG DISCOVERY (2014)

Article Multidisciplinary Sciences

Rescuing US biomedical research from its systemic flaws

Bruce Alberts et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2014)

Article Medicine, Research & Experimental

Systems biology-embedded target validation: improving efficacy in drug discovery

Drieke Vandamme et al.

WILEY INTERDISCIPLINARY REVIEWS-SYSTEMS BIOLOGY AND MEDICINE (2014)

Review Biochemistry & Molecular Biology

Putative Impact of RNA Editing on Drug Discovery

Niels Decher et al.

CHEMICAL BIOLOGY & DRUG DESIGN (2013)

Article Oncology

A Proposal Regarding Reporting of In Vitro Testing Results

Malcolm A. Smith et al.

CLINICAL CANCER RESEARCH (2013)

Editorial Material Pharmacology & Pharmacy

Phenotypic vs. Target-Based Drug Discovery for First-in-Class Medicines

D. C. Swinney

CLINICAL PHARMACOLOGY & THERAPEUTICS (2013)

Review Biochemistry & Molecular Biology

Innovation in academic chemical screening: filling the gaps in chemical biology

Samuel A. Hasson et al.

CURRENT OPINION IN CHEMICAL BIOLOGY (2013)

Review Pharmacology & Pharmacy

NIPTE: a multi-university partnership supporting academic drug development

Vadim J. Gurvich et al.

DRUG DISCOVERY TODAY (2013)

Article Chemistry, Medicinal

Broad Coverage of Commercially Available Lead-like Screening Space with Fewer than 350,000 Compounds

Jonathan B. Baell

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2013)

Article Chemistry, Medicinal

Development of Highly Potent and Selective Diaminothiazole Inhibitors of Cyclin-Dependent Kinases

Ernst Schonbrunn et al.

JOURNAL OF MEDICINAL CHEMISTRY (2013)

Article Biochemistry & Molecular Biology

Structure-guided design of a selective BCL-XL inhibitor

Guillaume Lessene et al.

NATURE CHEMICAL BIOLOGY (2013)

Article Biochemistry & Molecular Biology

Target validation using chemical probes

Mark E. Bunnage et al.

NATURE CHEMICAL BIOLOGY (2013)

Editorial Material Biotechnology & Applied Microbiology

The epigenetics pipeline

Vivian A. DeWoskin et al.

NATURE REVIEWS DRUG DISCOVERY (2013)

Review Biotechnology & Applied Microbiology

Validating therapeutic targets through human genetics

Robert M. Plenge et al.

NATURE REVIEWS DRUG DISCOVERY (2013)

Editorial Material Multidisciplinary Sciences

The Basics of Translation

Huda Y. Zoghbi

SCIENCE (2013)

Article Multidisciplinary Sciences

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

Daniel Martinez Molina et al.

SCIENCE (2013)

Editorial Material Biochemistry & Molecular Biology

How academic labs can approach the drug discovery process as a way to synergize with big pharma

Arianna Loregian et al.

TRENDS IN MICROBIOLOGY (2013)

Article Chemistry, Medicinal

Metal Impurities Cause False Positives in High-Throughput Screening Campaigns

Johannes C. Hermann et al.

ACS MEDICINAL CHEMISTRY LETTERS (2013)

Editorial Material Chemistry, Medicinal

Drug Discovery in an Academic Setting: Playing to the Strengths

Donna M. Huryn

ACS MEDICINAL CHEMISTRY LETTERS (2013)

Article Chemistry, Multidisciplinary

Challenges for Academic Drug Discovery

William L. Jorgensen

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2012)

Review Biochemistry & Molecular Biology

Structural Biology and Drug Discovery of Difficult Targets: The Limits of Ligandability

Sachin Surade et al.

CHEMISTRY & BIOLOGY (2012)

Review Pharmacology & Pharmacy

Can we discover pharmacological promiscuity early in the drug discovery process?

Jens-Uwe Peters et al.

DRUG DISCOVERY TODAY (2012)

Review Pharmacology & Pharmacy

Drug discovery in pharmaceutical industry: productivity challenges and trends

Ish Khanna

DRUG DISCOVERY TODAY (2012)

Review Pharmacology & Pharmacy

Relevance of systems pharmacology in drug discovery

Lourdes Cucurull-Sanchez et al.

DRUG DISCOVERY TODAY (2012)

Review Pharmacology & Pharmacy

What makes a good drug target?

Isabella Gashaw et al.

DRUG DISCOVERY TODAY (2012)

Article Chemistry, Medicinal

Development of a Rule-Based Method for the Assessment of Protein Druggability

Emanuele Perola et al.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2012)

Article Chemistry, Medicinal

Discovery and Synthesis of Hydronaphthoquinones as Novel Proteasome Inhibitors

Yiyu Ge et al.

JOURNAL OF MEDICINAL CHEMISTRY (2012)

Article Chemistry, Medicinal

Rules for Identifying Potentially Reactive or Promiscuous Compounds

Robert F. Bruns et al.

JOURNAL OF MEDICINAL CHEMISTRY (2012)

Article Chemistry, Medicinal

Identification of a Novel Family of BRAFV600E Inhibitors

Jie Qjn et al.

JOURNAL OF MEDICINAL CHEMISTRY (2012)

Article Cell Biology

A Preclinical Evaluation of Minnelide as a Therapeutic Agent Against Pancreatic Cancer

Rohit Chugh et al.

SCIENCE TRANSLATIONAL MEDICINE (2012)

Review Medicine, Research & Experimental

Therapeutics Development for Cystic Fibrosis: A Successful Model for a Multisystem Genetic Disease

Melissa A. Ashlock et al.

ANNUAL REVIEW OF MEDICINE, VOL 62, 2011 (2011)

Article Chemistry, Medicinal

Target Validation: Linking Target and Chemical Properties to Desired Product Profile

Paul G. Wyatt et al.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2011)

Article Chemistry, Medicinal

Druggability assessment of protein-protein interfaces

Jutta Wanner et al.

FUTURE MEDICINAL CHEMISTRY (2011)

Article Chemistry, Medicinal

Discovery and Characterizatlion of Small Molecule Inhibitors of the BET Family Bromodomains

Chun-wa Chung et al.

JOURNAL OF MEDICINAL CHEMISTRY (2011)

Editorial Material Biotechnology & Applied Microbiology

US academic drug discovery

Stephen Frye et al.

NATURE REVIEWS DRUG DISCOVERY (2011)

Article Biotechnology & Applied Microbiology

Trends in the exploitation of novel drug targets

Mathias Rask-Andersen et al.

NATURE REVIEWS DRUG DISCOVERY (2011)

Letter Biotechnology & Applied Microbiology

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

Florian Prinz et al.

NATURE REVIEWS DRUG DISCOVERY (2011)

Article Multidisciplinary Sciences

Structural conservation of druggable hot spots in protein-protein interfaces

Dima Kozakov et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2011)

Article Multidisciplinary Sciences

Organic synthesis toward small-molecule probes and drugs

Stuart L. Schreiber

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2011)

Article Cell Biology

How to Revive Breakthrough Innovation in the Pharmaceutical Industry

Bernard H. Munos et al.

SCIENCE TRANSLATIONAL MEDICINE (2011)

Editorial Material Biochemistry & Molecular Biology

Probing the Probes: Fitness Factors For Small Molecule Tools

Paul Workman et al.

CHEMISTRY & BIOLOGY (2010)

Review Biochemistry & Molecular Biology

Apparent activity in high-throughput screening: origins of compound-dependent assay interference

Natasha Thorne et al.

CURRENT OPINION IN CHEMICAL BIOLOGY (2010)

Article Pharmacology & Pharmacy

The translatability of animal models for clinical development: biomarkers and disease models

Alexandra Wendler et al.

CURRENT OPINION IN PHARMACOLOGY (2010)

Article Chemistry, Medicinal

Towards a more robust approach to selecting and prosecuting promising targets and compounds

Graeme Robertson

FUTURE MEDICINAL CHEMISTRY (2010)

Article Chemistry, Medicinal

Observations on screening-based research and some concerning trends in the literature

Jonathan B. Baell

FUTURE MEDICINAL CHEMISTRY (2010)

Article Multidisciplinary Sciences

N-myristoyltransferase inhibitors as new leads to treat sleeping sickness

Julie A. Frearson et al.

NATURE (2010)

Article Multidisciplinary Sciences

Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124

Douglas S. Auld et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2010)

Article Cell Biology

Driving Drug Discovery: The Fundamental Role of Academic Labs

B. Michael Silber

SCIENCE TRANSLATIONAL MEDICINE (2010)

Article Biochemistry & Molecular Biology

Quantifying Biological Activity in Chemical Terms: A Pharmacology Primer To Describe Drug Effect

Terry Kenakin

ACS CHEMICAL BIOLOGY (2009)

Article Biochemical Research Methods

A survey of across-target bioactivity results of small molecules in PubChem

Lianyi Han et al.

BIOINFORMATICS (2009)

Review Pharmacology & Pharmacy

Predicting druggable binding sites at the protein-protein interface

Jonathan C. Fuller et al.

DRUG DISCOVERY TODAY (2009)

Article Chemistry, Medicinal

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

Frank Lovering et al.

JOURNAL OF MEDICINAL CHEMISTRY (2009)

Article Multidisciplinary Sciences

Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4

Costas A. Lyssiotis et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2009)

Article Biochemical Research Methods

Best Practices in Compound Management for Preserving Compound Integrity and Accurately Providing Samples for Assays

Sandra L. Matson et al.

JOURNAL OF BIOMOLECULAR SCREENING (2009)

Review Pharmacology & Pharmacy

A structural biology view of target drugability

Ursula Egner et al.

EXPERT OPINION ON DRUG DISCOVERY (2008)

Review Biochemistry & Molecular Biology

High-throughput screening assays for the identification of chemical probes

James Inglese et al.

NATURE CHEMICAL BIOLOGY (2007)

Article Multidisciplinary Sciences

PTC124 targets genetic disorders caused by nonsense mutations

Ellen M. Welch et al.

NATURE (2007)

Article Medicine, Research & Experimental

Drug discovery in jeopardy

Pedro Cuatrecasas

JOURNAL OF CLINICAL INVESTIGATION (2006)

Review Pharmacology & Pharmacy

Screening the receptorome: an efficient approach for drug discovery and target validation

Ryan T. Strachan et al.

DRUG DISCOVERY TODAY (2006)

Article Multidisciplinary Sciences

Quantitative high-throughput screening: A titration-based approach that efficiently identifies biological activities in large chemical libraries

James Inglese et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2006)

Article Biochemical Research Methods

A detergent-based assay for the detection of promiscuous inhibitors

Brian Y. Feng et al.

NATURE PROTOCOLS (2006)

Review Biochemistry & Molecular Biology

Obtaining and screening compound collections: a user's guide and a call to chemists

PJ Hergenrother

CURRENT OPINION IN CHEMICAL BIOLOGY (2006)

Article Multidisciplinary Sciences

Towards a proteome-scale map of the human protein-protein interaction network

JF Rual et al.

NATURE (2005)

Review Pharmacology & Pharmacy

Target-based drug discovery: is something wrong?

F Sams-Dodd

DRUG DISCOVERY TODAY (2005)

Article Chemistry, Multidisciplinary

ALARM NMR: A rapid and robust experimental method to detect reactive false positives in biochemical screens

JR Huth et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2005)

Article Chemistry, Medicinal

Risk reduction in drug discovery and development

M Mackay et al.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2005)

Review Biotechnology & Applied Microbiology

Designing screens: How to make your hits a hit

WP Walters et al.

NATURE REVIEWS DRUG DISCOVERY (2003)

Article Biotechnology & Applied Microbiology

Virtual drug discovery and development for neglected diseases through public-private partnerships

S Nwaka et al.

NATURE REVIEWS DRUG DISCOVERY (2003)