scholarly journals Open Access Target Validation Is a More Efficient Way to Accelerate Drug Discovery

PLoS Biology ◽  
2015 ◽  
Vol 13 (6) ◽  
pp. e1002164 ◽  
Author(s):  
Wen Hwa Lee
Keyword(s):  
Drug Discovery ◽  
Open Access ◽  
Target Validation

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

2006 ◽  
Vol 11 (15-16) ◽  
pp. 708-716 ◽  
Author(s):  
Ryan T. Strachan ◽  
Gina Ferrara ◽  
Bryan L. Roth
Keyword(s):  
Drug Discovery ◽  
Target Validation ◽  
Efficient Approach

scholarly journals The IUPHAR/BPS Guide to PHARMACOLOGY in 2020: extending immunopharmacology content and introducing the IUPHAR/MMV Guide to MALARIA PHARMACOLOGY

2019 ◽  
Author(s):  
Jane F Armstrong ◽  
Elena Faccenda ◽  
Simon D Harding ◽  
Adam J Pawson ◽  
Christopher Southan ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Open Access ◽  
Molecular Interactions ◽  
Malaria Parasite ◽  
Antimalarial Activity ◽  
Molecular Targets ◽  
Interaction Data ◽  
Data Types ◽  
Global Challenge ◽  
Screening Assays

Abstract The IUPHAR/BPS Guide to PHARMACOLOGY (www.guidetopharmacology.org) is an open-access, expert-curated database of molecular interactions between ligands and their targets. We describe significant updates made over the seven releases during the last two years. The database is notably enhanced through the continued linking of relevant pharmacology with key immunological data types as part of the IUPHAR Guide to IMMUNOPHARMACOLOGY (www.guidetoimmunopharmacology.org) and by a major new extension, the IUPHAR/MMV Guide to Malaria PHARMACOLOGY (www.guidetomalariapharmacology.org). The latter has been constructed in partnership with the Medicines for Malaria Venture, an organization dedicated to identifying, developing and delivering new antimalarial therapies that are both effective and affordable. This is in response to the global challenge of over 200 million cases of malaria and 400 000 deaths worldwide, with the majority in the WHO Africa Region. It provides new pharmacological content, including molecular targets in the malaria parasite, interaction data for ligands with antimalarial activity, and establishes curation of data from screening assays, used routinely in antimalarial drug discovery, against the whole organism. A dedicated portal has been developed to provide quick and focused access to these new data.

Open-access liquid chromatography/mass spectrometry in a drug discovery environment

2002 ◽  
Vol 37 (9) ◽  
pp. 889-896 ◽  
Author(s):  
Larry M. Mallis ◽  
Ani B. Sarkahian ◽  
John M. Kulishoff ◽  
William L. Watts
Keyword(s):  
Mass Spectrometry ◽  
Liquid Chromatography ◽  
Drug Discovery ◽  
Open Access ◽  
Liquid Chromatography Mass Spectrometry ◽  
Chromatography Mass Spectrometry

scholarly journals Open Access Could Transform Drug Discovery: A Case Study of JQ1

2016 ◽  
Vol 11 (3) ◽  
pp. 321-332 ◽  
Author(s):  
Zeeshaan Arshad ◽  
James Smith ◽  
Mackenna Roberts ◽  
Wen Hwa Lee ◽  
Ben Davies ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Open Access

scholarly journals Encoded Library Technologies as Integrated Lead Finding Platforms for Drug Discovery

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1629 ◽  
Author(s):  
Johannes Ottl ◽  
Lukas Leder ◽  
Jonas V. Schaefer ◽  
Christoph E. Dumelin
Keyword(s):  
Drug Discovery ◽  
Cyclic Peptides ◽  
Chemical Space ◽  
Pharmaceutical Research ◽  
Peptide Libraries ◽  
Assay Development ◽  
Low Molecular Weight ◽  
Target Validation ◽  
Lead Finding ◽  
Chemical Matter

The scope of targets investigated in pharmaceutical research is continuously moving into uncharted territory. Consequently, finding suitable chemical matter with current compound collections is proving increasingly difficult. Encoded library technologies enable the rapid exploration of large chemical space for the identification of ligands for such targets. These binders facilitate drug discovery projects both as tools for target validation, structural elucidation and assay development as well as starting points for medicinal chemistry. Novartis internalized two complementing encoded library platforms to accelerate the initiation of its drug discovery programs. For the identification of low-molecular weight ligands, we apply DNA-encoded libraries. In addition, encoded peptide libraries are employed to identify cyclic peptides. This review discusses how we apply these two platforms in our research and why we consider it beneficial to run both pipelines in-house.

Kinase Chemogenomics: Targeting the Human Kinome for Target Validation and Drug Discovery

2004 ◽  
Vol 4 (3) ◽  
pp. 235-253 ◽  
Author(s):  
E. Haar ◽  
W. Walters ◽  
S. Pazhanisamy ◽  
P. Taslimi ◽  
A. Pierce ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Target Validation ◽  
Human Kinome

High-Throughput siRNA-Based Functional Target Validation

2004 ◽  
Vol 9 (4) ◽  
pp. 286-293 ◽  
Author(s):  
Hong Xin ◽  
Alejandro Bernal ◽  
Frank A. Amato ◽  
Albert Pinhasov ◽  
Jack Kauffman ◽  
...  
Keyword(s):  
Drug Discovery ◽  
High Throughput ◽  
High Throughput Screening ◽  
Target Genes ◽  
Discovery Process ◽  
Target Validation ◽  
Drug Discovery Process ◽  
Functional Identification ◽  
Screening Process ◽  
Lead Compounds

The drug discovery process pursued by major pharmaceutical companies for many years starts with target identification followed by high-throughput screening (HTS) with the goal of identifying lead compounds. To accomplish this goal, significant resources are invested into automation of the screening process or HTS. Robotic systems capable of handling thousands of data points per day are implemented across the pharmaceutical sector. Many of these systems are amenable to handling cell-based screening protocols as well. On the other hand, as companies strive to develop innovative products based on novel mechanisms of action(s), one of the current bottlenecks of the industry is the target validation process. Traditionally, bioinformatics and HTS groups operate separately at different stages of the drug discovery process. The authors describe the convergence and integration of HTS and bioinformatics to perform high-throughput target functional identification and validation. As an example of this approach, they initiated a project with a functional cell-based screen for a biological process of interest using libraries of small interfering RNA (siRNA) molecules. In this protocol, siRNAs function as potent gene-specific inhibitors. siRNA-mediated knockdown of the target genes is confirmed by TaqMan analysis, and genes with impacts on biological functions of interest are selected for further analysis. Once the genes are confirmed and further validated, they may be used for HTS to yield lead compounds.

scholarly journals Screening the Medicines for Malaria Venture Pathogen Box across Multiple Pathogens Reclassifies Starting Points for Open-Source Drug Discovery

2017 ◽  
Vol 61 (9) ◽  
Author(s):  
Sandra Duffy ◽  
Melissa L. Sykes ◽  
Amy J. Jones ◽  
Todd B. Shelper ◽  
Moana Simpson ◽  
...  
Keyword(s):  
Biological Activity ◽  
Drug Discovery ◽  
Open Access ◽  
Open Source ◽  
Target Identification ◽  
Source Model ◽  
Biological Evaluation ◽  
Neglected Diseases ◽  
Extensive Literature

ABSTRACT Open-access drug discovery provides a substantial resource for diseases primarily affecting the poor and disadvantaged. The open-access Pathogen Box collection is comprised of compounds with demonstrated biological activity against specific pathogenic organisms. The supply of this resource by the Medicines for Malaria Venture has the potential to provide new chemical starting points for a number of tropical and neglected diseases, through repurposing of these compounds for use in drug discovery campaigns for these additional pathogens. We tested the Pathogen Box against kinetoplastid parasites and malaria life cycle stages in vitro. Consequently, chemical starting points for malaria, human African trypanosomiasis, Chagas disease, and leishmaniasis drug discovery efforts have been identified. Inclusive of this in vitro biological evaluation, outcomes from extensive literature reviews and database searches are provided. This information encompasses commercial availability, literature reference citations, other aliases and ChEMBL number with associated biological activity, where available. The release of this new data for the Pathogen Box collection into the public domain will aid the open-source model of drug discovery. Importantly, this will provide novel chemical starting points for drug discovery and target identification in tropical disease research.

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