How many drug targets are there?
@article{Overington2006HowMD,
title={How many drug targets are there?},
author={John P. Overington and Bissan Al-Lazikani and Andrew L. Hopkins},
journal={Nature Reviews Drug Discovery},
year={2006},
volume={5},
pages={993-996},
url={https://api.semanticscholar.org/CorpusID:11979420}
}A consensus number of current drug targets for all classes of approved therapeutic drugs is proposed, and an emerging realization of the importance of polypharmacology and also the power of a gene-family-led approach in generating novel and important therapies is highlighted.
3,463 Citations
How to design multi-target drugs
- 2007
Medicine, Chemistry
The authors review the recent progress in this field, compare possible network attack strategies and propose several methods to find target-sets for multi-target drugs.
What is next for small-molecule drug discovery?
- 2009
Chemistry, Medicine
In recent years, several alternative strategies have appeared in the form of the emerging paradigms of polypharmacology, systems biology and personalized medicine, which point to key challenges and breakthroughs likely to affect the future of small-molecule drug discovery.
Trends in the exploitation of novel drug targets
- 2011
Medicine
The drugs that were approved by the US Food and Drug Administration during the past three decades are analysed and the interactions of these drugs with therapeutic targets that are encoded by the human genome are examined, using the DrugBank database and extensive manual curation.
The druggable genome: Evaluation of drug targets in clinical trials suggests major shifts in molecular class and indication.
- 2014
Medicine, Biology
A data set of clinical trial drug-target interactions based on CenterWatch's Drugs in Clinical Trials Database, one of the largest databases of its kind, is developed, identified 475 potentially novel clinical trialDrug targets currently being explored in clinical trials.
Soluble ligands as drug targets
- 2020
Medicine, Chemistry
This Review analyses drugs targeting ligands that have reached clinical development in the past three decades and discusses strategic issues such as the pros and cons of different ligand-targeting therapeutic modalities.
Soluble ligands as drug targets
- 2020
Medicine, Chemistry
This Review analyses drugs targeting ligands that have reached clinical development in the past three decades and discusses strategic issues such as the pros and cons of different ligand-targeting therapeutic modalities.
A comprehensive map of molecular drug targets
- 2017
Medicine, Chemistry
An updated comprehensive map of molecular targets of approved drugs is presented and the relationships between bioactivity class and clinical success, as well as the presence of orthologues between human and animal models and between pathogen and human genomes are explored.
Hypothesis for changing models: current pharmaceutical paradigms, trends and approaches in drug discovery
- 2015
Medicine, Chemistry
It is time to change the role of chemistry in Big Pharma and to re-position it as the central science to progress and to lead to much needed innovation.
28 References
Therapeutic Targets: Progress of Their Exploration and Investigation of Their Characteristics
- 2006
Medicine, Chemistry
The characteristics of the currently explored targets are investigated to analyze their sequence, structure, family representation, pathway association, tissue distribution, and genome location features for finding clues useful for searching for new targets.
The druggable genome
- 2002
Medicine, Biology
An assessment of the number of molecular targets that represent an opportunity for therapeutic intervention is crucial to the development of post-genomic research strategies within the pharmaceutical…
Progress and problems in the exploration of therapeutic targets.
- 2006
Medicine, Chemistry
Drugs, their targets and the nature and number of drug targets
- 2006
Medicine, Chemistry
This work considers the nature of drug targets, and by classifying known drug substances on the basis of the discussed principles it provides an estimation of the total number of current drug targets.
A small molecule–kinase interaction map for clinical kinase inhibitors
- 2005
Medicine, Chemistry
An efficient way to determine kinase inhibitor specificity by measuring binding of small molecules to the ATP site of kinases is described, which represents a systematic small molecule-protein interaction map for clinical compounds across a large number of related proteins.
Can we rationally design promiscuous drugs?
- 2006
Chemistry, Medicine
DrugBank: a comprehensive resource for in silico drug discovery and exploration
- 2006
Computer Science, Medicine
DrugBank is a unique bioinformatics/cheminformatics resource that combines detailed drug data with comprehensive drug target information and is fully searchable supporting extensive text, sequence, chemical structure and relational query searches.
Global mapping of pharmacological space
- 2006
Chemistry, Medicine
This work presents the global mapping of pharmacological space by the integration of several vast sources of medicinal chemistry structure-activity relationships (SAR) data and demonstrates that probabilistic models can be used to predict pharmacology from a large knowledge base.
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
- 2004
Chemistry, Medicine
An unexpected nanomolar affinity is demonstrated of the COX-2 specific arylsulfonamide-type celecoxib and valdecoxib for isoenzymes of the totally unrelated carbonic anhydrase (CA) family, such as CA I, II, IV, and IX, whereas the rofecoxib methyl sulfone-type has no effect.
Kinase Inhibition with BAY 43–9006 in Renal Cell Carcinoma
- 2004
Medicine
The toxic effects of BAY 43–9006 were manageable and included hypertension, edema, diarrhea, hand and foot syndrome, rash, and hair loss where the rash involved the scalp and patients who required a dose reduction could be restored to full dose after a few months.