What is druggable genome?

Approximately 3,000 genes are considered part of the “druggable genome,” a set of genes encoding proteins that scientists can or predict they can modulate using experimental small molecule compounds. Therefore, a large number of proteins remain for scientists to explore as potential therapeutic targets.

How much of the human genome is druggable?

We identified a total of 3,052 genes in the druggable set that were not represented in any of the LD intervals corresponding to a GWAS association; 62.7%, 69.2%, and 71.6% of Tier 1, 2, and 3 genes, respectively….Count of GWAS published per disease area.

What is a druggable target?

Druggability is a term used in drug discovery to describe a biological target (such as a protein) that is known to or is predicted to bind with high affinity to a drug. Disease relevance alone however is insufficient for a protein to become a drug target. In addition, the target must be druggable.

What do you understand by Druggability of a gene?

Definitions of ‘druggability’ vary: ‘the ability of a protein target to bind small molecules with high affinity’ – sometimes (perhaps more appropriately) called ‘ligandability’ ‘the likelihood of finding orally bioavailable small molecules that bind to a. particular target in a disease-modifying way’

What is a drug like molecule?

Based on one definition, a drug-like molecule has a logarithm of partition coefficient (log P) between -0.4 and 5.6, molecular weight 160-480 g/mol, molar refractivity of 40-130, which is related to the volume and molecular weight of the molecule and has 20-70 atoms. However, several poisons have a good druglikeness.

Can a drug target a gene?

Drug-target interactions are defined as any type of interaction between a drug and a protein target. Drug-gene interactions are changes in gene expression induced by a drug.

How many druggable targets are there?

Drug targets and druggable targets Currently, marketed drugs mediate their effects through a relatively small number of potential human target proteins. Published estimates of the number of current human drug targets range from 200 to 500. Drews2 estimate 483 target proteins in humans and pathogens.

What makes a good drug?

Key aspects to be considered are a high unmet medical need (no drug is available or existing therapies have serious limitations with regard to efficacy or safety or both) and there is a reasonable market size. The full therapeutic potential of many drug targets is often not obvious at the time of their discovery.

How many Druggable targets are there?

Potential drug targets Currently, there are 4009 genes in the UniProt database having experimental evidence for being involved in various disease conditions, including cancer, neurologic, systemic and cardiovascular disease.

What is boiled egg in Swissadme?

For details about development and validation of the BOILED-Egg, please refer to this article: A BOILED-Egg to predict gastrointestinal absorption and brain penetration of small molecules. Developed and maintained by the Molecular Modeling Group of the SIB | Swiss Institute of Bioinformatics.

What does high logP mean?

A negative value for logP means the compound has a higher affinity for the aqueous phase (it is more hydrophilic); when logP = 0 the compound is equally partitioned between the lipid and aqueous phases; a positive value for logP denotes a higher concentration in the lipid phase (i.e., the compound is more lipophilic).

How many genes are part of the Druggable Genome?

Abnormal protein expression is associated with many human diseases, which makes proteins key targets for therapeutic agents. Approximately 3,000 genes are considered part of the “druggable genome,” a set of genes encoding proteins that scientists can or predict they can modulate using experimental small molecule compounds.

Why is the IDG important to the Druggable Genome?

Illuminating the Druggable Genome (IDG) A gene contains (encodes) the information that each cell uses to make (express) a protein, which is essential for the body to function properly. Abnormal protein expression is associated with many human diseases, which makes proteins key targets for therapeutic agents.

How is druggability used to describe drug discovery?

Druggability. Druggability is a term used in drug discovery to describe a biological target (such as a protein) that is known to or is predicted to bind with high affinity to a drug. Furthermore, by definition, the binding of the drug to a druggable target must alter the function of the target with a therapeutic benefit to the patient.

When did NIH start illuminating the Druggable Genome?

To improve scientific understanding of the three understudied protein families, NIH launched an effort called Illuminating the Druggable Genome (IDG) in 2013, with the first awards made in 2014.