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| Drug Target Identification |
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o25K-40K different genes in the human genome
with splicing & post-translational modification the number of functional proteins is likely greater
oEstimated that up to 10 genes contribute to a multifactorial disease
Typically these are linked to 5-10 gene products in physiological circuits which are targetable
o~5000-10000 potential drug targets! |
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o1179 FDA-approved small molecule & biotech drugs (different chemical entities)
o890 / 1179 has human protein targets
o390 Human Drug Target Proteins for Approved Drugs. |
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| are synthetically locked, or 'stapled', into an alpha-helical shape with an optimized cross-linking chemistry to mimic the structure found at the interface of many protein-protein interactions. |
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Protein therapeutics with enzymatic or regulatory activity
Group 1a: Replace a protein which is deficient or abnormal
Group 1b: Augment an existing pathway
Group 1c: Provide a novel function or activity |
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Protein therapeutics with special targeting activity
Group 2a: Interfering with a molecule or organism by binding to it and blocking its function or targeting it for degradation
Group 2b: Stimulating a signalling pathway
Group 2c: Delivering other compounds or proteins |
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Protein vaccines
Group 3a: Protecting against a deleterious foreign agent
Group 3b: Treating an autoimmune disease
Group 3c: Treating cancer |
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