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Druggable Genome and Proteome

“the most fruitful basis for the discovery of a new drug is to start with an old drug” (James W Black, Nobel de Medicina 1988). Druggable Genome and Proteome. Karen A. Méndez L. Druggability. Thomas H Keller, et al. Current Opinion in Chemical Biology 2006, 10:357–361.

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Druggable Genome and Proteome

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  1. “the most fruitful basis for the discovery of a new drug is to start with an old drug” (James W Black, Nobel de Medicina 1988) DruggableGenome and Proteome Karen A. Méndez L

  2. Druggability Thomas H Keller, et al. Current Opinion in Chemical Biology 2006, 10:357–361

  3. Drug- like compounds Lipinski (2001) --˃ Rule of 5 (RO5) Thomas H Keller, et al. Current Opinion in Chemical Biology 2006, 10:357–361

  4. Rule of 5 • 1. RO5 applies only to compounds that are delivered by the oral route. • 2. RO5 applies only to compounds that are absorbed by passive mechanisms • 3. There are important exceptions (MW and natural compounds). • 4. RO5 compliant compounds are not automatically good drugs

  5. Disease and Druggable Genome Hopkins y Groom (2002) Dixon SJ and Stockwell BR (2009)

  6. Overington et al.Nature Reviews Drug Discovery5, 993–996 (December 2006) | doi:10.1038/nrd2199

  7. Druggable Proteome Pharmaceutically Tractable Genome Door: Protein Lock: Drug Binding Site Key: Drug Yıldırım et al, Drug–target network. NATURE BIOTECHNOLOGY VOLUME 25 NUMBER 10 OCTOBER 2007

  8. Druggable Network Yıldırım et al, Drug–target network. NATURE BIOTECHNOLOGY VOLUME 25 NUMBER 10 OCTOBER 2007

  9. Distribution of Drugs and Drug Targets Yıldırım et al, Drug–target network. NATURE BIOTECHNOLOGY VOLUME 25 NUMBER 10 OCTOBER 2007

  10. Distribution of Drugs and Drug Targets Yıldırım et al, Drug–target network. NATURE BIOTECHNOLOGY VOLUME 25 NUMBER 10 OCTOBER 2007

  11. References • Dixon SJ and Stockwell BR (2009) Identifying druggable disease-modifying gene products, CurrOpinChemBiol 13: 549–555 • Yıldırımet al, Drug–target network. NATURE BIOTECHNOLOGY VOLUME 25 NUMBER 10 OCTOBER 2007 • Overingtonet al.Nature Reviews Drug Discovery5, 993–996 (December 2006) | doi:10.1038/nrd2199 • Thomas H Keller, et al. Current Opinion in Chemical Biology 2006, 10:357–361 • Zheng CJ et al. (2006) Therapeutic Targets: Progress of Their Exploration and Investigation of Their Characteristics, • Pharmacol Rev 58: 259–279 • Russ AP and Lampel S (2005) The druggablegenome:an update, Drug Discov Today 10 (23/24): 1607-1610 • Hopkins AL and Groom CR (2002) The druggable genome, Nat Rev Drug Discov 1: 727-730

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