Drug Targets: Proteins

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Drug Targets Proteins

• Chapter 2

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Amino acids
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Protein structure

• Primary

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Protein structure

• Secondary

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Protein structure

• Tertiary

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Protein structure

• Quaternary

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Protein as drug targets

• Not very common
• Fuzeon (enfuvurtide) anti-HIV drug - polypeptide
  of 36 units injected subcutaneously
• Zoladex (goserelin) prostate and breast cancer
  treatment (made 700 million last year)

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Post-translational Modifications

• Modifications of proteins after translation have
  a wide range of effects.
• Scurvy
• Excessive bleeding
• Cell to cell recognition, disease processes, drug
  treatments
• Enzyme regulation through protein cleavage

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Proteomics

• Genomics- process to identify the genetic code
• Proteomics process to identify all proteins in
  each cell of the body and how they interact with
  each other
• More complex than genomics because of the many
  interactions between proteins.

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Drug action at proteins

• Structural Proteins
• Typically not drug targets (exception tublin)
• Transport Proteins
• Several important drugs target transport proteins
• Enzymes Receptors
• Most important drug targets
• Many cell processes depend on the interactions of
  proteins with each other promoting or inhibiting
  these processes could lead to many novel drug
  compounds

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Structural proteins

• Tubulin

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Carrier proteins
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Carrier proteins

• Examples of drugs that can move into the cell

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Carrier proteins

• Drugs that block the binding site of carrier
  proteins