Protein Complex Production from the Drug Discovery Standpoint

Area of Science:

• Biochemistry
• Pharmacology
• Drug Discovery

Background:

• * Small molecule drug discovery relies on in vitro assays for optimizing drug potency and selectivity.
• * Disease-relevant drug targets often function as protein complexes, not single proteins.
• * Protein cofactors are crucial for the function and regulation of many drug targets.

Purpose of the Study:

• * To review the trend of using protein complexes in drug discovery.
• * To highlight examples of rational drug design using protein complexes.
• * To demonstrate how this approach can reduce late-stage drug development attrition.

Main Methods:

• * Literature review of recent studies.
• * Analysis of case examples in rational drug discovery.
• * Focus on biologically relevant protein complexes as therapeutic targets.

Main Results:

• * Increasing use of protein complexes in drug discovery assays.
• * Examples show improved understanding of target function within complexes.
• * Potential for enhanced drug efficacy and reduced toxicity.

Conclusions:

• * Targeting protein complexes represents a significant advancement in drug discovery.
• * This strategy offers a more biologically relevant approach to identifying drug candidates.
• * Utilizing protein complexes can mitigate risks associated with efficacy and toxicity in later development phases.