Homodimers as enzyme inhibitors

The symmetrical arrangement of enzymes into homodimers or tetramers defines the active site of the enzyme in a highly symmetrical fashion. Thus, symmetrical inhibitors will correspond generally to the binding site of the enzyme. 

The protein kinase C (PKC) enzyme family plays a pivotal role in the signal transduction pathways of hormones, neurotransmitters and other endogenous substances. The 11 PKC isoenzymes identified are involved in the activation of many cellular functions. PKCs possess a C-terminal catalytic region with a serine/threonine kinase function and N-terminal regulatory region. The regulatory region is 

Inhibitors of factor Xa (FXa), a serine protease involved in the cascade coagulation, would allow to control the coagulation process and bleeding problems. Discovery of orally 

CHAPTER 18 Homo and Heterodimer Ligands the Twin Drug Approach 

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