Reviews & Analysis

Inhibitor of apoptosis (IAP) antagonists have recently entered the stage of clinical evaluation for many different types of cancer. Here, Fulda and Vucic review the different approaches that have been used to target IAP proteins, and discuss their translation into therapeutic anticancer strategies.

Studies of psychiatric disorders have traditionally focused on emotional symptoms, such as depression, anxiety and hallucinations, but poorly controlled cognitive deficits are also prominent and severely compromise quality of life. This article critically discusses our understanding of the nature and causes of cognitive impairment in psychiatric disorders, and reviews the opportunities and challenges in improving cognition in patients, including the development of more effective translational research approaches.

Here, the authors highlight how RNA-blocking oligonucleotides can redirect alternative splicing, repair defective RNA, restore protein production or downregulate gene expression, and so may be useful for treating disorders such as Duchenne muscular dystrophy, spinal muscular atrophy and β-thalassaemia.

Here, the authors highlight the role of proteinase-activated receptors in physiology and in conditions such as cancer and cardiovascular disorders. They also review possible strategies for developing proteinase-activated receptor antagonists and the challenges associated with this goal.

Serine hydrolases are one of the largest and most diverse enzyme classes in nature and have many crucial roles in human physiology and disease. Several serine hydrolases are targets of clinically approved drugs, but many enzymes in this family remain poorly characterized and lack selective inhibitors. Here, Bachovchin and Cravatt discuss the therapeutic potential of serine hydrolases and present novel inhibitor discovery strategies.