Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is an attractive therapeutic target due to its involvement in cancer and neurodegenerative diseases. Researchers from the National Health Research Institutes and their collaborators have presented a series of DYRK1A inhibitors for reducing neurofibrillary tangle formation  in Alzheimer’s disease.

Cannabinoid CB1 receptors have been a potential target for nonopioid-based pain treatment, but actually targeting the pathway has been hindered by issues with tolerance and unwanted CNS side effects. Peripherally selective CB1 agonists developed to overcome these problems have not fully resolved these issues, meaning the peripheral selectivity has to be substantially enhanced.

Histone deacetylase 3 (HDAC3) is involved in transcriptional regulation, phosphorylation and the inhibition of tumor suppressor genes. Its upregulation in several types of tumors, such as colorectal, prostate, breast and ovarian cancers, among others, makes it a potential therapeutic target in cancer.

Researchers from Ileadbms Co. Ltd. presented the discovery and preclinical characterization of IL-21120033, a new CXCR7 agonist being developed for the treatment of inflammatory bowel disease.

Targeted protein degradation (TPD) is an alternative to conventional protein inhibition that is gaining attention due to advantages such as ensuring complete elimination of the target protein, reduced off-target effects or the potential to target previously inaccessible or “undruggable” proteins. Proteolysis targeting chimeras (PROTACs) are agents used for TPD that have proven effective for degradation of histone deacetylase (HDAC), among other different proteins.