Overexpression of focal adhesion kinase (FAK) has been observed in several types of cancer, including gastric, esophageal and colorectal cancers. Several FAK inhibitors have advanced to clinical evaluation for the treatment of cancer, however, none have entered the market.
The specific tau isoforms, such as 3-repeat (3R) and 4-repeat (4R) isoforms, and the distinct conformational strains that misfolded tau can adopt are determinants of the molecular and clinical heterogeneity observed across tauopathies.
Using its proprietary FBDD platform, Blacksmith discovered FG-2101, the prodrug form of FG-960, the first known non-hydroxamate LpxC inhibitor that exerted activity against LpxC at the nanomolar range.
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.
Researchers from the University of Queensland recently provided details on the discovery and preclinical characterization of a new hematopoietic prostaglandin D2 synthase (HPGDS) inhibitor, CLS-189, being developed for the treatment of Duchenne muscular dystrophy (DMD).
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.
Right open reading frame kinase 2 (RIOK2) plays an essential role in ribosome assembly and cell growth, survival and stress responses. Research has linked RIOK2 to tumor progression and poor prognosis in several types of cancer such as breast, lung, prostate or hematological tumors.
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