BMPR2 mutations are the most common genetic cause of pulmonary arterial hypertension (PAH). Pulmonary artery endothelial cells (PAECs) with reduced BMPR2 expression are linked to a persistent DNA damage after reoxygenation. Forkhead box F1 (FOXF1) is a transcription factor with affinity for endothelial cells in the lung, and its reduced expression has also been associated with DNA damage in those cells and PAH.
Patients with polycystic kidney disease (PKD) are at high risk of developing end-stage renal disease, especially clear cell renal cell carcinoma (ccRCC). Since SET domain-containing 2 (SETD2) has been previously identified as an important tumor suppressor and an immunosuppressor in ccRCC, a recent study aimed to investigate the role of SETD2 in the progression of PKD into ccRCC.
Why cancer? The mechanisms that drive and maintain tumorigenesis are still a mystery. This is a play with different actors who have different roles in several contexts. One of these scenarios is represented by genetic and epigenetic conditions that determine the early trajectories of cancer cells. In addition, different mechanisms will control phenotypes and states that can take one or another direction toward cancer.
Treeline Biosciences Inc. has described proteolysis targeting chimeras (PROTACs) comprising cereblon (CRBN) ligands coupled to a Bcl-2-like protein 1 (Bcl-xL; Bcl-X; BCL2L1) targeting moiety via linker acting as Bcl-xL degradation inducers.
Revolution Medicines Inc. has divulged son of sevenless homolog 1 (SOS1) inhibitors reported to be useful for the treatment of cancer, neurofibromatosis type 1, cardiofaciocutaneous, Noonan, Costello and Legius syndrome (neurofibromatosis type 1-like syndrome), among others.
Yale University has identified compounds reported to be useful for the treatment of dry age-related macular degeneration (AMD), Fuchs endothelial corneal dystrophy, cataract, glaucoma and keratoconus.
The Korean Research Institute of Bioscience and Biotechnology has synthesized peptides reported to be useful for the treatment of inflammatory disorders.
Chiesi Farmaceutici SpA has disclosed imidazole derivatives acting as TGF-β receptor type-1 (TGFBR1; ALK5; SKR4; TβR-I) inhibitors reported to be useful for the treatment of idiopathic pulmonary fibrosis (IPF).
Researchers from the National Research Centre of Egypt and Cairo University have reported the discovery of novel acetylcholinesterase (AChE) inhibitors as candidates for the management of Alzheimer’s disease.
Triple-negative breast cancer (TNBC) is a highly metastatic and heterogeneous type of tumor, representing 15% of breast cancer cases. To tackle the drug-resistant phenotype of TNBC, effective targeted combinatorial approaches are urgently needed. Writing in EMBO Molecular Medicine journal, researchers from the Centre for Genomic Regulation and collaborators demonstrate that the simultaneous inhibition of lysyl oxidase-like 2 (LOXL2) and bromodomain-containing protein 4 (BRD4) synergistically limits TNBC proliferation in vitro and in vivo.