Synonymous or silent mutations do not change the sequence of the protein that they encode. With some exceptions, they do not trigger any effect. Last year, however, a study by researchers from the University of Michigan tried to refute this concept after finding that they altered the protein function. But breaking dogmas can have answers. A group of scientists from various institutions has found that this work could have a method error.
Researchers have identified a druggable pocket on the phosphatase Wip1, which regulates the tumor suppressor TP53 as well as DNA damage repair proteins. The work, which was published in Frontiers in Molecular Biosciences on April 18, 2023, by researchers from the University of Pennsylvania, could lead to therapeutics targeting Wip1. And the computational deep learning methods used to identify the pocket are broadly useful for identifying what the authors call “cryptic” pockets.
Humanwell Healthcare (Group) Co. Ltd. researchers have prepared and tested AP2-associated protein kinase 1 (AAK1) inhibitors that are reported to be useful for the treatment of bipolar disorder, pain, schizophrenia, Alzheimer’s and Parkinson’s disease.
Research at Beijing Scitech-Mq Pharmaceuticals Ltd. has led to the identification of inhibitors of epidermal growth factor receptor (EGFR; HER1; erbB1) and its mutants which are reported to be useful for the treatment of cancer and autoimmune diseases.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have patented benzodiazepine derivatives acting as GABA(A) receptor subunit α2β2γ1 positive allosteric modulators and reported to be useful for the treatment of neurological disorders.
Lysyl oxidase homologue 2 (LOXL2) inhibitors have been reported in a Yuhan Corp. patent as potentially useful for the treatment of idiopathic pulmonary fibrosis, nonalcoholic steatohepatitis (NASH), chronic kidney disease and cirrhosis.
Petra Pharma Corp. has patented phosphatidylinositol 3-kinase α (PI3Kα, PIK3CA) (H1047R mutant) allosteric inhibitors reported to be useful for the treatment of cancer, congenital lipomatous overgrowth, vascular malformations, epidermal naevi and skeletal abnormalities and PIK3CA-related overgrowth spectrum.
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