Masanori Miwa

TL;DR: It is found that a novel G protein-coupled receptor, TGR5, is responsive to bile acids as a cell-surface receptor, and was abundantly expressed in monocytes/macrophages in human and rabbit.

TL;DR: A human-origin protein or its salt can be used in determining a ligand to this protein; preventives and/or remedies for diseases in association with the dysfunction of the above protein; screening compounds (agonists, antagonists, etc.) capable of altering binding properties of the ligand as discussed by the authors.

TL;DR: In this paper, the authors reported novel and selective inhibitory peptides to K-Ras(G12D) and obtained KRpep-2 (Ac-RRCPLYISYDPVCRR-NH2) as a consensus sequence.

TL;DR: The crystal structure of the human K-Ras(G12D) mutant was determined and revealed that the peptide binds near Switch II and allosterically blocks protein-protein interactions with the guanine nucleotide exchange factor, providing valuable information that will facilitate the design of direct Ras inhibitors.

TL;DR: The discovery of the potent and selective Brr2 inhibitor 9 with helicase inhibitory activity demonstrates an effective strategy to explore selective inhibitors for helicases, and could be a promising starting point for exploring molecular probes to elucidate biological functions and the therapeutic relevance of Brr1.