Yokoo, Hidetomo; Shibata, Norihito; Naganuma, Miyako; Murakami, Yuki; Fujii, Kiyonaga; Ito, Takahito; Aritake, Kosuke; Naito, Mikihiko; Demizu, Yosuke published the artcile< Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer>, Quality Control of 89793-12-4, the main research area is prostaglandin D2 ubiquitin proteasome system protein knockdown PROTACs.
Although hematopoietic prostaglandin D synthase (H-PGDS) is an attractive target for treatment of a variety of diseases, including allergic diseases and Duchenne muscular dystrophy, no H-PGDS inhibitors have yet been approved for treatment of these diseases. Therefore, the development of novel agents having other modes of action to modulate the activity of H-PGDS is required. In this study, a chimeric small mol. that degrades H-PGDS via the ubiquitin-proteasome system, PROTAC(H-PGDS)-1(I), was developed. PROTAC(H-PGDS)-1 is composed of two ligands, TFC-007 (that binds to H-PGDS) and pomalidomide (that binds to cereblon). PROTAC(H-PGDS)-1 showed potent activity in the degradation of H-PGDS protein via the ubiquitin-proteasome system and in the suppression of prostaglandin D2 (PGD2) production Notably, PROTAC(H-PGDS)-1 showed sustained suppression of PGD2 production after the drug removal, whereas PGD2 production recovered following removal of TFC-007. Thus, the H-PGDS degrader-PROTAC(H-PGDS)-1-is expected to be useful in biol. research and clin. therapies.
ACS Medicinal Chemistry Letters published new progress about Allergy. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Quality Control of 89793-12-4.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia