수업
협동과정 뇌과학전공 초청세미나 5.11 ( 연사: 강혜진 성균관대학교 생명과학과 교수)
2023-05-08
- 제목 : A Multiplexed GPCR Screening Platform that Sheds Light on New Biology
- 연사 : 강혜진 교수님 (성균관대학교 생명과학과)
- 초정자 : 김형 교수님 (서울대학교 생명과학부)
- 일시 : 2023년 5월 11일 (목) 오전 11시
- 장소: 서울대학교 관악캠퍼스 28동 101호
- Abstract :New ligands are discovered through a multiplexed GPCR screening platform, which gives information on novel biology, particularly enlightening of 1) novel itch receptor function and 2) development of new chemogenetic tools. The MRGPRX receptor family (MRGPRX1–4) is a group of mas-related G-protein-coupled receptors that has only recently emerged. MRGPRX2 and MRGPRX4 are two of the most important physiological and pathological mediators of itch and mast cell-mediated hypersensitivity reactions. MRGPRX2 couples to both Gi and Gq in mast cells. We present the creation of effective antagonist probes for MRGPRX2, as well as agonist-stabilized structures of MRGPRX2 bound to Gi1 and Gq in ternary complexes with the natural peptide cortistatin-14 and a synthesized agonist probe, respectively. A particular MRGPRX4 agonist is also described, as well as its structure in a complex with MRGPRX4 and Gq. These discoveries should help speed up the development of structure-guided therapeutics for pain, itch, and mast cell-mediated hypersensitivity. Chemogenetic technologies such as Designer Receptors Exclusively Activated by Designer Drugs (DREADDs) have substantially impacted biological research. Here we will reveal how recent advances in GPCR structural biology and the availability of large libraries of drug-like compounds have allowed us to create new chemogenetic tools and actuators.