Microphthalmia associated transcription factor (Mitf) is a key regulatory transcriptional factor of pigmentation-related genes including tyrosinase. Previously, we reported the construction of a protein chip to detect binding of Mitf protein and E-box DNA. To discover the small molecule inhibitors of Mitf-DNA binding, by using the protein chip, we screened 27 chemicals which were selected from a pharmacophore data base by virtual screening. Among them, compound #18 was found to show the most potent inhibitory activity against Mitf-DNA binding. To confirm its inhibitory activity against Mitf-DNA binding, an electrophoretic mobility shift assay (EMSA) was performed. The depigmenting activity of compound #18 was confirmed by cellular melanin assay, RT-PCR, and Western blot. These results demonstrated that compound #18 is the first reported small molecule inhibitor of MITF-DNA binding with depigmenting activity and that the Mitf protein chip is a powerful HTS tool for the discovery of depigmenting agents based on inhibition of Mitf-DNA binding.
저자
Eun-Ki Kim [ Department of Biological Engineering, Skin-bioactive Material NRL, Inha University ]
한국생물공학회 [The Korean Society for Biotechnology and Bioengineering]
설립연도
1984
분야
공학>생물공학
소개
이 법인은 생물 공학의 발전과 보급에 이바지하고, 회원 상호 간의 연구 협력과 친목을 도모함을 목적으로 한다
1. 생물공학 분야의 발전을 위한 연구 협력
2. 생물공학의 실용화를 촉진시키기 위한 산학 협동
3. 학술연구 발표회, 강연회, 연수회 등 학술활동의 개최
4. 국,영문 학술지,소식지,학술회의 Proceedings 및 학술도서의 발간
5. 생물공학 발전을 위한 정책 건의
6. 기타 국제 교류 등 본 학회의 목적 달성을 위한 제반 활동