PreadyPort-MDR1 | 수송체 평가 세포주 | 고마바이오텍

특징  

• MDR1 gene은 약물수송단백질인 P-glycoprotein (P-gp)을 encoding하는 유전자입니다. P-gp는 세포막에 존재하는 중요 당단백으로 약물배출에 관여하는 transporter 입니다. 
• MDR1 efflux transporter는 장내 흡수, 담즙 및 약물의 소변 배설, 중추 신경계로의 활성 분자 진입에 중요한 역할을 하는 유비쿼터스 조직 분포를 가지고 있습니다.
  
• PreadyPort-MDR1은 MDR1을 발현하는 분화된 MDCK II cell이 미리 seeding된 24well 혹은 96 transwell insert plate 입니다.
  
• PMDA, FDA, EMA에서는 BCRP, MDR1/P-gp를 reference efflux transporter로서 이용하도록 권고하고 있습니다. 

적용

• MDR1 substrates, inhibitors and inducers
• MDR1 transporter-based drug-drug interactions (concomitantly administered drugs)
• Drug permeability by passive diffusion through a physiologically relevant barrier
• Drug permeability by passive diffusion and MDR1 transporter through the Blood Brain Barrier

종류    

사용 과정

실험 데이터

사용 논문

• Palmer, N., Agnew, C., Benn, C., et al. (2024). Fragment-Based Discovery of a Series of Allosteric-Binding Site Modulators of β-Glucocerebrosidase. Journal of Medicinal Chemistry, 67, 1438–1454. DOI: 10.1021/acs.jmedchem.4c00702.
• Aubets, J., Jansat, J-M., Salva, M., et al. (2019). No evidence for interactions of dimethylfumarate (DMF) and its main metabolite monomethylfumarate (MMF) with human cytochrome P450 (CYP) enzymes and the P-glycoprotein (P-gp) drug transporter. Pharmacol Res Perspect, 2019;e00540. DOI: 10.1002/prp2.540.
• Mukkavilli, R., Jadhav, G., Vangala, S. (2017). Evaluation of Drug Transport in MDCKII-Wild Type, MDCKII-MDR1, MDCKII-BCRP and Caco-2 Cell Lines. Current Pharmaceutical Biotechnology, 18(14), 1151-1158(8). DOI: 10.2174/1389201019666180308091855.
• ICH M12 Drug Interaction Studies, 2022.
• FDA Guidance for Industry: In Vitro Drug Interactions Studies – Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions, 2020.
  
• EMA Guideline on Investigation of Drug Interactions, 2012.
  
• PMDA Guideline on Drug Interaction for Drug Development and Appropriate Provision of Information, 2018.