Multidrug resistance (MDR) is one of the main obstacles in the chemotherapy of cancer. MDR is associated with the over expression of P-glycoprotein (P-gp), resulting in increased efflux of chemotherapy from cancer cells. Inhibiting Pgp as a method to reverse MDR in cancer patients has been studied extensively, but the results have generally been disappointing. First-generation agents were limited by unacceptable toxicity, whereas second-generation agents had better tolerability but were confounded by unpredictable pharmacokinetic interactions and interactions with other transporter proteins. Third-generation inhibitors have high potency and specificity for P-gp. Furthermore, pharmacokinetic studies to date have shown no appreciable impact on drug metabolism and no clinically significant drug interactions with common chemotherapy agents. Third-generation P-gp inhibitors have shown promise in clinical trials. The continued development of these agents may establish the true therapeutic potential of P-gp-mediated MDR reversal.
목차
Abstract 1. Introduction 2. Experimental Section 2.1. Domain Organization 2.2. Drug Binding and Transport 2.3. Polyspecificity of Drug Binding Pocket 2.4. P-gp Modulators 3. Result and Discussion References
Changdev G. Gadhe [ Department of Bio-New Drug Development, College of Medicine, Chosun University ]
Seung Joo Cho [ Department of Bio-New Drug Development, College of Medicine, Chosun University, Department of Cellular·Molecular Medicine and Research Center for Resistant Cells, College of Medicine, Chosun University ]
Corresponding author
조선대학교 기초과학연구원 [The Natural Science Research Institute of Chosun]
설립연도
2008
분야
자연과학>자연과학일반
소개
본 연구원은 기초과학을 진흥하기 위한 연구·교육 및 그 보급을 목적으로 한다. 이 목적을 달성하기 위하여 다음 각 호의 사업을 수행한다.
1. 기초과학 제 분야에 관한 조사와 연구
2. 기초과학에 관한 학술행사(학술대회, 학술세미나, 심포지엄, 초청강연회 등) 개최
3. 학문후속세대 및 일반인을 위한 기초과학 교육
4. 기관지『조선자연과학논문지』 발간
5. 『자연과학연구총서』, 『자연과학번역총서』 등 단행본 발간
6. 기타 본 연구원의 목적과 관련된 사업
간행물
간행물명
통합자연과학논문집(구 조선자연과학논문집) [Journal of Integrative Natural Science]