CAD note by Ms. Pushpa Sahani
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This seminar discusses computer aided drug development with a focus on efflux transporters that impact drug absorption and distribution. It describes the roles of P-glycoprotein (P-gp), Breast Cancer Resistance Protein (BCRP), and nucleoside transporters. P-gp and BCRP are ATP-dependent efflux pumps that transport various substrates out of cells, reducing drug absorption and enhancing excretion. Inhibition of these pumps can improve drug delivery. Nucleoside transporters also transport natural and synthetic nucleoside drugs and impact their disposition. Understanding these transporters through computer modeling can help optimize drug properties.
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This document discusses various drug transporters and how computational models have been used to better understand them. It summarizes that P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP) are ATP-dependent efflux transporters that impact drug absorption and resistance. The document then reviews pharmacophore and QSAR models developed for these transporters to predict substrate and inhibitor requirements. Finally, it discusses nucleoside transporters and similar computational models generated to understand these transporters and their role in drug disposition.
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This document discusses active transport mechanisms including P-glycoprotein (P-gp), Breast Cancer Resistance Protein (BCRP), and nucleoside transporters. It provides details on the role of these transporters in drug absorption, distribution, and excretion. The document also describes computational models that have been developed to predict substrate requirements and inhibition of these transporters using quantitative structure-activity relationship (QSAR) analyses and pharmacophore modeling of available in vitro data. Developing an understanding of active transport mechanisms is important for computational programs aimed at predicting absorption, distribution, metabolism, excretion and toxicity (ADMET) properties of drug candidates.
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CAD note by Ms. Pushpa Sahani
- 1. SEMINAR ON SUBJECT: COMPUTER AIDED DRUG DEVELOPMENT SUBMITTED BY: SUBMITTED TO: PUSHPA SAHANI Prof K MAHALINGAN 2nd SEM M. Pharm Department of Pharmaceutics
- 5. P-GP • P-glycoprotein (p-gp) is an ATP-dependent effl ux transporter that transports a broad range of substrates out the cell. • It affects drug disposition by reducing absorption and enhancing renal and hepatic excretion. • For example, P-gp is known to limit the intestinal absorption of the anticancer drug paclitaxel and restricts the CNS penetration of human immunodeficiency virus (HIV) protease inhibitors. • It also responsible for multidrug resistance in cancer chemotherapy.
- 7. Inhibition of P-gp • The inhibition of efflux pump is mainly done in order to improve the delivery of therpeutic agents. • In general P-gp can be inhibited by 2 mechanism 1. Blocking drug binding site either competively or non competively. 2.interfering with ATP
- 8. BCRP • Breast cancer resistance protein • It is an another ATP dependent efflux transport • It confers resistance to a variety of anticancer agents anthracyclins • In addition to high level of experession in hematological and solid tumors BCRP is expressed in intestine,liver and brain thus implicating is very complicated role in drug disposition behaviour
- 9. Nucleoside Transporter • It transport both naturally occuring nucleoside and synthetic analogs that are used as anticancer drugs and viral drugs. • There are various type of nucleoside transporter including concentrative nucleoside transporter (CNT1 CNT2 CNT3) & equilibrative nucleoside transporter (ENT1 ENT2 ENT3). • Each have different substrate specificity.
- 10. • It have broad affinity, low selectivity & are ubiquitously located. • CNT have high affinity, selective located in epittelia of intestive kidney, liver & brain, indicating their involvement in drug disposition, distribution & excretion. • The first 3D, QSAR model for nucleoside transporter was generated back in 1190. • All model show the common features required for nucleoside transporter mediated transport: 2 hydrophobic features & one hydrogen bond acceptor on the pentose ring.
- 11. References Computer application in pharmaceutical research and development, by sean Ekins published by john wiley and sons inc. http://crdd.osdd.net/admet.php https://en.wikipedia.org/wiki httpps://www.solvobiotech.com/transporters/bc rp