Log in

Relevant bibliographies by topics / P-gp inhibition

Contents

Journal articles
Dissertations / Theses
Book chapters
Conference papers

Academic literature on the topic 'P-gp inhibition'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles

Select a source type:

Consult the lists of relevant articles, books, theses, conference reports, and other scholarly sources on the topic 'P-gp inhibition.'

Next to every source in the list of references, there is an 'Add to bibliography' button. Press on it, and we will generate automatically the bibliographic reference to the chosen work in the citation style you need: APA, MLA, Harvard, Chicago, Vancouver, etc.

You can also download the full text of the academic publication as pdf and read online its abstract whenever available in the metadata.

Journal articles on the topic "P-gp inhibition"

1

Han, Seung, Qili Lu, Kyeong Lee, and Young Choi. "LC478, a Novel Di-Substituted Adamantyl Derivative, Enhances the Oral Bioavailability of Docetaxel in Rats." Pharmaceutics 11, no. 3 (2019): 135. http://dx.doi.org/10.3390/pharmaceutics11030135.

Full text

Abstract:

P-glycoprotein (P-gp)-mediated efflux of docetaxel in the gastrointestinal tract mainly impedes its oral chemotherapy. Recently, LC478, a novel di-substituted adamantyl derivative, was identified as a non-cytotoxic P-gp inhibitor in vitro. Here, we assessed whether LC478 enhances the oral bioavailability of docetaxel in vitro and in vivo. LC478 inhibited P-gp mediated efflux of docetaxel in Caco-2 cells. In addition, 100 mg/kg of LC478 increased intestinal absorption of docetaxel, which led to an increase in area under plasma concentration-time curve (AUC) and absolute bioavailability of docet

APA, Harvard, Vancouver, ISO, and other styles

2

O'Brien, Fionn E., Gerard Clarke, Timothy G. Dinan, John F. Cryan, and Brendan T. Griffin. "Human P-glycoprotein differentially affects antidepressant drug transport: relevance to blood–brain barrier permeability." International Journal of Neuropsychopharmacology 16, no. 10 (2013): 2259–72. http://dx.doi.org/10.1017/s1461145713000692.

Full text

Abstract:

Abstract The pharmacological concept that inhibition of the drug efflux pump P-glycoprotein (P-gp) enhances brain distribution of the antidepressant imipramine in the rat has recently been demonstrated. To determine if these findings are relevant to humans, the present study investigated if imipramine is a transported substrate of human P-gp. Furthermore, additional experiments were carried out to determine if findings in relation to imipramine and human P-gp would apply to other antidepressants from a range of different classes. To this end, bidirectional transport experiments were carried ou

APA, Harvard, Vancouver, ISO, and other styles

3

Dewanjee, Saikat, Tarun Dua, Niloy Bhattacharjee, et al. "Natural Products as Alternative Choices for P-Glycoprotein (P-gp) Inhibition." Molecules 22, no. 6 (2017): 871. http://dx.doi.org/10.3390/molecules22060871.

Full text

APA, Harvard, Vancouver, ISO, and other styles

4

Demeule, Michel, Alain Laplante, Arash Sepehr-Araé, et al. "Inhibition of P-glycoprotein by cyclosporin A analogues and metabolites." Biochemistry and Cell Biology 77, no. 1 (1999): 47–58. http://dx.doi.org/10.1139/o99-011.

Full text

Abstract:

The interaction between P-glycoprotein (P-gp) from membranes isolated from multidrug-resistant Chinese hamster ovary cells and cyclosporin A (CsA) analogues and its metabolites was characterized. Screening of these latter as chemosensitizers was performed using three different assays: (i) vinblastine uptake, (ii) photoaffinity labeling by [125I]iodoaryl azidoprazosin, and (iii) P-gp ATPase activity. Oxidation of the hydroxyl group at position 1 of CsA (200-096), CsG (215-834), or CsD (PSC-833) increased their inhibition of P-gp. CsA analogues (208-032, 208-183) modified at position 11 retained

APA, Harvard, Vancouver, ISO, and other styles

5

SCHRICKX, J. A., and J. FINK-GREMMELS. "A porcine lymphocyte model for P-gp inhibition studies." Journal of Veterinary Pharmacology and Therapeutics 34, no. 5 (2011): 499–501. http://dx.doi.org/10.1111/j.1365-2885.2011.01270.x.

Full text

APA, Harvard, Vancouver, ISO, and other styles

6

Sianipar, Erlia Anggrainy, Melva Louisa, and Septelia Inawati Wanandi. "Kurkumin Meningkatkan Sensitivitas Sel Kanker Payudara terhadap Tamoksifen Melalui Penghambatan Ekspresi P-glikoprotein dan Breast Cancer Resistance Protein." Jurnal Farmasi Galenika (Galenika Journal of Pharmacy) (e-Journal) 4, no. 1 (2018): 1–11. http://dx.doi.org/10.22487/j24428744.2018.v4.i1.9209.

Full text

Abstract:

The decreasing of sensitivity or resistance to tamoxifen occured after long-term treatment in breast cancer. One of the major factor in tamoxifen resistance is over expression of efflux transporter P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP). Curcumin has known as inhibitor of P-gp and BCRP. The addition of curcumin to the tamoxifen resistant cells is expected to increase the sensitivity of breast cancer cells to tamoxifen. This study aim to know the effect of curcumin in increasing the cell sensitivity to tamoxifen through inhibition of P-gp and BCRP transporter efflux.

APA, Harvard, Vancouver, ISO, and other styles

7

Lee, Jaeok, Song Wha Chae, A. Reum Oh, et al. "Effects of Piperazine Derivative on Paclitaxel Pharmacokinetics." Pharmaceutics 11, no. 1 (2019): 23. http://dx.doi.org/10.3390/pharmaceutics11010023.

Full text

Abstract:

Paclitaxel (PTX) is an anticancer agent that is used to treat many cancers but it has a very low oral bioavailability due, at least in part, to the drug efflux transporter, P-glycoprotein (P-gp). Therefore, this study was performed to enhance oral bioavailability of PTX. In this study, we investigated the effects of several piperazine derivatives on P-gp function in vitro. Compound 4 was selected as the most potent P-gp inhibitor from the in vitro results for examining the pharmacokinetic (PK) changes of PTX in rats. Compound 4 increased the AUCinf of PTX without alterations in the Cmax value.

APA, Harvard, Vancouver, ISO, and other styles

8

Perini, Pietro, Sara Redaelli, Rocco Piazza, Michela Viltadi, Frank Boschelli, and Carlo Gambacorti. "Bosutinib is a Substrate of the ABC Efflux Transporter P-Glycoprotein." Blood 114, no. 22 (2009): 3763. http://dx.doi.org/10.1182/blood.v114.22.3763.3763.

Full text

Abstract:

Abstract Abstract 3763 Poster Board III-699 Bosutinib (Bos) (Wyeth Pharmaceuticals) is a dual Src-Abl tyrosine kinase inhibitor developed to inhibit the activity of BCR-ABL in chronic myeloid leukemia. P-glycoprotein (P-gp) is an ATP-binding cassette (ABC) transporter responsible of Imatinib (Im) efflux, and its increased expression can be related to Im resistance. The aim of the study was to define if P-gp is also responsible for the cellular efflux of Bos, and if P-gp altered expression can be related to Bos resistance. Four different K562 Ph+ cell lines were used. 1) K562S, Im sensitive; 2)

APA, Harvard, Vancouver, ISO, and other styles

9

Lee, Jaeok, Jiyeon Kang, Na-Yun Kwon, et al. "Dual Inhibition of P-gp and BCRP Improves Oral Topotecan Bioavailability in Rodents." Pharmaceutics 13, no. 4 (2021): 559. http://dx.doi.org/10.3390/pharmaceutics13040559.

Full text

Abstract:

P-glycoprotein (P-gp) inhibition has been studied to overcome multidrug resistance in cancer chemotherapy but failed in clinical trials due to low/toxic effects. Recently, a dual modulation of transporters and natural derivatives have been examined to surmount this limitation. We examined breast cancer resistance protein (BCRP) inhibition in vitro and in vivo by P-gp inhibitors derived from natural compounds in previous studies. P-gp inhibitors increased the accumulation of the anticancer drug, topotecan (TPT)—a substrate of P-gp and BCRP, albeit with higher affinity for BCRP—in BCRP-overexpre

APA, Harvard, Vancouver, ISO, and other styles

10

Teodori, Elisabetta, Laura Braconi, Silvia Bua, et al. "Dual P-Glycoprotein and CA XII Inhibitors: A New Strategy to Reverse the P-gp Mediated Multidrug Resistance (MDR) in Cancer Cells." Molecules 25, no. 7 (2020): 1748. http://dx.doi.org/10.3390/molecules25071748.

Full text

Abstract:

A new series of N,N-bis(alkanol)amine aryl diesters was synthesized and studied as dual P-glycoprotein (P-gp) and carbonic anhydrase XII inhibitors (CA XII). These hybrids should be able to synergistically overcome P-gp mediated multidrug resistance (MDR) in cancer cells. It was reported that the efflux activity of P-gp could be modulated by CA XII, as the pH reduction caused by CA XII inhibition produces a significant decrease in P-gp ATPase activity. The new compounds reported here feature both P-gp and CA XII binding moieties. These hybrids contain a N,N-bis(alkanol)amine diester scaffold f

APA, Harvard, Vancouver, ISO, and other styles

More sources

Dissertations / Theses on the topic "P-gp inhibition"

1

Persson, Eva. "Drug Dissolution under Physiologically Relevant Conditions In Vitro and In Vivo." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis : Universitetsbiblioteket [distributör], 2006. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-7195.

Full text

APA, Harvard, Vancouver, ISO, and other styles

2

Pogorzelec, Michael P. J. "Protein kinase inhibitor effects on P-glycoprotein (P-gp) activity and expression in various cell lines." 2015. http://hdl.handle.net/1993/30206.

Full text

Abstract:

Little is known about potential influences of kinase pathway modulation on expression and activity of P-glycoprotein (P-gp). A protein kinase inhibitor (PKI) library was screened, to determine its effects on activity and expression of P-gp, in various cell lines. Cell lines were incubated with PKI for 24 h. Subsequent P-gp substrate accumulation studies were performed. Changes in P-gp activity and/or expression ≥ 25% compared to control were considered hits. Kinase pathways identified as P-gp activity hits were examined for their ability to modulate permeability. PKI families GSK-3, Craf1

APA, Harvard, Vancouver, ISO, and other styles

3

Kim, Winnie Young. "Modulation of P-glycoprotein (P-gp/MDR1) expression and function by sex-steroid hormones and its effect on HIV protease inhibitor pharmacokinetics /." 2004. http://gateway.proquest.com/openurl?url_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:dissertation&res_dat=xri:pqdiss&rft_dat=xri:pqdiss:3149696.

Full text

APA, Harvard, Vancouver, ISO, and other styles

4

Matos, Ana Marta de Jesus Gomes de. "Development of a small library of macrocyclic diterpenes through molecular derivatization : evaluation of their activity as P-gp inhibitor." Master's thesis, 2013. http://hdl.handle.net/10451/11253.

Full text

Abstract:

Tese de mestrado, Química Farmacêutica e Terapêutica, Universidade de Lisboa, Faculdade de Farmácia, 2013<br>The present dissertation focuses on the relevance of macrocyclic diterpenes as leads for natural product-based anticancer drug development. In particular, the applicability of this type of compounds as P-glycoprotein (P-gp) inhibitors is thoroughly explored, given the well-known role of P-gp overexpression in the emergence of many multidrug resistant cancers, a major public health problem worldwide. Herein, a small library of macrocyclic lathyrane diterpenes was developed through molec

APA, Harvard, Vancouver, ISO, and other styles

Book chapters on the topic "P-gp inhibition"

1

M. Jasim, Adnan, and Mohammed J. Jawad. "Pharmaceutical Applications of Vitamin E TPGS." In Vitamin E in Health and Disease - Interactions, Diseases and Health Aspects [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.97474.

Full text

Abstract:

D-tocopheryl polyethylene glycol succinate (Vitamin E TPGS) has been approved as a safe pharmaceutical adjuvant by FDA, and several drug delivery systems (DDS) based on TPGS have been developed. TPGS properties as a P-gp inhibitor, solubilizer/absorption and permeation enhancer in drug delivery and TPGS-related formulations such as nanocrystals, nanosuspensions, tablets/solid dispersions, vaccine system adjuvant, nutritional supplement, film plasticizer, anticancer reagent, and so on, are discussed in this review. Consequenly, TPGS can inhibit ATP-dependent P-glycoprotein activity and act as a potent excipient that promotes the efficiency of delivery and the therapeutic effect of drugs. Inhibition of P-gp occurs through mitochondria-dependent inhibition of the P-gp pump. Many of the latest studies address the use of TPGS for many poorly water-soluble or permeable drugs in the manufacture of nanodrugs or other formulations. In addition, it has been reported that TPGS shows a robust improvement in chylomicron secretion at low concentrations and improves intestinal lymphatic transport, which would also boost the potential of drug absorption. It also indicates that there are still many problems facing clinical translation of TPGS-based nanomedicines, requiring a more deep evaluation of TPGS properties and a future-based delivery method.

APA, Harvard, Vancouver, ISO, and other styles

Conference papers on the topic "P-gp inhibition"

1

Cheon, Ji Hyun, Yu Jin Park, Ji Yeon Son, Sung Pil Yoon, and Hyung Sik Kim. "Abstract 2059: Co-treatment of XL019, a selective Jak2 inhibitor, highly sensitizes drug-resistant cancer cells by increasing P-gp inhibition." In Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC. American Association for Cancer Research, 2017. http://dx.doi.org/10.1158/1538-7445.am2017-2059.

Full text

APA, Harvard, Vancouver, ISO, and other styles

2

Park, Yu Jin, Ji Hyun Cheon, Ji Yeon Son, Sung Pil Yoon, and Hyung Sik Kim. "Abstract 2058: Co-treatment of NVP-BSK805 highly sensitizes drug-resistant cancer cells by increasing P-gp inhibition." In Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC. American Association for Cancer Research, 2017. http://dx.doi.org/10.1158/1538-7445.am2017-2058.

Full text

APA, Harvard, Vancouver, ISO, and other styles

3

Topletz-Erickson, Ariel R., Anthony Lee, Hao Sun, JoAl Mayor, Luke Walker, and Christopher J. Endres. "Abstract 3016: Tucatinib inhibits CYP3A, CYP2C8 and P-gp-mediated elimination and is impacted by CYP2C8 inhibition in healthy volunteers." In Proceedings: AACR Annual Meeting 2020; April 27-28, 2020 and June 22-24, 2020; Philadelphia, PA. American Association for Cancer Research, 2020. http://dx.doi.org/10.1158/1538-7445.am2020-3016.

Full text

APA, Harvard, Vancouver, ISO, and other styles

4

Sakariassen, S. K., E. Fressinaud, D. Meyer, J. J. Sixma, and R. H. Baumgartner. "RHEOLOGY AND PLATELET-SURFACE ADHESION." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1643987.

Full text

Abstract:

The process of platelet adhesion to sites of vascular injury is pivotal for the arrest of bleeding. The same process may, on the other hand, lead to formation of mural thrombi and may play a role in atherogenesis through the release of platelet-derived growth factor. The events of platelet-surface adhesion may be divided into initial attachment and the subsequent spreading on the surface. These interactions are mediated by a variety of factors, including glycoproteins (GP) in the platelet membrane, von Willebrand factor (vWF) in plasma, and the composition of the surface.However, in most insta

APA, Harvard, Vancouver, ISO, and other styles

We offer discounts on all premium plans for authors whose works are included in thematic literature selections. Contact us to get a unique promo code!