Literature DB >> 26642765

Synthesis of a new inhibitor of breast cancer resistance protein with significantly improved pharmacokinetic profiles.

Yuexian Li1, Jiyeon Woo2, Jessica Chmielecki3, Cindy Q Xia4, Mingxiang Liao4, Bei-Ching Chuang4, Johnny J Yang4, Miao Y Guan4, Mihaela Plesescu4, Shimoga R Prakash4.   

Abstract

The design, synthesis, in vitro inhibitory potency, and pharmacokinetic (PK) profiles of Ko143 analogs are described. Compared to commonly used Ko143, the new breast cancer resistance protein (BCRP) inhibitor (compound A) showed the same potency and a significantly improved PK profile in rats (lower clearance [1.54L/h/kg] and higher bioavailability [123%]). Ko143 on the other hand suffers from poor bioavailability. Compared to Ko143, compound A would be a useful probe for delineating the role of BCRP during in vivo studies in animals.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  BCRP; Compound A; Inhibitors; Ko134; Ko143; PK profiles

Mesh：

Substances：

Year:  2015        PMID： 26642765     DOI： 10.1016/j.bmcl.2015.11.077

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

1.  Development of Simple and Accurate in Silico Ligand-Based Models for Predicting ABCG2 Inhibition.

Authors:  Shuheng Huang; Yingjie Gao; Xuelian Zhang; Ji Lu; Jun Wei; Hu Mei; Juan Xing; Xianchao Pan
Journal:  Front Chem       Date:  2022-05-18       Impact factor: 5.545

2.  ADMET evaluation in drug discovery. 20. Prediction of breast cancer resistance protein inhibition through machine learning.

Authors:  Dejun Jiang; Tailong Lei; Zhe Wang; Chao Shen; Dongsheng Cao; Tingjun Hou
Journal:  J Cheminform       Date:  2020-03-05       Impact factor: 5.514

3.  Botryllamide G is an ABCG2 inhibitor that improves lapatinib delivery in mouse brain.

Authors:  Jonathan D Strope; Cody J Peer; Tristan M Sissung; O Morgan Hall; Phoebe A Huang; Emily M Harris; Kirk R Gustafson; Curtis J Henrich; Dina M Sigano; Gary T Pauly; Joel P Schneider; Susan E Bates; William D Figg
Journal:  Cancer Biol Ther       Date:  2019-11-10       Impact factor: 4.742

Review 4.  Recent advances in the search of BCRP- and dual P-gp/BCRP-based multidrug resistance modulators.

Authors:  Silvia Dei; Laura Braconi; Maria Novella Romanelli; Elisabetta Teodori
Journal:  Cancer Drug Resist       Date:  2019-09-19

5.  The Evaluation of l-Tryptophan Derivatives as Inhibitors of the l-Type Amino Acid Transporter LAT1 (SLC7A5).

Authors:  Julien Graff; Jennifer Müller; Anna Sadurní; Matthias Rubin; Inês André Canivete Cuissa; Claudia Keller; Marco Hartmann; Simon Singer; Jürg Gertsch; Karl-Heinz Altmann
Journal:  ChemMedChem       Date:  2022-08-10       Impact factor: 3.540
  5 in total

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