Protein Information

Name P gp
Synonyms ABC20; MDR1; ABCB 1; ABCB1; ATP binding cassette sub family B member 1; CD243; CD243 antigen; CLCS…

Compound Information

Name naphthalene
CAS naphthalene

Reference List

PubMed Abstract RScore(About this table)
16959878 Chang JH, Kochansky CJ, Shou M: The role of P-glycoprotein in the bioactivation of raloxifene. . Drug Metab Dispos. 2006 Dec;34(12):2073-8. Epub 2006 Sep 7.

The aim of this work was to examine the role of P-glycoprotein (Pgp) in the bioactivation of a Pgp substrate, raloxifene, and a non-Pgp substrate, naphthalene.
82(1,1,1,2) Details
19135510 Pan WC, Chen RM, Shen YC, Chen CC, Ueng YF: Suppressive effect of tobacco smoke extracts on oral P-glycoprotein function and its impact in smoke-induced insult to oral epidermal cells. Toxicol Lett. 2009 Mar 10;185(2):116-23. Epub 2008 Dec 24.

Naphthalene, mainly detected in the ITS, decreased Rh 123 efflux.
2(0,0,0,2) Details
18473435 Nakagawa-Goto K, Bastow KF, Chen TH, Morris-Natschke SL, Lee KH: Antitumor agents 260. J Med Chem. 2008 Jun 12;51(11):3297-303. Epub 2008 May 13.

The unique activity of 1-analogues is likely MDR-mediated because cotreatment with verapamil, a P-gp inhibitor, partially reversed the selective toxicity of both 1 and 10.
Interestingly, only 1-analogues with a naphthalene B-ring (8 and 14) showed significant cytotoxic activity against KB and other cancer cell lines.
1(0,0,0,1) Details