FBA-TPQ, a novel marine-derived compound as experimental therapy for prostate cancer.
We recently synthesized a series of novel makaluvamine compounds, and found that the most potent was FBA-TPQ. The effects of FBA-TPQ on human (LNCaP and PC3) and murine (TRAMP C1) prostate cancer cells were evaluated. Potential mechanisms of action of the compound were also determined. FBA-TPQ exhibited dose-dependent cytotoxicity in the low micromolar range, inhibited proliferation, caused cell cycle arrest, and induced apoptosis in prostate cancer cell lines. The compound also decreased the expression of the androgen receptor and PSA. The results presented herein support the further development of FBA-TPQ as a novel agent for prostate cancer.
Wang
Feng
F
Division of Clinical Pharmacology, Department of Pharmacology and Toxicology, University of Alabama at Birmingham, 1670 University Blvd, 113 Volker Hall, Birmingham, AL 35294, USA.
Ezell
Scharri J
SJ
Zhang
Yong
Y
Wang
Wei
W
Rayburn
Elizabeth R
ER
Nadkarni
Dwayaja H
DH
Murugesan
Srinivasan
S
Velu
Sadanandan E
SE
Zhang
Ruiwen
R
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D008297:Male; D051379:Mice; D017430:Prostate-Specific Antigen / Q000378:metabolism; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D011944:Receptors, Androgen / Q000378:metabolism
C550613:7-(4-fluorobenzylamino)-1,3,4,8-tetrahydropyrrolo(4,3,2-de)quinolin-8(1H)-one; D000970:Antineoplastic Agents; D011758:Pyrroles; D015363:Quinolones; D011944:Receptors, Androgen; D017430:Prostate-Specific Antigen