Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Sulindac Sulfide Selectively Increases Sensitivity of ABCC1 Expressing Tumor Cells to Doxorubicin and Glutathione Depletion. Journal of biomedical research. . NIHMSID: NIHMS841536.
Pan-RAS inhibitors: Hitting multiple RAS isozymes with one stone. Advances in cancer research. . NIHMSID: NIHMS1884316.
Piazza GA, Wallace RW. Calmodulin accelerates the rate of polymerization of human platelet actin and alters the structural characteristics of actin filaments. Proc Natl Acad Sci U S A. 1985 Mar;82(6):1683-7. doi: 10.1073/pnas.82.6.1683. PubMed PMID: 3856849; PubMed Central PMCID: PMC397336.
Wallace RW, Piazza GA. Calmodulin and actin polymerization. Methods Enzymol. 1987;139:846-57. doi: 10.1016/0076-6879(87)39131-1. PubMed PMID: 3587050.
Piazza G, Callanan H, Mowery J, Hixson D. Evidence for a novel interaction between fibronectin and rat hepatocyte dipeptidylpeptidase IV. Biochemical Journal; 1989.
Hong WJ, Piazza GA, Hixson DC, Doyle D. Expression of enzymatically active rat dipeptidyl peptidase IV in Chinese hamster ovary cells after transfection. Biochemistry. 1989 Oct 17;28(21):8474-9. doi: 10.1021/bi00447a030. PubMed PMID: 2605197.
Stearns ME, Piazza GA. Properties of kinesin isolated from human prostatic DU 145 tumor cells and bovine brain. Biochem Cell Biol. 1990 Feb;68(2):436-40. doi: 10.1139/o90-061. PubMed PMID: 2140513.
Piazza GA, Ritter JL, Baracka CA. Lysophosphatidic acid induction of transforming growth factors alpha and beta: modulation of proliferation and differentiation in cultured human keratinocytes and mouse skin. Exp Cell Res. 1995 Jan;216(1):51-64. doi: 10.1006/excr.1995.1007. PubMed PMID: 7813633.
Piazza GA, Rahm AL, Krutzsch M, Sperl G, Paranka NS, Gross PH, Brendel K, Burt RW, Alberts DS, Pamukcu R. Antineoplastic drugs sulindac sulfide and sulfone inhibit cell growth by inducing apoptosis. Cancer Res. 1995 Jul 15;55(14):3110-6. PubMed PMID: 7606732.
Thompson HJ, Briggs S, Paranka NS, Piazza GA, Brendel K, Gross PH, Sperl GJ, Pamukcu R, Ahnen DJ. Inhibition of mammary carcinogenesis in rats by sulfone metabolite of sulindac. J Natl Cancer Inst. 1995 Aug 16;87(16):1259-60. PubMed PMID: 7563174.
Piazza G, Pamukcu R. Apoptosis induction as a mechanism for the antineoplastic properties of FGN-1, a drug for treating premalignant lesions. Boston, MA: Apoptosis; Practical Applications and Novel Therapies, IBC Publishing Co; 1997.
Thompson HJ, Jiang C, Lu J, Mehta RG, Piazza GA, Paranka NS, Pamukcu R, Ahnen DJ. Sulfone metabolite of sulindac inhibits mammary carcinogenesis. Cancer Res. 1997 Jan 15;57(2):267-71. PubMed PMID: 9000566.
Piazza GA, Rahm AK, Finn TS, Fryer BH, Li H, Stoumen AL, Pamukcu R, Ahnen DJ. Apoptosis primarily accounts for the growth-inhibitory properties of sulindac metabolites and involves a mechanism that is independent of cyclooxygenase inhibition, cell cycle arrest, and p53 induction. Cancer Res. 1997 Jun 15;57(12):2452-9. PubMed PMID: 9192825.
Piazza GA, Alberts DS, Hixson LJ, Paranka NS, Li H, Finn T, Bogert C, Guillen JM, Brendel K, Gross PH, Sperl G, Ritchie J, Burt RW, Ellsworth L, Ahnen DJ, Pamukcu R. Sulindac sulfone inhibits azoxymethane-induced colon carcinogenesis in rats without reducing prostaglandin levels. Cancer Res. 1997 Jul 15;57(14):2909-15. PubMed PMID: 9230200.
Arber N, Han E, Sgambato A, Piazza G, Pamukcu R, Ahnen A, Delohery T, Begemman M, Wegharst, Kim N, Weinstein I. c-K-ras overexpression in rat enterocytes causes resistance to sulindac sulfide induced apoptosis. Gastroenterology; 1998.
Han EK, Arber N, Yamamoto H, Lim JT, Delohery T, Pamukcu R, Piazza GA, Xing WQ, Weinstein IB. Effects of sulindac and its metabolites on growth and apoptosis in human mammary epithelial and breast carcinoma cell lines. Breast Cancer Res Treat. 1998 Apr;48(3):195-203. doi: 10.1023/a:1005924730450. PubMed PMID: 9598866.
Malkinson AM, Koski KM, Dwyer-Nield LD, Rice PL, Rioux N, Castonguay A, Ahnen DJ, Thompson H, Pamukcu R, Piazza GA. Inhibition of 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone-induced mouse lung tumor formation by FGN-1 (sulindac sulfone). Carcinogenesis. 1998 Aug;19(8):1353-6. doi: 10.1093/carcin/19.8.1353. PubMed PMID: 9744528.
Skopińska-Rózewska E, Piazza GA, Sommer E, Pamukcu R, Barcz E, Filewska M, Kupis W, Caban R, Rudziński P, Bogdan J, Mlekodaj S, Sikorska E. Inhibition of angiogenesis by sulindac and its sulfone metabolite (FGN-1): a potential mechanism for their antineoplastic properties. Int J Tissue React. 1998;20(3):85-9. PubMed PMID: 9894180.
Goluboff ET, Shabsigh A, Saidi JA, Weinstein IB, Mitra N, Heitjan D, Piazza GA, Pamukcu R, Buttyan R, Olsson CA. Exisulind (sulindac sulfone) suppresses growth of human prostate cancer in a nude mouse xenograft model by increasing apoptosis. Urology. 1999 Feb;53(2):440-5. doi: 10.1016/s0090-4295(98)00513-5. PubMed PMID: 9933075.
Lim JT, Piazza GA, Han EK, Delohery TM, Li H, Finn TS, Buttyan R, Yamamoto H, Sperl GJ, Brendel K, Gross PH, Pamukcu R, Weinstein IB. Sulindac derivatives inhibit growth and induce apoptosis in human prostate cancer cell lines. Biochem Pharmacol. 1999 Oct 1;58(7):1097-107. doi: 10.1016/s0006-2952(99)00200-2. PubMed PMID: 10484067.
Stoner GD, Budd GT, Ganapathi R, DeYoung B, Kresty LA, Nitert M, Fryer B, Church JM, Provencher K, Pamukcu R, Piazza G, Hawk E, Kelloff G, Elson P, van Stolk RU. Sulindac sulfone induced regression of rectal polyps in patients with familial adenomatous polyposis. Adv Exp Med Biol. 1999;470:45-53. doi: 10.1007/978-1-4615-4149-3_5. PubMed PMID: 10709673.
Thompson WJ, Piazza GA, Li H, Liu L, Fetter J, Zhu B, Sperl G, Ahnen D, Pamukcu R. Exisulind induction of apoptosis involves guanosine 3',5'-cyclic monophosphate phosphodiesterase inhibition, protein kinase G activation, and attenuated beta-catenin. Cancer Res. 2000 Jul 1;60(13):3338-42. PubMed PMID: 10910034.
Lawson KR, Ignatenko NA, Piazza GA, Cui H, Gerner EW. Influence of K-ras activation on the survival responses of Caco-2 cells to the chemopreventive agents sulindac and difluoromethylornithine. Cancer Epidemiol Biomarkers Prev. 2000 Nov;9(11):1155-62. PubMed PMID: 11097222.
Piazza GA, Thompson WJ, Pamukcu R, Alila HW, Whitehead CM, Liu L, Fetter JR, Gresh WE Jr, Klein-Szanto AJ, Farnell DR, Eto I, Grubbs CJ. Exisulind, a novel proapoptotic drug, inhibits rat urinary bladder tumorigenesis. Cancer Res. 2001 May 15;61(10):3961-8. PubMed PMID: 11358813.
Bunn PA Jr, Chan DC, Earle K, Zhao TL, Helfrich B, Kelly K, Piazza G, Whitehead CM, Pamukcu R, Thompson W, Alila H. Preclinical and clinical studies of docetaxel and exisulind in the treatment of human lung cancer. Semin Oncol. 2002 Feb;29(1 Suppl 4):87-94. doi: 10.1053/sonc.2002.31529. Review. PubMed PMID: 11894018.
Chan DC, Earle KA, Zhao TL, Helfrich B, Zeng C, Baron A, Whitehead CM, Piazza G, Pamukcu R, Thompson WJ, Alila H, Nelson P, Bunn PA Jr. Exisulind in combination with docetaxel inhibits growth and metastasis of human lung cancer and prolongs survival in athymic nude rats with orthotopic lung tumors. Clin Cancer Res. 2002 Mar;8(3):904-12. PubMed PMID: 11895925.
Joe AK, Liu H, Xiao D, Soh JW, Pinto JT, Beer DG, Piazza GA, Thompson WJ, Weinstein IB. Exisulind and CP248 induce growth inhibition and apoptosis in human esophageal adenocarcinoma and squamous carcinoma cells. J Exp Ther Oncol. 2003 Mar-Apr;3(2):83-94. doi: 10.1046/j.1359-4117.2003.01076.x. PubMed PMID: 12822514.
Whitehead CM, Earle KA, Fetter J, Xu S, Hartman T, Chan DC, Zhao TL, Piazza G, Klein-Szanto AJ, Pamukcu R, Alila H, Bunn PA Jr, Thompson WJ. Exisulind-induced apoptosis in a non-small cell lung cancer orthotopic lung tumor model augments docetaxel treatment and contributes to increased survival. Mol Cancer Ther. 2003 May;2(5):479-88. PubMed PMID: 12748310.
Rice PL, Kelloff J, Sullivan H, Driggers LJ, Beard KS, Kuwada S, Piazza G, Ahnen DJ. Sulindac metabolites induce caspase- and proteasome-dependent degradation of beta-catenin protein in human colon cancer cells. Mol Cancer Ther. 2003 Sep;2(9):885-92. PubMed PMID: 14555707.
Lim JT, Piazza GA, Pamukcu R, Thompson WJ, Weinstein IB. Exisulind and related compounds inhibit expression and function of the androgen receptor in human prostate cancer cells. Clin Cancer Res. 2003 Oct 15;9(13):4972-82. PubMed PMID: 14581372.
Thompson IM, Albanes D, Basler JW, Crawford ED, Denis LJ, Djavan B, Fleshner N, Johnson-Pais TL, Klein EA, Kristal AR, Lucia MS, Parnes HL, Piazza GA, Platz EA, Pollock BH, Price DK, Reichardt JK, Tangen CM, Tolcher AW, McMann MC. First International Conference on Chemoprevention of Prostate Cancer. Overview consensus statement. J Urol. 2004 Feb;171(2 Pt 2):S3-4. doi: 10.1097/01.ju.0000107100.06725.51. Review. PubMed PMID: 14713744.
Basler JW, Piazza GA. Nonsteroidal anti-inflammatory drugs and cyclooxygenase-2 selective inhibitors for prostate cancer chemoprevention. J Urol. 2004 Feb;171(2 Pt 2):S59-62; discussion S62-3. doi: 10.1097/01.ju.0000107839.06670.27. Review. PubMed PMID: 14713756.
Kim KP, Whitehead C, Piazza G, Wargovich MJ. Combinatorial chemoprevention: efficacy of lovostatin and exisulind on the formation and progression of aberrant crypt foci. Anticancer Res. 2004 May-Jun;24(3a):1805-11. PubMed PMID: 15274359.
Piazza G. Utilizing a new tool for drug discovery: Building a better toolbox for research by increasing the availability of molecular probes. Genetic Engineering News; 2005.
White E, Maddry J, Ananthan S, Piazza G. Southern Research Molecular Libraries Screening Center. Screening; 2008.
Jia L, Noker PE, Piazza GA, Leuschner C, Hansel W, Gorman GS, Coward LU, Tomaszewski J. Pharmacokinetics and pharmacodynamics of Phor21-betaCG(ala), a lytic peptide conjugate. J Pharm Pharmacol. 2008 Nov;60(11):1441-8. doi: 10.1211/jpp.60.11.0004. PubMed PMID: 18957164; PubMed Central PMCID: PMC2825277.
Lu W, Tinsley HN, Keeton A, Qu Z, Piazza GA, Li Y. Suppression of Wnt/beta-catenin signaling inhibits prostate cancer cell proliferation. Eur J Pharmacol. 2009 Jan 5;602(1):8-14. doi: 10.1016/j.ejphar.2008.10.053. Epub 2008 Nov 9. PubMed PMID: 19026633; PubMed Central PMCID: PMC2637082.
Piazza GA, Keeton AB, Tinsley HN, Gary BD, Whitt JD, Mathew B, Thaiparambil J, Coward L, Gorman G, Li Y, Sani B, Hobrath JV, Maxuitenko YY, Reynolds RC. A novel sulindac derivative that does not inhibit cyclooxygenases but potently inhibits colon tumor cell growth and induces apoptosis with antitumor activity. Cancer Prev Res (Phila). 2009 Jun;2(6):572-80. doi: 10.1158/1940-6207.CAPR-09-0001. Epub 2009 May 26. PubMed PMID: 19470791; PubMed Central PMCID: PMC3227417.
Abadi AH, Ibrahim TM, Abouzid KM, Lehmann J, Tinsley HN, Gary BD, Piazza GA. Design, synthesis and biological evaluation of novel pyridine derivatives as anticancer agents and phosphodiesterase 3 inhibitors. Bioorg Med Chem. 2009 Aug 15;17(16):5974-82. doi: 10.1016/j.bmc.2009.06.063. Epub 2009 Jul 3. PubMed PMID: 19628397; PubMed Central PMCID: PMC4980832.
Abadi AH, Abouel-Ella DA, Lehmann J, Tinsley HN, Gary BD, Piazza GA, Abdel-Fattah MA. Discovery of colon tumor cell growth inhibitory agents through a combinatorial approach. Eur J Med Chem. 2010 Jan;45(1):90-7. doi: 10.1016/j.ejmech.2009.09.029. Epub 2009 Sep 20. PubMed PMID: 19836860; PubMed Central PMCID: PMC4980843.
Tinsley HN, Gary BD, Keeton AB, Zhang W, Abadi AH, Reynolds RC, Piazza GA. Sulindac sulfide selectively inhibits growth and induces apoptosis of human breast tumor cells by phosphodiesterase 5 inhibition, elevation of cyclic GMP, and activation of protein kinase G. Mol Cancer Ther. 2009 Dec;8(12):3331-40. doi: 10.1158/1535-7163.MCT-09-0758. PubMed PMID: 19996273; PubMed Central PMCID: PMC2805153.
Abadi AH, Abouel-Ella DA, Ahmed NS, Gary BD, Thaiparambil JT, Tinsley HN, Keeton AB, Piazza GA. Synthesis of novel tadalafil analogues and their evaluation as phosphodiesterase inhibitors and anticancer agents. Arzneimittelforschung. 2009;59(8):415-21. doi: 10.1055/s-0031-1296417. PubMed PMID: 19813465; PubMed Central PMCID: PMC4980831.
Abadi AH, Gary BD, Tinsley HN, Piazza GA, Abdel-Halim M. Synthesis, molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors, new stereochemical perspective. Eur J Med Chem. 2010 Apr;45(4):1278-86. doi: 10.1016/j.ejmech.2009.10.046. PubMed PMID: 20206015; PubMed Central PMCID: PMC4980838.
Piazza GA, Keeton AB, Tinsley HN, Whitt JD, Gary BD, Mathew B, Singh R, Grizzle WE, Reynolds RC. NSAIDs: Old Drugs Reveal New Anticancer Targets. Pharmaceuticals (Basel). 2010 May 25;3(5):1652-1667. doi: 10.3390/ph3051652. Review. PubMed PMID: 27713322; PubMed Central PMCID: PMC4034002.
Zhang L, Nebane NM, Wennerberg K, Li Y, Neubauer V, Hobrath JV, McKellip S, Rasmussen L, Shindo N, Sosa M, Maddry JA, Ananthan S, Piazza GA, White EL, Harsay E. A high-throughput screen for chemical inhibitors of exocytic transport in yeast. Chembiochem. 2010 Jun 14;11(9):1291-301. doi: 10.1002/cbic.200900681. PubMed PMID: 20461743; PubMed Central PMCID: PMC3090732.
Zhang Y, Zhang J, Wang L, Quealy E, Gary BD, Reynolds RC, Piazza GA, Lü J. A novel sulindac derivative lacking cyclooxygenase-inhibitory activities suppresses carcinogenesis in the transgenic adenocarcinoma of mouse prostate model. Cancer Prev Res (Phila). 2010 Jul;3(7):885-95. doi: 10.1158/1940-6207.CAPR-09-0273. Epub 2010 Jun 29. PubMed PMID: 20587701; PubMed Central PMCID: PMC4990820.
Tinsley HN, Gary BD, Thaiparambil J, Li N, Lu W, Li Y, Maxuitenko YY, Keeton AB, Piazza GA. Colon tumor cell growth-inhibitory activity of sulindac sulfide and other nonsteroidal anti-inflammatory drugs is associated with phosphodiesterase 5 inhibition. Cancer Prev Res (Phila). 2010 Oct;3(10):1303-13. doi: 10.1158/1940-6207.CAPR-10-0030. Epub 2010 Sep 28. PubMed PMID: 20876730; PubMed Central PMCID: PMC2955813.
Ahmed NS, Gary BD, Piazza GA, Tinsley HN, Laufer S, Abadi AH. A novel access to arylated and heteroarylated beta-carboline based PDE5 inhibitors. Med Chem. 2010 Nov;6(6):374-87. doi: 10.2174/157340610793563992. PubMed PMID: 21054274; PubMed Central PMCID: PMC4980833.
Ahmed NS, Gary BD, Tinsley HN, Piazza GA, Laufer S, Abadi AH. Design, synthesis and structure-activity relationship of functionalized tetrahydro-β-carboline derivatives as novel PDE5 inhibitors. Arch Pharm (Weinheim). 2011 Mar;344(3):149-57. doi: 10.1002/ardp.201000236. Epub 2010 Dec 22. PubMed PMID: 21384413; PubMed Central PMCID: PMC4980839.
What would you like to do?