title: CG100649, a novel COX-2 inhibitor, inhibits colorectal adenoma and carcinoma growth in mouse models.
abstract: Nonsteroidal anti-inflammatory drugs (NSAIDs) and selective cyclooxygenase-2 (COX-2) inhibitors (COXIBs) can reduce the risk of developing colorectal cancer (CRC) and are being considered for use as adjuvant therapy for treatment of CRC patients. However, long-term use of most NSAIDs, except aspirin, increases cardiovascular risk, hampering use of these drugs in CRC prevention and possibly for treatment. CG100649 is a new member of the COXIB family, which is proposed to inhibit both COX-2 and carbonic anhydrase-I/-II (CA-I/-II) activity. Using mouse models, we show here that CG100649 inhibits premalignant and malignant colorectal lesions in mouse models, partly through inhibiting tumor cell proliferation. These pre-clinical findings suggest a need for further exploration of CG100649 for CRC prevention and treatment. The long-term safety profile of CG100649, particularly regarding its effect on cardiovascular risk, is yet to be determined.
authors.affiliation: Arizona State University Biodesign Institute, Tempe, Arizona (O.M., D.W., R.N.D); Departments of Cancer Biology (S.H.K, H.W., D.X., V.R.H), and General Oncology (P.Y.), The University of Texas MD Anderson Cancer Center, Houston, Texas.
authors.forename: Sun-Hee
authors.initials: SH
authors.lastname: Kim
authors.affiliation: Arizona State University Biodesign Institute, Tempe, Arizona (O.M., D.W., R.N.D); Departments of Cancer Biology (S.H.K, H.W., D.X., V.R.H), and General Oncology (P.Y.), The University of Texas MD Anderson Cancer Center, Houston, Texas.
authors.forename: Ofer
authors.initials: O
authors.lastname: Margalit
authors.affiliation: Arizona State University Biodesign Institute, Tempe, Arizona (O.M., D.W., R.N.D); Departments of Cancer Biology (S.H.K, H.W., D.X., V.R.H), and General Oncology (P.Y.), The University of Texas MD Anderson Cancer Center, Houston, Texas.
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Katoh
authors.affiliation: Arizona State University Biodesign Institute, Tempe, Arizona (O.M., D.W., R.N.D); Departments of Cancer Biology (S.H.K, H.W., D.X., V.R.H), and General Oncology (P.Y.), The University of Texas MD Anderson Cancer Center, Houston, Texas.
authors.forename: Dingzhi
authors.initials: D
authors.lastname: Wang
authors.affiliation: Arizona State University Biodesign Institute, Tempe, Arizona (O.M., D.W., R.N.D); Departments of Cancer Biology (S.H.K, H.W., D.X., V.R.H), and General Oncology (P.Y.), The University of Texas MD Anderson Cancer Center, Houston, Texas.
authors.forename: Hong
authors.initials: H
authors.lastname: Wu
authors.affiliation: Arizona State University Biodesign Institute, Tempe, Arizona (O.M., D.W., R.N.D); Departments of Cancer Biology (S.H.K, H.W., D.X., V.R.H), and General Oncology (P.Y.), The University of Texas MD Anderson Cancer Center, Houston, Texas.
authors.forename: Dianren
authors.initials: D
authors.lastname: Xia
authors.affiliation: Arizona State University Biodesign Institute, Tempe, Arizona (O.M., D.W., R.N.D); Departments of Cancer Biology (S.H.K, H.W., D.X., V.R.H), and General Oncology (P.Y.), The University of Texas MD Anderson Cancer Center, Houston, Texas.
authors.forename: Vijaykumar R
authors.initials: VR
authors.lastname: Holla
authors.affiliation: Arizona State University Biodesign Institute, Tempe, Arizona (O.M., D.W., R.N.D); Departments of Cancer Biology (S.H.K, H.W., D.X., V.R.H), and General Oncology (P.Y.), The University of Texas MD Anderson Cancer Center, Houston, Texas.
authors.forename: Peiying
authors.initials: P
authors.lastname: Yang
authors.affiliation: Arizona State University Biodesign Institute, Tempe, Arizona (O.M., D.W., R.N.D); Departments of Cancer Biology (S.H.K, H.W., D.X., V.R.H), and General Oncology (P.Y.), The University of Texas MD Anderson Cancer Center, Houston, Texas.
authors.forename: Raymond N
authors.initials: RN
authors.lastname: DuBois
mesh_terms: D000236:Adenoma / Q000188:drug therapy*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D002277:Carcinoma / Q000188:drug therapy*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D015179:Colorectal Neoplasms / Q000188:drug therapy*; D052246:Cyclooxygenase 2 Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D015232:Dinoprostone / Q000378:metabolism; D005663:Furans / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D051379:Mice; D013449:Sulfonamides / Q000494:pharmacology / Q000627:therapeutic use*; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; C000599293:CG100649; D052246:Cyclooxygenase 2 Inhibitors; D005663:Furans; D013449:Sulfonamides; D015232:Dinoprostone
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