The CLK inhibitor SM08502 induces anti-tumor activity and reduces Wnt pathway gene expression in gastrointestinal cancer models
Tam, Betty Y., Chiu, Kevin, Chung, Heekyung, Bossard, Carine, Nguyen, John Duc, Creger, Emily, Eastman, Brian W., Mak, Chi Ching, Ibanez, Maureen, Ghias, Abdullah, Cahiwat, Joseph, Do, Long, Cho, Shawn, Nguyen, Jackie, Deshmukh, Vishal, Stewart, Josh, Chen, Chiao-Wen, Barroga, Charlene, Dellamary, Luis, KC, Sunil K., Phalen, Timothy J., Hood, John, Cha, Steven, Yazici, Yusuf
Published in Cancer letters (31.03.2020)
Published in Cancer letters (31.03.2020)
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Journal Article
Tricyclic Benzimidazoles as Potent Poly(ADP-ribose) Polymerase-1 Inhibitors
Skalitzky, Donald J, Marakovits, Joseph T, Maegley, Karen A, Ekker, Anne, Yu, Xiao-Hong, Hostomsky, Zdenek, Webber, Stephen E, Eastman, Brian W, Almassy, Robert, Li, Jianke, Curtin, Nicola J, Newell, David R, Calvert, A. Hilary, Griffin, Roger J, Golding, Bernard T
Published in Journal of medicinal chemistry (16.01.2003)
Published in Journal of medicinal chemistry (16.01.2003)
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Journal Article
Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors
White, Alex W., Curtin, Nicola J., Eastman, Brian W., Golding, Bernard T., Hostomsky, Zdenek, Kyle, Suzanne, Li, Jianke, Maegley, Karen A., Skalitzky, Donald J., Webber, Stephen E., Yu, Xiao-Hong, Griffin, Roger J.
Published in Bioorganic & medicinal chemistry letters (17.05.2004)
Published in Bioorganic & medicinal chemistry letters (17.05.2004)
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Journal Article
3-[3-Fluoro-5-(5-pyridin-2-yl-2 H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist
Poon, Steve F., Eastman, Brian W., Chapman, Deborah F., Chung, Janice, Cramer, Merryl, Holtz, Gregory, Cosford, Nicholas D.P., Smith, Nicholas D.
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
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Journal Article
Structure-Based Design of a Parallel Synthetic Array Directed Toward the Discovery of Irreversible Inhibitors of Human Rhinovirus 3C Protease
Johnson, Theodore O, Hua, Ye, Luu, Hiep T, Brown, Edward L, Chan, Fora, Chu, Shao Song, Dragovich, Peter S, Eastman, Brian W, Ferre, Rose Ann, Fuhrman, Shella A, Hendrickson, Thomas F, Maldonado, Fausto C, Matthews, David A, Meador, James W, Patick, Amy K, Reich, Siegfried H, Skalitzky, Donald J, Worland, Stephen T, Yang, Michelle, Zalman, Leora S
Published in Journal of medicinal chemistry (09.05.2002)
Published in Journal of medicinal chemistry (09.05.2002)
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Journal Article
The Pan-Clk/Dyrk Inhibitor Cirtuvivint (SM08502) Exposes Mechanistic Underpinnings of Alternative Splicing As a Therapeutic Vulnerability in Heme Malignancies
Bossard, Carine, McMillan, Elizabeth A., Creger, Emily, Eastman, Brian, Mak, Chi-Ching, Beaupre, Darrin M., White, Michael A.
Published in Blood (23.11.2021)
Published in Blood (23.11.2021)
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Abstract P250: Evaluation of systemic pan-CLK/DYRK inhibition on organ function and tissue self-renewal
Falahatpisheh, Hadi, Dehghani, Maryam, Morrow, Jane, Tsao, Catherine, Dorrow, Steven, Stewart, Josh, Bossard, Carine, Eastman, Brian, Mak, Chi-Ching, Pandher, Karamjeet, White, Michael A.
Published in Molecular cancer therapeutics (01.12.2021)
Published in Molecular cancer therapeutics (01.12.2021)
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Journal Article
Abstract P242: Preclinical efficacy landscape of the pan-CLK/DYRK inhibitor Cirtuvivint (SM08502)
Bossard, Carine, Creger, Emily, McMillan, Elizabeth A., Merkwirth, Carsten, Ibanez, Maureen, Bhat, Deepti, Stewart, Josh, Eastman, Brian, Mak, Chi-Ching, Deshmukh, Vishal, White, Michael A.
Published in Molecular cancer therapeutics (01.12.2021)
Published in Molecular cancer therapeutics (01.12.2021)
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Journal Article
Abstract C08: SM08502, a novel, small-molecule CDC-like kinase (CLK) inhibitor, demonstrates activity against cancer stem cell (CSC)-enriched pancreatic cancer cells and suppresses stemness in vitro
Bossard, Carine, Cruz, Nathalia, Eastman, Brian, Mak, Chi-Ching, KC, Sunil, Tam, Betty, Phalen, Timothy, Cha, Steven
Published in Cancer research (Chicago, Ill.) (15.12.2019)
Published in Cancer research (Chicago, Ill.) (15.12.2019)
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Journal Article
Abstract 6401: SM08502, a novel, small-molecule CDC-like kinase (CLK) inhibitor, demonstrates strong antitumor effects and Wnt and cyclin D-CDK4/6-RB pathway inhibition in hormone-receptor-positive (HR+) breast cancer models
Chung, Heekyung, Sitts, Lauren, Wu, Chu-Chiao, Eastman, Brian, Mak, Chi Ching, KC, Sunil, Stewart, Josh, Bossard, Carine, Phalen, Timothy J., Cha, Steven
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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Abstract 5691: SM08502, a novel, small-molecule CDC-like kinase (CLK) inhibitor, demonstrates strong antitumor effects and Wnt pathway inhibition in castration-resistant prostate cancer (CRPC) models
Bossard, Carine, Cruz, Nathalia, Chiu, Kevin, Eastman, Brian, Mak, Chi Ching, KC, Sunil, Bucci, Gail, Stewart, Josh, Phalen, Timothy J., Cha, Steven
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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Journal Article
Abstract A09: SM08502, a novel, small-molecule CDC-like kinase (CLK) inhibitor, demonstrates strong inhibition of the Wnt signaling pathway and antitumor effects in diverse ovarian cancer models
Chung, Heekyung, Sitts, Lauren, Creger, Emily, Liao, Erica, Eastman, Brian, Mak, Chi-Ching, Sunil, K.C., Tam, Betty, Bucci, Gail, Stewart, Josh, Bossard, Carine, Phalen, Timothy, Cha, Steven
Published in Clinical cancer research (01.07.2020)
Published in Clinical cancer research (01.07.2020)
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Journal Article
Abstract P3-13-01: SM08502, a novel, small-molecule CDC-like kinase (CLK) inhibitor, demonstrates strong inhibition of the Wnt signaling pathway and antitumor effects as monotherapy and in combination with chemotherapy in triple-negative breast cancer (TNBC) models
Chung, Heekyung, Sitts, Lauren, Creger, Emily, Nguyen, John Duc, Eastman, Brian, Mak, Chi-Ching, KC, Sunil, Tam, Betty, Bossard, Carine, Phalen, Timothy, Cha, Steven
Published in Cancer research (Chicago, Ill.) (15.02.2020)
Published in Cancer research (Chicago, Ill.) (15.02.2020)
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Abstract A02: SM08502, a novel, small-molecule CDC-like kinase (CLK) inhibitor, downregulates the Wnt signaling pathway and demonstrates antitumor activity in pancreatic cancer cell lines and in vivo xenograft models
Bossard, Carine, Cruz, Nathalia, Eastman, Brian, Mak, Chi-Ching, Sunil, K.C., Tam, Betty, Bucci, Gail, Stewart, Josh, Phalen, Timothy, Cha, Steven
Published in Cancer research (Chicago, Ill.) (15.12.2019)
Published in Cancer research (Chicago, Ill.) (15.12.2019)
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Abstract C09: Inhibition of tumor growth and post-treatment regrowth by SM08502, a novel, small-molecule CDC-like kinase (CLK) inhibitor, in combination with standard of care in pancreatic cancer models
Bossard, Carine, Astsaturov, Igor, Cruz, Nathalia, Eastman, Brian, Mak, Chi-Ching, Sunil, K.C., Tam, Betty, Bucci, Gail, Stewart, Josh, Phalen, Timothy, Cha, Steven
Published in Cancer research (Chicago, Ill.) (15.12.2019)
Published in Cancer research (Chicago, Ill.) (15.12.2019)
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Journal Article
Effects of SM08502, a novel, oral small-molecule inhibitor of Wnt pathway signaling, on gene expression and antitumor activity in colorectal cancer (CRC) models
Bossard, Carine, Chiu, Kevin, Chung, Heekyung, Nguyen, John Duc, Creger, Emily, Eastman, Brian, Mak, Chi Ching, Do, Long, Cho, Shawn, KC, Sunil, Phalen, Timothy, Tambiah, Jeyanesh, Cha, Steven
Published in Journal of clinical oncology (20.05.2019)
Published in Journal of clinical oncology (20.05.2019)
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Journal Article
Abstract 3928: The pan-CLK/DYRK inhibitor cirtuvivint selectively disrupts alternative splicing and has broad anti-tumor activity in preclinical models
McMillan, Elizabeth A., Bossard, Carine, Creger, Emily, Merkwirth, Carsten, Pippa, Raffaella, Jarvis, Matthew, Sriram, Krishna, Pedraza, Melinda, Ibanez, Maureen, Bhat, Deepti, Lai, Carolyn, Stewart, Josh, Eastman, Brian, Mak, Chi-Ching, White, Michael A., Beaupre, Darrin
Published in Cancer research (Chicago, Ill.) (15.06.2022)
Published in Cancer research (Chicago, Ill.) (15.06.2022)
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