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Bruce Ruggeri
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Journal Articles

Abstract 5973: The brain penetrant CDK4/6 Inhibitor, PRT3645, is highly effective in combination with other targeted therapies in preclinical models of NSCLC, CRC, and HER2-positive breast cancer

Yue Zou, Srijita Dhar, Kirsten Gallagher, Andrew Buesking, Sarah Pawley, Ryan Holmes, Xiaowei Wu, Katarina Rohlfing, Min Wang, Joseph Rager, Tom Emm, Stefan Ruepp, Miles Cowart, Jing Ni, Jean Zhao, Bruce Ruggeri, Andrew Combs, Kris Vaddi, Sandy Geeganage, Ashish Juvekar, Sang Hyun Lee, Peggy Scherle
Journal: Cancer Research
Cancer Res (2023) 83 (7_Supplement): 5973.
https://doi.org/10.1158/1538-7445.AM2023-5973
Published: 04 April 2023
View article titled, Abstract 5973: The brain penetrant CDK4/6 Inhibitor, PRT3645, is highly effective in combination with other targeted therapies in preclinical models of NSCLC, CRC, and HER2-positive breast cancer
Journal Articles

Abstract 4897: PRT543, a methyl transferase inhibitor, has potent anti-tumor activity against adenoid cystic carcinoma of salivary glands

Vasudha Mishra, Alka Singh, Xiangying Chen, Michael Korzinkin, Claudia Wing, Viktoria Sarkisova, Alexandra Ozerova, Oksana Glushchenko, Venkat Thodima, Koichi Ito, Peggy Scherle, Mark Lingen, Rifat Hasina, Alexander Pearson, Ari Rosenberg, Alex Zhavoronkov, Bruce Ruggeri, Nishant Agrawal, Evgeny Izumchenko
Journal: Cancer Research
Cancer Res (2023) 83 (7_Supplement): 4897.
https://doi.org/10.1158/1538-7445.AM2023-4897
Published: 04 April 2023
View article titled, Abstract 4897: PRT543, a methyl transferase inhibitor, has potent anti-tumor activity against adenoid cystic carcinoma of salivary glands
Journal Articles

Abstract 6277: Selective and orally bioavailable SMARCA2 targeted degraders induce synthetic lethality in SMARCA4- deficient solid tumor

Koichi Ito, Artem Shvartsbart, Joseph Rager, Anjana Agarwal, Michael Hulse, Komali Vykuntam, Min Wang, Justin Kurian, Miles Cowart, Joy Cote, Monisha Sivakumar, Jack Carter, Jessica Burtell, Alex Grego, Andrew Moore, Neha Bhagwat, Stefan Ruepp, Tom Emme, Liang Lu, Philip Pitis, Corey Basch, Klare Bersch, Song Mei, Raul Leal, John Rose, Danielle Roth, Ganfeng Cao, Kris Vaddi, Sandy Geeganage, Bruce Ruggeri, Andrew Combs, Peggy Scherle
Journal: Cancer Research
Cancer Res (2023) 83 (7_Supplement): 6277.
https://doi.org/10.1158/1538-7445.AM2023-6277
Published: 04 April 2023
View article titled, Abstract 6277: Selective and orally bioavailable SMARCA2 targeted degraders induce synthetic lethality in SMARCA4- deficient solid tumor
Journal Articles

Abstract 1132: Exploiting MGMT loss using a new class of DNA modifiers which selectively target tumor DNA and overcome therapy resistance mechanisms across multiple tumor types

Bruce Ruggeri, Kyle Tarantino, Ranjini Sundaram, Kingson Lin, Seth Herzon, Joseph Park, Spenser Johnson, Susan Gueble, Ranjit S. Bindra
Journal: Cancer Research
Cancer Res (2023) 83 (7_Supplement): 1132.
https://doi.org/10.1158/1538-7445.AM2023-1132
Published: 04 April 2023
View article titled, Abstract 1132: Exploiting MGMT loss using a new class of DNA modifiers which selectively target tumor DNA and overcome therapy resistance mechanisms across multiple tumor types
Journal Articles

Abstract 2159: PRMT5 inhibitor PRT543 displays potent antitumor activity in U2AF1S34F and RBM10LOF spliceosome-mutant non-small cell lung cancer in vitro and in vivo

Jack Carter, Koichi Ito, Venkat Thodima, Monisha Sivakumar, Michael Hulse, Joseph Rager, Komali Vykuntam, Neha Bhagwat, Kris Vaddi, Bruce Ruggeri, Peggy Scherle
Journal: Cancer Research
Cancer Res (2022) 82 (12_Supplement): 2159.
https://doi.org/10.1158/1538-7445.AM2022-2159
Published: 15 June 2022
View article titled, Abstract 2159: PRMT5 inhibitor PRT543 displays potent antitumor activity in U2AF1<sup>S34F</sup> and RBM10<sup>LOF</sup> spliceosome-mutant non-small cell lung cancer <em>in vitro</em> and <em>in vivo</em>
Journal Articles

Abstract 5471: PRT2527, a novel highly selective cyclin-dependent kinase 9 (CDK9) inhibitor, is active in preclinical models of prostate cancer

Elisa Federici, Gianluca Civenni, Aleksandra Kokanovic, Giada Sandrini, Luca Guarrera, Simone Mosole, Alessia Cacciatore, Valeria Uboldi, Manuel Lessi, Giovanni Papa, Domenico Albino, Elisa Storelli, Jessica Merulla, Andrea Rinaldi, Marco Bolis, Yang Zhang, Kris Vaddi, Peggy Scherle, Bruce Ruggeri, Giuseppina M. Carbone, Carlo V. Catapano
Journal: Cancer Research
Cancer Res (2022) 82 (12_Supplement): 5471.
https://doi.org/10.1158/1538-7445.AM2022-5471
Published: 15 June 2022
View article titled, Abstract 5471: PRT2527, a novel highly selective cyclin-dependent kinase 9 (CDK9) inhibitor, is active in preclinical models of prostate cancer
Journal Articles

Abstract 2300: Brain penetrant CDK4/6 inhibitor PRT3645 demonstrates anti-tumor activity and enhances survival in glioblastoma and breast cancer brain metastasis models

Ashish Juvekar, Yang Zhang, Andrew Buesking, Min Wang, Dave Rominger, Joseph Rager, Stefan Ruepp, Kirsten Gallagher, Yue Zou, Miles Cowart, Xiaowei Wu, Sarah Pawley, Ryan Holmes, William Gowen-MacDonald, Kris Vaddi, Andrew Combs, Bruce Ruggeri, Peggy Scherle
Journal: Cancer Research
Cancer Res (2022) 82 (12_Supplement): 2300.
https://doi.org/10.1158/1538-7445.AM2022-2300
Published: 15 June 2022
View article titled, Abstract 2300: Brain penetrant CDK4/6 inhibitor PRT3645 demonstrates anti-tumor activity and enhances survival in glioblastoma and breast cancer brain metastasis models
Journal Articles

Abstract 3263: Preclinical characterization of PRT3789, a potent and selective SMARCA2 targeted degrader

Michael Hulse, Anjana Agarwal, Min Wang, Jack Carter, Monisha Sivakumar, Brian Vidal, Justin Brown, Andrew Moore, Alexander Grego, Neha Bhagwat, Joseph Rager, Liang Lu, Corey Basch, Klare Bersch, Chaofeng Dai, Philip Pitis, Andrew Combs, Bruce Ruggeri, Kris Vaddi, Peggy Scherle, Koichi Ito
Journal: Cancer Research
Cancer Res (2022) 82 (12_Supplement): 3263.
https://doi.org/10.1158/1538-7445.AM2022-3263
Published: 15 June 2022
View article titled, Abstract 3263: Preclinical characterization of PRT3789, a potent and selective SMARCA2 targeted degrader
Journal Articles

Abstract 420: Combination of the MCL1 inhibitor PRT1419 and SMARCA2 degrader PRT3789 shows combinatorial benefit in SMARCA4 deleted lung cancer

Norman Fultang, Neha Bhagwat, Diane Heiser, Alexander Grego, Michael Hulse, Venkat Thodima, Koichi Ito, Kris Vaddi, Bruce Ruggeri, Peggy Scherle
Journal: Cancer Research
Cancer Res (2022) 82 (12_Supplement): 420.
https://doi.org/10.1158/1538-7445.AM2022-420
Published: 15 June 2022
View article titled, Abstract 420: Combination of the MCL1 inhibitor PRT1419 and SMARCA2 degrader PRT3789 shows combinatorial benefit in SMARCA4 deleted lung cancer
Journal Articles

Abstract 983: Preclinical characterization of PRT1419, a potent, selective and orally available inhibitor of MCL1

Neha Bhagwat, Alexander Grego, William Gowen-MacDonald, Min Wang, Miles Cowart, Xiaowei Wu, Jincong Zhuo, Andrew Combs, Bruce Ruggeri, Peggy Scherle, Kris Vaddi
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 983.
https://doi.org/10.1158/1538-7445.AM2021-983
Published: 01 July 2021
View article titled, Abstract 983: Preclinical characterization of PRT1419, a potent, selective and orally available inhibitor of MCL1
Journal Articles

Abstract 1137: PRMT5 inhibition regulates alternative splicing and DNA damage repair pathways in SF3B1 R625G expressing uveal melanoma cells

Koichi Ito, Venkat Thodima, Jack Carter, Neha Bhagwat, Monisha Sivakumar, Alexander Grego, Joseph Rager, Mizue Terai, Takami Sato, Omar Abdel-Wahab, Bruce Ruggeri, Peggy Scherle, Kris Vaddi
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 1137.
https://doi.org/10.1158/1538-7445.AM2021-1137
Published: 01 July 2021
View article titled, Abstract 1137: PRMT5 inhibition regulates alternative splicing and DNA damage repair pathways in SF3B1 R625G expressing uveal melanoma cells
Journal Articles

Abstract 1139: Potent SMARCA2 targeted degraders induce genetic synthetic lethality in SMARCA4 deleted cancer

Koichi Ito, Anjana Agarwal, Philip Pitis, Min Wang, Jack Carter, Miles Cowart, Chaofeng Dai, William Gowen-MacDonald, Eliza Elliot, Brian Vidal, Jacob Spruance, Hsin-Yao Tang, Bruce Ruggeri, Liang Lu, Andrew Combs, Hong Lin, Peggy Scherle, Kris Vaddi
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 1139.
https://doi.org/10.1158/1538-7445.AM2021-1139
Published: 01 July 2021
View article titled, Abstract 1139: Potent SMARCA2 targeted degraders induce genetic synthetic lethality in SMARCA4 deleted cancer
Journal Articles

Abstract 1138: PRMT5 inhibition downregulates MYB and NOTCH1 signaling, key molecular drivers of adenoid cystic carcinoma

Jack Carter, Koichi Ito, Venkat Thodima, Neha Bhagwat, Joseph Rager, Nicole Spardy Burr, Jeffrey Kaufman, Bruce Ruggeri, Peggy Scherle, Kris Vaddi
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 1138.
https://doi.org/10.1158/1538-7445.AM2021-1138
Published: 01 July 2021
View article titled, Abstract 1138: PRMT5 inhibition downregulates MYB and NOTCH1 signaling, key molecular drivers of adenoid cystic carcinoma
Journal Articles

Abstract 1185: PRMT5 inhibition epigenetically regulates DNA damage response pathways in cancer cells and sensitizes to chemotherapy and PARP inhibition

Koichi Ito, Jack Carter, Venkat Thodima, Youyou Zhang, Monisha Sivakumar, Mu Xu, Neha Bhagwat, Joseph Rager, Jacob Spruance, Lin Zhang, Bruce Ruggeri, Peggy Scherle, Kris Vaddi
Journal: Cancer Research
Cancer Res (2021) 81 (13_Supplement): 1185.
https://doi.org/10.1158/1538-7445.AM2021-1185
Published: 01 July 2021
View article titled, Abstract 1185: PRMT5 inhibition epigenetically regulates DNA damage response pathways in cancer cells and sensitizes to chemotherapy and PARP inhibition
Journal Articles

Abstract 2915: Preclinical characterization of PRT543, a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5), with broad antitumor activity in in vitro and in vivo models

Neha Bhagwat, Yang Zhang, Hong Lin, Min Wang, Dave Rominger, Tom Emm, Divya Chugani-Mahtani, Dimitrios Angelis, Rupa Shetty, Raul Leal, William Gowen-MacDonald, Alexander Grego, Juan Luengo, Taghi Manshouri, Friederike Pastore, Ross L. Levine, Srdan Verstovsek, Bruce Ruggeri, Peggy Scherle, Kris Vaddi
Journal: Cancer Research
Cancer Res (2020) 80 (16_Supplement): 2915.
https://doi.org/10.1158/1538-7445.AM2020-2915
Published: 15 August 2020
View article titled, Abstract 2915: Preclinical characterization of PRT543, a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5), with broad antitumor activity in <em>in vitro</em> and <em>in vivo</em> models
Journal Articles

Abstract 2919: Discovery of PRT811, a potent, selective, and orally bioavailable brain penetrant PRMT5 Inhibitor for the treatment of brain tumors

Yang Zhang, Hong Lin, Min Wang, Dimitrios Angelis, Michael Hawkins, Dave Rominger, Tom Emm, Juan Luengo, Bruce Ruggeri, Peggy Scherle, Kris Vaddi
Journal: Cancer Research
Cancer Res (2020) 80 (16_Supplement): 2919.
https://doi.org/10.1158/1538-7445.AM2020-2919
Published: 15 August 2020
View article titled, Abstract 2919: Discovery of PRT811, a potent, selective, and orally bioavailable brain penetrant PRMT5 Inhibitor for the treatment of brain tumors
Journal Articles

Abstract 3710: Establishment of a patient-derived acute myeloid leukemia (AML) ex vivo platform for evaluation of novel therapeutic agents

Bhavna Verma, Swetha Tati, Bruce Ruggeri, Amy Wesa
Journal: Cancer Research
Cancer Res (2019) 79 (13_Supplement): 3710.
https://doi.org/10.1158/1538-7445.AM2019-3710
Published: 01 July 2019
View article titled, Abstract 3710: Establishment of a patient-derived acute myeloid leukemia (AML) <em>ex vivo</em> platform for evaluation of novel therapeutic agents
Journal Articles

Abstract 1888: The FAD-directed LSD1 specific inhibitor, INCB059872, is a promising epigenetic agent for AML therapy by inducing differentiation of leukemic stem/progenitor cells

Antony Chadderton, Min Ye, Melody Diamond, Valerie Roman, Michael Weber, Chunhong He, Liangxing Wu, Swamy Yeleswaram, Alan Roberts, Wenqing Yao, Gregory Hollis, Reid Huber, Peggy Scherle, Bruce Ruggeri, Sang Hyun Lee
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 1888.
https://doi.org/10.1158/1538-7445.AM2018-1888
Published: 01 July 2018
View article titled, Abstract 1888: The FAD-directed LSD1 specific inhibitor, INCB059872, is a promising epigenetic agent for AML therapy by inducing differentiation of leukemic stem/progenitor cells
Journal Articles

Abstract 1876: INCB052793, a JAK1 selective inhibitor, is highly efficacious in PDX and xenograft models of acute myeloid leukemia (AML) expressing elevated endogenous pSTAT3/pSTAT5

Ashish Juvekar, Sindy Condon, Xiaoming Wen, Bruce Ruggeri, Peggy Scherle, Reid Huber, Yunlong Li, Wenqing Yao, Song Mei, Deepak Bhasin, Maria Mancini
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 1876.
https://doi.org/10.1158/1538-7445.AM2018-1876
Published: 01 July 2018
View article titled, Abstract 1876: INCB052793, a JAK1 selective inhibitor, is highly efficacious in PDX and xenograft models of acute myeloid leukemia (AML) expressing elevated endogenous pSTAT3/pSTAT5
Journal Articles

Abstract 1893: The evaluation of INCB059872, an FAD-directed inhibitor of LSD1, in preclinical models of T-ALL

Melody Diamond, Yvonne Lo, Antony Chadderton, Min Ye, Valerie Roman, Michael Weber, Chunhong He, Liangxing Wu, Swamy Yeleswaram, Alan Roberts, Wenqing Yao, Gregory Hollis, Reid Huber, Peggy Scherle, Bruce Ruggeri, Sang Hyun Lee
Journal: Cancer Research
Cancer Res (2018) 78 (13_Supplement): 1893.
https://doi.org/10.1158/1538-7445.AM2018-1893
Published: 01 July 2018
View article titled, Abstract 1893: The evaluation of INCB059872, an FAD-directed inhibitor of LSD1, in preclinical models of T-ALL