Discovery of PF-06855800, a SAM competitive PRMT5 inhibitor with potent antitumor activity

被引：4

作者：

Mcalpine, Indrawan J. ^{[1
]}

Tatlock, John ^{[1
]}

Billitti, Joseph ^{[1
]}

Braganza, John ^{[1
]}

Brooun, Alexei ^{[1
]}

Deng Ya-Li ^{[1
]}

Hirakawa, Brad ^{[1
]}

Jensen-Pergakes, Kristen ^{[1
]}

Kumpf, Robert ^{[1
]}

Liu, Wei ^{[1
]}

Maegley, Karen ^{[1
]}

McTigue, Michele ^{[1
]}

Patman, Ryan ^{[1
]}

Rui, Eugene ^{[1
]}

Scales, Stephanie ^{[1
]}

Spiegel, Noah ^{[1
]}

Tran-Dube, Michelle ^{[1
]}

Wang, Fen ^{[1
]}

Wang, Zhenxiong ^{[1
]}

Yamazaki, Shinji ^{[1
]}

Zhang, Tao ^{[1
]}

Wythes, Martin ^{[1
]}

机构：

[1] Pfizer Global R&D, San Diego, CA USA

来源：

CANCER RESEARCH | 2018年 / 78卷 / 13期

关键词：

D O I：

10.1158/1538-7445.AM2018-4857

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

4857

引用

页数：2

共 50 条

[1] Discovery of SAM competitive, brain-restricted PRMT5 inhibitors with potent antitumor activity
Tatlock, John
Billitti, Joseph
Braganza, John
Brooun, Alexei
Deng, Ya-Li
Hirakawa, Brad
Jensen-Pergakes, Kristen
Kumpf, Robert
Liu, Wei
Maegley, Karen
McAlpine, Indrawan
McTigue, Michele
Patman, Ryan
Rui, Eugene
Scales, Stephanie
Tran-Dube, Michelle
Wang, Fen
Wang, Zhenxiong
Yamazaki, Shinji
Zhang, Tao
Wythes, Martin
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2018, 255
[2] Discovery of SAM competitive and non-nucleoside derivative PRMT5 inhibitors with potent antitumor activity
Yang, Xiaozhi
Zhou, Wei
Li, Chenglong
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2019, 257
[3] SAM competitive PRMT5 inhibitor PF06939999 demonstrates antitumor activity in splicing dysregulated NSCLC with decreased liability of drug resistance.
Jensen-Pergakes, Kristen
Tatlock, John
Maegley, Karen
McAlpine, Indrawan
McTigue, Michele
Xie, Tao
Dillon, Christopher
Wang, Yuli
Yamazaki, Shinji
Spiegel, Noah
Shi, Manli
Nemeth, Amy
Miller, Natalie
Hendrickson, Eleanore
Lam, Hieu
Sherrill, John
Liu, Wei
Deng, Ya-Li
Chung, Chi-Yeh
McMillan, Elizabeth A.
Palde, Prakash
Brooun, Alexei
Braganza, John
Kephart, Susan E.
Kumpf, Robert
Patman, Ryan
Rui, Eugene
Scales, Stephanie
Tran-Dube, Michelle
Wang, Fen
Wythes, Martin
Paul, Thomas
[J]. CANCER RESEARCH, 2021, 81 (13)
[4] SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance
Jensen-Pergakes, Kristen
Tatlock, John
Maegley, Karen A.
McAlpine, Indrawan J.
McTigue, Michele
Xie, Tao
Dillon, Christopher P.
Wang, Yuli
Yamazaki, Shinji
Spiegel, Noah
Shi, Manli
Nemeth, Amy
Miller, Natalie
Hendrickson, Eleanore
Hieu Lam
Sherrill, John
Chung, Chi-Yeh
McMillan, Elizabeth A.
Bryant, Shannon Karlicek
Palde, Prakash
Braganza, John
Brooun, Alexei
Deng, Ya-Li
Goshtasbi, Vesta
Kephart, Susan E.
Kumpf, Robert A.
Liu, Wei
Patman, Ryan L.
Rui, Eugene
Scales, Stephanie
Tran-Dube, Michelle
Wang, Fen
Wythes, Martin
Paul, Thomas A.
[J]. MOLECULAR CANCER THERAPEUTICS, 2022, 21 (01) : 3 - 15
[5] The discovery and preclinical characterization of the SAM-competitive PRMT5 inhibitor UCT-000445
McDermott, Martina S.
O'Brien, Neil A.
O'Boyle, Brendan
Bartberger, Michael
Loson, Oliver C.
Chau, Kevin
Schwab, Ella
Hong, Jenny
Zhou, Jiaying
Hu, Chuhong
Luo, Tong
Ayala, Raul
Glasby, John
Stoltz, Brian M.
Slamon, Dennis J.
[J]. CANCER RESEARCH, 2023, 83 (07)
[6] LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity
Bonday, Zahid Q.
Cortez, Guillermo S.
Grogan, Michael J.
Antonysamy, Stephen
Weichert, Ken
Bocchinfuso, Wayne P.
Li, Fengling
Kennedy, Steven
Li, Binghui
Mader, Mary M.
Arrowsmith, Cheryl H.
Brown, Peter J.
Eram, Mohammad S.
Szewczyk, Magdalena M.
Barsyte-Lovejoy, Dalia
Vedadi, Masoud
Guccione, Ernesto
Campbell, Robert M.
[J]. ACS MEDICINAL CHEMISTRY LETTERS, 2018, 9 (07): : 612 - 617
[7] Discovery and Pharmacological Characterization of JNJ-64619178, a Novel Small-Molecule Inhibitor of PRMT5 with Potent Antitumor Activity
Brehmer, Dirk
Beke, Lijs
Wu, Tongfei
Millar, Hillary J.
Moy, Christopher
Sun, Weimei
Mannens, Geert
Pande, Vineet
Boeckx, An
van Heerde, Erika
Nys, Thomas
Gustin, Emmanuel M.
Verbist, Bie
Zhou, Longen
Fan, Yue
Bhargava, Vipul
Safabakhsh, Pegah
Vinken, Petra
Verhulst, Tinne
Gilbert, Angelique
Rai, Sumit
Graubert, Timothy A.
Pastore, Friederike
Fiore, Danilo
Gu, Junchen
Johnson, Amy
Philippar, Ulrike
Morschhauser, Barbara
Walker, David
De Lange, Desiree
Keersmaekers, Vikki
Viellevoye, Marcel
Diels, Gaston
Schepens, Wim
Thuring, Jan Willem
Meerpoel, Lieven
Packman, Kathryn
Lorenzi, Matthew V.
Laquerre, Sylvie
[J]. MOLECULAR CANCER THERAPEUTICS, 2021, 20 (12) : 2317 - 2328
[8] AGX323-A SAM-competitive, orally available inhibitor of protein arginine methyltransferase 5 (PRMT5) with potent cellular antiproliferative and in vivo antitumor activity against selected solid cancer types.
Lee, Francis Y. F.
Wu, Wen-Lian
Yang, Zhiqiang
Tan, John
[J]. CANCER RESEARCH, 2021, 81 (13)
[9] A novel MTA non-competitive PRMT5 inhibitor.
Malik, Rohit
Park, Peter K.
Barbieri, Christopher M.
Blat, Yuval
Sheriff, Steven
Weigelt, Carolyn A.
Kopcho, Lisa M.
Celiktas, Muge
Ruzanov, Max
Naglich, Joseph G.
Price, Jennifer L.
Harner, Mary
Omalley, Kevin M.
Deng, Jingjing
Schmitz, William
Li, Guo
Ruan, Zheming
Qin, Lan-ying
Duke, Gerald J.
Rodrigo, Iyoncy
Witmer, Mark R.
Harden, David G.
Demes, Shilpa
Arey, Brian J.
Soars, Matt
Fink, Brian E.
Gavai, Ashvinikumar V.
Vite, Gregory D.
Voliva, Charles F.
[J]. CANCER RESEARCH, 2021, 81 (13)
[10] A novel PRMT5 inhibitor with potent in vitro and in vivo activity in preclinical lung cancer models
Brehmer, Dirk
Wu, Tongfei
Mannens, Geert
Beke, Lijs
Vinken, Petra
Gaffney, Dana
Sun, Weimei
Pande, Vineet
Thuring, Jan-Willem
Millar, Hillary
Poggesi, Italo
Somers, Ivan
Boeckx, An
Parade, Marc
van Heerde, Erika
Nys, Thomas
Yanovich, Carol
Herkert, Barbara
Verhulst, Tinne
Du Jardin, Marc
Meerpoel, Lieven
Moy, Christopher
Diels, Gaston
Viellevoye, Marcel
Schepens, Wim
Poncelet, Alain
Linders, Joannes T.
Lawson, Edward C.
Edwards, James P.
Chetty, Dushen
Laquerre, Sylvie
Lorenzi, Matthew V.
[J]. CANCER RESEARCH, 2017, 77

← 1 2 3 4 5 →