KSQ-4279, a first-in-class USP1 inhibitor shows strong combination activity in BRCA mutant cancers with intrinsic or acquired resistance to PARP inhibitors

被引：0

作者：

Cadzow, L. ^{[1
]}

Gokhale, P. C. ^{[2
]}

Ganapathy, S. ^{[2
]}

Sullivan, P. ^{[3
]}

Nayak, S. ^{[3
]}

Shenker, S. ^{[4
,5
]}

Schlabach, M.

Tobin, E. ^{[3
]}

Matulonis, U. A. ^{[6
]}

Liu, J. F. ^{[6
]}

Stegmeier, F. ^{[7
]}

Wylie, A. ^{[3
]}

机构：

[1] KSQ Therapeutics Inc, Pharmacol, Cambridge, MA USA

[2] Dana Farber Canc Inst, Belfer Ctr Appl Canc Sci, Boston, MA USA

[3] KSQ Therapeutics Inc, Oncol, Cambridge, MA USA

[4] KSQ Therapeutics Inc, Computat Biol, Cambridge, MA USA

[5] KSQ Therapeutics Inc, Target Discovery, Cambridge, MA USA

[6] Dana Farber Canc Inst, Dept Med Oncol, Boston, MA USA

[7] KSQ Therapeutics Inc, Res, Cambridge, MA USA

来源：

EUROPEAN JOURNAL OF CANCER | 2022年 / 174卷

关键词：

D O I：

暂无

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

105

引用

页码：S37 / S38

页数：2

共 12 条

[1] KSQ-4279, a first-in-class USP1 inhibitor shows strong combination activity with multiple PARP inhibitors in BRCA mutant cancers
Tobin, Erica
Sullivan, Pamela
Murray, Morgan
Gannon, Hugh
Dodson, Anne
Shenker, Sol
Stegmeier, Frank
Wylie, Andrew
Cadzow, Louise
CANCER RESEARCH, 2023, 83 (07)
[2] Development of KSQ-4279 as a first-in-class USP1 inhibitor for the treatment of BRCA-deficient cancers
Cadzow, L.
Brenneman, J.
Sullivan, P.
Liu, H.
Shenker, S.
McGuire, M.
Grasberger, P.
Sinkevicius, K.
Hafeez, N.
Histen, G.
Chipumuro, E.
Hixon, J.
Krall, E.
Cogan, S.
Wilt, J.
Schlabach, M.
Stegmeier, F.
Olaharski, A.
Wylie, A.
EUROPEAN JOURNAL OF CANCER, 2020, 138 : S52 - S52
[3] KSQ-4279: A first-in-class USP1 inhibitor for the treatment of cancers with homologous recombination deficiencies
Cadzow, Louise
Tobin, Erica
Sullivan, Pamela
Shenker, Sol
Nayak, Sumeet
Ali, Janid
Gannon, Hugh
Dodson, Anne
Grasberger, Paula
Carlson, Alyssa
McGuire, Michael
Brenneman, Jehrod
Liu, Hanlan
Olaharski, Andrew
Sinkevicius, Kerstin
Hixon, Jeff
Krall, Elsa
Schlabach, Mike
Goulet, Matt
Wilt, Jeremy
Harris, Patricia
Stegmeier, Frank
Wylie, Andrew
CANCER RESEARCH, 2022, 82 (12)
[4] The USP1 Inhibitor KSQ-4279 Overcomes PARP Inhibitor Resistance in Homologous Recombination-Deficient Tumors
Cadzow, Louise
Brenneman, Jehrod
Tobin, Erica
Sullivan, Pamela
Nayak, Sumeet
Ali, Janid A.
Shenker, Sol
Griffith, Jim
McGuire, Michael
Grasberger, Paula
Mishina, Yuji
Murray, Morgan
Dodson, Anne E.
Gannon, Hugh
Krall, Elsa
Hixon, Jeff
Chipumuro, Edmond
Sinkevicius, Kerstin
Gokhale, Prafulla C.
Ganapathy, Suthakar
Matulonis, Ursula A.
Liu, Joyce F.
Olaharski, Andrew
Sangurdekar, Dipen
Liu, Hanlan
Wilt, Jeremy
Schlabach, Michael
Stegmeier, Frank
Wylie, Andrew A.
CANCER RESEARCH, 2024, 84 (20) : 3419 - 3434
[5] Functional genomic characterization of the USP1 inhibitor KSQ-4279 reveals a distinct mechanism of action and resistance profile relative to other DDR targeting drugs.
Shenker, Sol
Gannon, Hugh
Carlson, Alyssa
Grasberger, Paula
Sullivan, Pamela
Middleton, Chris
Dodson, Anne
Bullock, Caroline
McGuire, Michael
Tobin, Erica
Sinkevicius, Kerstin
Schlabach, Mike
Stegmeier, Frank
Cadzow, Louise
Wylie, Andrew
CANCER RESEARCH, 2021, 81 (13)
[6] TNG348, a selective USP1 inhibitor, shows strong preclinical combination activity with PARP inhibitors and other agents targeting DNA repair
Simoneau, Antoine
Pratt, Charlotte
Corner, Grace
Wu, Hsin-Jung
Choi, Ashley
Khendu, Tenzing
Meier, Samuel
Yu, Yi
Liu, Shangtao
Zhang, Wenhai
Whittington, Douglas
Mallender, William
Sudsakorn, Sirimas
Chen, Yingnan
Haines, Brian
Throner, Scott
Crystal, Adam
Huang, Alan
Maxwell, John
Andersen, Jannik
MOLECULAR CANCER THERAPEUTICS, 2023, 22 (12)
[7] USP1 inhibitors show robust combination activity and a distinct resistance profile from PARP inhibitors
Sullivan, P.
Shenker, S.
McGuire, M.
Grasberger, P.
Sinkevicius, K.
Tobin, E.
Chipumuro, E.
Histen, G.
Hafeez, N.
Rahal, R.
Schlabach, M.
Stegmeier, F.
Cadzow, L.
Wylie, A.
EUROPEAN JOURNAL OF CANCER, 2020, 138 : S7 - S8
[8] Preclinical candidate LAE120, a novel selective USP1 inhibitor shows effective anticancer and combination activity with PARP inhibitor
Wang, Jintao
Chen, Yan
Chen, Junyan
Jiang, Ling
Lin, Xiaofen
Cai, Chaojun
Zhang, Minhua
Li, Ming
Gu, Justin
CANCER RESEARCH, 2024, 84 (06)
[9] First-in-human phase I trial of the oral first-in-class ubiquitin specific peptidase 1 (USP1) inhibitor KSQ-4279 (KSQi), given as single agent (SA) and in combination with olaparib (OLA) or carboplatin (CARBO) in patients (pts) with advanced solid tumors, enriched for deleterious homologous recombination repair (HRR) mutations.
Yap, Timothy A.
Lakhani, Nehal J.
Patnaik, Amita
Lee, Elizabeth Katherine
Gutierrez, Martin
Moore, Kathleen N.
Carneiro, Benedito A.
Hays, John L.
Huang, Marilyn
LoRusso, Patricia
Wylie, Andrew
Cadzow, Louise
Goulet, Matthew
Tobin, Erica
Krieter, Oliver
Schmid, Daniela
Blake, Sophia M.
Dieterich, Max
Jamois, Candice
Harris, Patricia M.
JOURNAL OF CLINICAL ONCOLOGY, 2024, 42 (16)
[10] The first-in-class ERK inhibitor ulixertinib (BVD-523) shows activity in MAPK-driven pediatric low-grade glioma models as single agent and in combination with MEK inhibitors or senolytics
Sigaud, Romain
Roesch, Lisa
Gatzweiler, Charlotte
Benzel, Julia
von Soosten, Laura
Peterziel, Heike
Najafi, Sara
Ayhan, Simay
Hofmann, Nina
Foerster, Kathrin I.
Burhenne, Juergen
Longuespee, Remi
van Tilburg, Cornelis M.
Jones, David T.
Pfister, Stefan M.
Knoerzer, Deborah
Kreider, Brent
Sauter, Max
Pajtler, Kristian W.
Zuckermann, Marc
Oehme, Ina
Witt, Olaf
Milde, Till
CANCER RESEARCH, 2022, 82 (12)

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