Identification of TRE-130 as Reversible Inhibitor of Pan-EGFR Mutants while Sparing EGFR Wild-Type Activity

被引：2

作者：

Duggirala, Krishna Babu ^{[1
,2
]}

Choe, Hyeonjeong ^{[1
]}

Jeon, Byeong Uk ^{[1
]}

Jung, Myoung Eun ^{[1
]}

Go, Areum ^{[1
]}

Lim, Byungho ^{[1
]}

Park, Chaewon ^{[3
]}

Yoon, Jiyeun ^{[3
]}

Chae, Chong Hak ^{[1
]}

Cho, Byoung Chul ^{[3
]}

Choi, Gildon ^{[1
,2
]}

Lee, Kwangho ^{[1
,2
]}

机构：

[1] Korea Res Inst Chem Technol, Bio & Drug Discovery Div, Daejeon 34114, South Korea

[2] Univ Sci & Technol, Med Chem & Pharmacol, Daejeon 34113, South Korea

[3] Yonsei Univ, Coll Med, Yonsei Canc Ctr, Seoul 03722, South Korea

来源：

BULLETIN OF THE KOREAN CHEMICAL SOCIETY | 2019年 / 40卷 / 12期

关键词：

EGFR T790M/C797S; Kinases; NSCLC; Diaminopyrimidines; Sulfonylurea; LUNG-CANCER; RESISTANCE; MUTATIONS; AZD9291; POTENT;

D O I：

10.1002/bkcs.11886

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

[No abstract available]

引用

页码：1222 / 1225

页数：4

共 50 条

[1] Furmonertinib is an Oral, Irreversible, Highly BrainPenetrant Pan-EGFR Inhibitor with Activity Against Classical and Atypical EGFR Mutations
Musib, L.
Kowanetz, M.
Li, Q.
Luo, H.
Hu, J.
Lutzker, S.
JOURNAL OF THORACIC ONCOLOGY, 2023, 18 (03) : E14 - E15
[2] LNG-451 is a potent, CNS-penetrant, wild-type EGFR sparing inhibitor of EGFR exon 20 insertion mutations
Murray, Brion W.
Pandey, Anjali
Roth, Bruce
Saxton, Tracy
Estes, Daniel J.
Agrawal, Himanshu
Vishwakarma, Santosh
Hallur, Gurulingappa
Ahmad, Ishtiyaque
Trivedi, Ravi
Jenkins, Helen
Pearson, Paul G.
CANCER RESEARCH, 2022, 82 (12)
[3] A novel multi-target inhibitor harboring selectivity of inhibiting EGFR T790M sparing wild-type EGFR
Song, Xiaoping
Qi, Xin
Wang, Qiang
Zhu, Weiming
Li, Jing
AMERICAN JOURNAL OF CANCER RESEARCH, 2017, 7 (09): : 1884 - 1898
[4] Restoration of EGFR-TKI resistance by endocytosis inhibitor PAO in lung cancer with wild-type EGFR
Kim, Boyeon
Sung, Jae Sook
Kim, Yeul Hong
CANCER RESEARCH, 2016, 76
[5] Discovery of Novel EGFR Inhibitor Targeting Wild-Type and Mutant Forms of EGFR: In Silico and In Vitro Study
Todsaporn, Duangjai
Zubenko, Alexander
Kartsev, Victor
Aiebchun, Thitinan
Mahalapbutr, Panupong
Petrou, Anthi
Geronikaki, Athina
Divaeva, Liudmila
Chekrisheva, Victoria
Yildiz, Ilkay
Choowongkomon, Kiattawee
Rungrotmongkol, Thanyada
MOLECULES, 2023, 28 (07):
[6] EGFR tyrosine kinase inhibitor in advanced non-small cell lung cancer with wild-type EGFR
Wang, Z.
Wu, Y. L.
Yang, J.
Wang, B.
Huang, Y.
Zhou, Q.
Xu, C.
JOURNAL OF CLINICAL ONCOLOGY, 2011, 29 (15)
[7] In Vitro and In Vivo Characterization of Irreversible Mutant-Selective EGFR Inhibitors That Are Wild-Type Sparing
Sjin, Robert Tjin Tham
Lee, Kwangho
Walter, Annette O.
Dubrovskiy, Aleksandr
Sheets, Michael
St Martin, Thia
Labenski, Matthew T.
Zhu, Zhendong
Tester, Richland
Karp, Russell
Medikonda, Aravind
Chaturvedi, Prasoon
Ren, Yixuan
Haringsma, Henry
Etter, Jeff
Raponi, Mitch
Simmons, Andrew D.
Harding, Thomas C.
Niu, Deqiang
Nacht, Mariana
Westlin, William F.
Petter, Russell C.
Allen, Andrew
Singh, Juswinder
MOLECULAR CANCER THERAPEUTICS, 2014, 13 (06) : 1468 - 1479
[8] From HTS lead to clinic: Discovery of PF-06747775. A high affinity irreversible inhibitor targeting oncogenic EGFR mutants with selectivity over wild-type EGFR
Planken, Simon
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2018, 256
[9] Pan-HER inhibition in EGFR wild-type non-small-cell lung cancer
Peters, Solange
Smit, Egbert
LANCET ONCOLOGY, 2014, 15 (12): : 1289 - 1290
[10] Characterization of a novel irreversible third generation EGFR TKI that targets T790M-mediated resistant EGFR-mutant NSCLC while sparing wild type EGFR
Zientek, Mike
Baxi, Sangita
Cheng, Henry
Fantin, Valeria
Feng, Jun Li
Given, Allison
Goldberg, Zelanna
Guo, Jie
Hemkens, Michelle
Kath, John
Lafontaine, Jennifer
Li, Gary
Mehta, Pramod
Murray, Brion
Nair, Sajiv
Planken, Simon
Ray, Chad
Wang, Yuli
Shi, Manli
Sistla, Anand
Smeal, Tod
Stevens, Greg
Tan, Wei
Vicini, Paolo
Walls, Marlena
Yang, Liu
Yin, Min-Jean
Weinrich, Scott L.
CANCER RESEARCH, 2015, 75

← 1 2 3 4 5 →