Fibroblast growth factor receptor (FGFR)-selective tyrosine kinase inhibitors (TKI), such as infigratinib, show potency and selectivity for FGFR3 at pharmacologically 'relevant doses for the potential treatment of achondroplasia (ACH)

被引:0
|
作者
Dobscha, Katherine [1 ]
Wei, Ge [1 ]
Dambkowski, Carl [1 ]
Rogoff, Daniela [1 ]
机构
[1] QED Therapeut Inc, San Francisco, CA USA
关键词
D O I
暂无
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
P-726
引用
收藏
页码:273 / 273
页数:1
相关论文
共 41 条
  • [21] Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3
    Shvartsbart, Artem
    Roach, Jeremy J.
    Witten, Michael R.
    Koblish, Holly
    Harris, Jennifer J.
    Covington, Maryanne
    Hess, Rodrigo
    Lin, Luping
    Frascella, Michelle
    Truong, Lisa
    Leffet, Lynn
    Conlen, Patricia
    Beshad, Elham
    Klabe, Ron
    Katiyar, Kamna
    Kaldon, Laura
    Young-Sciame, Ruth
    He, Xin
    Petusky, Susan
    Chen, Kwang-Jong
    Horsey, April
    Lei, Hsiang-Ting
    Epling, Leslie B.
    Deller, Marc C.
    Vechorkin, Oleg
    Yao, Wenqing
    JOURNAL OF MEDICINAL CHEMISTRY, 2022, 65 (22) : 15433 - 15442
  • [22] B-701, a selective and potent inhibitor of fibroblast growth factor receptor 3 (FGFR3), may enhance the activity of bladder cancer therapies
    Holash, J.
    Schwartz, K.
    Lau, S.
    EUROPEAN JOURNAL OF CANCER, 2016, 69 : S20 - S20
  • [23] Insulin-like growth factor I (IGF-I) rescues apoptosis induced by achondroplasia-type mutation of fibroblast growth factor receptor 3 (FGFR3) in chondrocytes.
    Koike, M
    Yamanaka, Y
    Nishimura, R
    Tanaka, H
    Seino, Y
    JOURNAL OF BONE AND MINERAL RESEARCH, 1999, 14 : S324 - S324
  • [24] FGFR3/fibroblast growth factor receptor 3 inhibits autophagy through decreasing the ATG12-ATG5 conjugate, leading to the delay of cartilage development in achondroplasia
    Wang, Xiaofeng
    Qi, Huabing
    Wang, Quan
    Zhu, Ying
    Wang, Xianxing
    Jin, Min
    Tan, Qiaoyan
    Huang, Qizhao
    Xu, Wei
    Li, Xiaogang
    Kuang, Liang
    Tang, Yubing
    Du, Xiaolan
    Chen, Di
    Chen, Lin
    AUTOPHAGY, 2015, 11 (11) : 1998 - 2013
  • [25] Identification of potential drug molecules against fibroblast growth factor receptor 3 (FGFR3) by multi-stage computational-biophysics correlate
    Ahmad, Sajjad
    Almanaa, Taghreed N.
    Khan, Saifullah
    Aljahdali, Salma Mohammed
    Waheed, Yasir
    Aljasir, Mohammad Abdullah
    Al-Megrin, Wafa Abdullah I.
    Aziz, Aamir
    Ateeq, Muhammad
    Amin, Fazli
    Khattak, Saeed Ullah
    Sanami, Samira
    JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 2025, 43 (03): : 1240 - 1248
  • [26] Fibroblast growth factor receptor 3 (FGFR3) alterations in PROOF 302: A phase III trial of infigratinib (BGJ398) as adjuvant therapy in patients (pts) with invasive urothelial carcinoma (UC)
    Grivas, Petros
    Daneshmand, Siamak
    Makarov, Vladimir
    Bellmunt, Joaquim
    Sridhar, Srikala S.
    Sonpavde, Guru P.
    Cole, Suzanne
    Tripathi, Abhishek
    Faltas, Bishoy Morris
    Lerner, Seth P.
    Fleming, Mark T.
    Loriot, Yohann
    Meeks, Joshua J.
    Master, Viraj A.
    Davis, Kimberlee
    Van Veenhuyzen, David Friedrich
    Afifi, Shugufa
    Pal, Sumanta Kumar
    Gupta, Shilpa
    JOURNAL OF CLINICAL ONCOLOGY, 2023, 41 (16)
  • [27] Hypochondroplasia, achondroplasia, and thanatophoric dysplasia caused by mutations of the fibroblast-growth-factor-receptor-3-gene (FGFR 3) [Hypochondroplasie, achondroplasie und thanatophore dysplasie als folge von mutationen des fibroblastenwachstumsfaktor-rezeptor-3-gens (FGFR3)]
    Hilbert M.
    Hilbert K.
    Spranger J.
    Wildhardt G.
    Winterpacht A.
    Wüchner C.
    Zabel B.
    Monatsschrift Kinderheilkunde, 1998, 146 (7) : 687 - 691
  • [28] Expression of fibroblast growth factor receptor-3 (FGFR3), signal transducer and activator of transcription-1, and cyclin-dependent kinase inhibitor p21 during endochondral ossification: Differential role of FGFR3 in skeletal development and fracture repair
    Nakajima, A
    Shimizu, S
    Moriya, H
    Yamazaki, M
    ENDOCRINOLOGY, 2003, 144 (10) : 4659 - 4668
  • [29] A Lys644Glu substitution in fibroblast growth factor receptor 3 (FGFR3) causes dwarfism in mice by activation of STATs and ink4 cell cycle inhibitors
    Li, CL
    Chen, L
    Iwata, T
    Kitagawa, M
    Fu, XY
    Deng, CX
    HUMAN MOLECULAR GENETICS, 1999, 8 (01) : 35 - 44
  • [30] A Functional Genetic Screen Identifies the Phosphoinositide 3-kinase Pathway as a Determinant of Resistance to Fibroblast Growth Factor Receptor Inhibitors in FGFR Mutant Urothelial Cell Carcinoma
    Wang, Liqin
    Sustic, Tonci
    de Oliveira, Rodrigo Leite
    Lieftink, Cor
    Halonen, Pasi
    van de Ven, Marieke
    Beijersbergen, Roderick L.
    van den Heuvel, Michel M.
    Bernards, Rene
    van der Heijden, Michiel S.
    EUROPEAN UROLOGY, 2017, 71 (06) : 858 - 862