1196548-56-7Relevant academic research and scientific papers
Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders
Chen, Liqun,Chen, Yanke,Zhang, Chunyan,Jiao, Bingyang,Liang, Sheng,Tan, Qiong,Chai, Hongyu,Yu, Weihua,Qian, Yongzheng,Yang, Hui,Yao, Wuyi,Yu, Jianguo,Luo, Ying,Plewe, Michael,Wang, Jialiang,Han, Xiao-Ran,Liu, Jing
, p. 14562 - 14575 (2020)
We report compounds 5 (CG416) and 6 (CG428) as two first-in-class tropomyosin receptor kinase (TRK) degraders that target the intracellular kinase domain of TRK. Degraders 5 and 6 reduced levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colo
TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE
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, (2021/09/04)
This disclosure relates to bivalent compounds (e.g., bi-functional small molecule compounds), compositions comprising one or more of the bivalent compounds, and to methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof. The disclosure also relates to methods for identifying such bivalent compounds.
MODIFIED PROTEINS AND PROTEIN DEGRADERS
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, (2021/12/08)
Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE
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, (2020/03/15)
Bivalent compounds, compositions comprising one or more of the bivalent compounds, and methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof are provided. Methods for identifying such bivalent compounds are provided, either.
(R)-2-Phenylpyrrolidine substituted imidazopyridazines: A new class of potent and selective pan-TRK inhibitors
Choi, Ha-Soon,Rucker, Paul V.,Wang, Zhicheng,Fan, Yi,Albaugh, Pamela,Chopiuk, Greg,Gessier, Francois,Sun, Fangxian,Adrian, Francisco,Liu, Guoxun,Hood, Tami,Li, Nanxin,Jia, Yong,Che, Jianwei,McCormack, Susan,Li, Allen,Li, Jie,Steffy, Auzon,Culazzo, Annemarie,Tompkins, Celine,Phung, Van,Kreusch, Andreas,Lu, Min,Hu, Bin,Chaudhary, Apurva,Prashad, Mahavir,Tuntland, Tove,Liu, Bo,Harris, Jennifer,Seidel, H. Martin,Loren, Jon,Molteni, Valentina
, p. 562 - 567 (2015/05/27)
Deregulated kinase activities of tropomyosin receptor kinase (TRK) family members have been shown to be associated with tumorigenesis and poor prognosis in a variety of cancer types. In particular, several chromosomal rearrangements involving TRKA have be
