Discovery of a PROTAC targeting ALK with in vivo activity
G Yan, X Zhong, L Yue, C Pu, H Shan, S Lan… - European Journal of …, 2021 - Elsevier
Anaplastic lymphoma kinase (ALK) was involved in the development of various cancer
types. Although several ALK inhibitors have been advanced to clinical trials, the emergence …
types. Although several ALK inhibitors have been advanced to clinical trials, the emergence …
Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC)
CH Kang, DH Lee, CO Lee, J Du Ha, CH Park… - Biochemical and …, 2018 - Elsevier
Recently, proteolysis targeting chimera (PROTAC) technology is highlighted in drug
discovery area as a new therapeutic approach. PROTAC as a heterobifunctional molecule is …
discovery area as a new therapeutic approach. PROTAC as a heterobifunctional molecule is …
Development of alectinib-based PROTACs as novel potent degraders of anaplastic lymphoma kinase (ALK)
S Xie, Y Sun, Y Liu, X Li, X Li, W Zhong… - Journal of medicinal …, 2021 - ACS Publications
A series of novel anaplastic lymphoma kinase (ALK) degraders were designed and
synthesized based on proteolysis-targeting chimera (PROTAC) technology by linking two …
synthesized based on proteolysis-targeting chimera (PROTAC) technology by linking two …
Proteolysis targeting chimeras (PROTACs) of anaplastic lymphoma kinase (ALK)
Anaplastic lymphoma kinase (ALK) activation has been associated with many types of
human cancer. Significant efforts have been devoted to the development of ALK inhibitors to …
human cancer. Significant efforts have been devoted to the development of ALK inhibitors to …
Structure-based discovery of SIAIS001 as an oral bioavailability ALK degrader constructed from Alectinib
C Ren, N Sun, Y Kong, X Qu, H Liu, H Zhong… - European Journal of …, 2021 - Elsevier
Fusion proteins of the anaplastic lymphoma kinase (ALK) are promising therapeutic targets
for cancer and other human diseases, especially for non-small cell lung cancer (NSCLC) …
for cancer and other human diseases, especially for non-small cell lung cancer (NSCLC) …
Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance
N Sun, C Ren, Y Kong, H Zhong, J Chen, Y Li… - European Journal of …, 2020 - Elsevier
Abstract EML4-ALK and NPM-ALK fusion proteins possess constitutively activated ALK
(anaplastic lymphoma kinase) activity, which in turn leads to the development of non-small …
(anaplastic lymphoma kinase) activity, which in turn leads to the development of non-small …
Discovery of the GSH responsive “Y-PROTACs” targeting ALK and CDK4/6 as a potential treatment for cancer
S Wang, D Luo, C Pu, X Ma, H Zhang, Z Feng… - European Journal of …, 2023 - Elsevier
Combination of different molecular target inhibitors is an available method to improve the
therapeutic effect on tumors. Herein, to achieve both tumor cell targeting and ALK …
therapeutic effect on tumors. Herein, to achieve both tumor cell targeting and ALK …
Drug discovery targeting anaplastic lymphoma kinase (ALK)
As a receptor tyrosine kinase of insulin receptor (IR) subfamily, anaplastic lymphoma kinase
(ALK) has been validated to play important roles in various cancers, especially anaplastic …
(ALK) has been validated to play important roles in various cancers, especially anaplastic …
Chemically induced degradation of anaplastic lymphoma kinase (ALK)
We present the development of the first small molecule degraders that can induce anaplastic
lymphoma kinase (ALK) degradation, including in non-small-cell lung cancer (NSCLC) …
lymphoma kinase (ALK) degradation, including in non-small-cell lung cancer (NSCLC) …
Design, synthesis, and biological activity of urea derivatives as anaplastic lymphoma kinase inhibitors
G Boije af Gennäs, L Mologni, S Ahmed… - …, 2011 - Wiley Online Library
In anaplastic large‐cell lymphomas, chromosomal translocations involving the kinase
domain of anaplastic lymphoma kinase (ALK), generally fused to the 5'part of the …
domain of anaplastic lymphoma kinase (ALK), generally fused to the 5'part of the …