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 …

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 …

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 …

Proteolysis targeting chimeras (PROTACs) of anaplastic lymphoma kinase (ALK)

C Zhang, XR Han, X Yang, B Jiang, J Liu… - European journal of …, 2018 - Elsevier
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 …

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) …

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 …

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 …

Drug discovery targeting anaplastic lymphoma kinase (ALK)

X Kong, P Pan, H Sun, H Xia, X Wang… - Journal of Medicinal …, 2019 - ACS Publications
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 …

Chemically induced degradation of anaplastic lymphoma kinase (ALK)

CE Powell, Y Gao, L Tan, KA Donovan… - Journal of medicinal …, 2018 - ACS Publications
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) …

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 …