2018
DOI: 10.1038/s41375-018-0113-1
|View full text |Cite
|
Sign up to set email alerts
|

First-in-class oral small molecule inhibitor of the tyrosine kinase ROR1 (KAN0439834) induced significant apoptosis of chronic lymphocytic leukemia cells

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
1
1
1
1

Citation Types

2
52
0

Year Published

2018
2018
2024
2024

Publication Types

Select...
6
1
1

Relationship

2
6

Authors

Journals

citations
Cited by 37 publications
(54 citation statements)
references
References 13 publications
2
52
0
Order By: Relevance
“…SUDHL4 (GCB type) ROR1 + ; MS (GCB type) ROR1 + ; RC-K8 (GCB type) ROR1 + ; OCI-LY3 (ABC type) ROR1 + ; U2932 (ABC type) ROR1 − . ROR1 expression was analyzed by flowcytometry and Western blot (see below) including expression of phosphorylated ROR1 protein (pROR1) [29]. Cells were cultured in RPMI-1640 medium (Life Technologies, Karlsruhe, Germany), supplemented with 10% fetal calf serum (Life Technologies), penicillin (100 IU/mL) and streptomycin (100 µg/mL) (Life Technologies).…”
Section: Cell Linesmentioning
confidence: 99%
See 2 more Smart Citations
“…SUDHL4 (GCB type) ROR1 + ; MS (GCB type) ROR1 + ; RC-K8 (GCB type) ROR1 + ; OCI-LY3 (ABC type) ROR1 + ; U2932 (ABC type) ROR1 − . ROR1 expression was analyzed by flowcytometry and Western blot (see below) including expression of phosphorylated ROR1 protein (pROR1) [29]. Cells were cultured in RPMI-1640 medium (Life Technologies, Karlsruhe, Germany), supplemented with 10% fetal calf serum (Life Technologies), penicillin (100 IU/mL) and streptomycin (100 µg/mL) (Life Technologies).…”
Section: Cell Linesmentioning
confidence: 99%
“…The development of the first small molecule inhibitor of the tyrosine kinase ROR1 (KAN0439834) was recently described [29]. Following a high-throughput screening campaign against the tyrosine kinase domain of ROR1, more than 2000 compounds were synthesized in the hit-to-lead and lead optimization stages.…”
Section: Small Molecule Ror1 Tyrosine Kinase Inhibitors (Kan0439834 Amentioning
confidence: 99%
See 1 more Smart Citation
“…In addition to cirmtuzumab, a number of other anti-ROR1 therapies are also in pre-clinical development Ca, cancer; CLL, chronic lymphocytic leukaemia; Endo, endometrial; met, metastatic; SC, squamous cell; TNBC, triple-negative breast cancer. (Hojjat-Farsangi et al 2017, Yin et al 2017, Hassannia et al 2018. Of these, ROR1 chimeric antigen receptor (CAR)-T cell therapy has attracted interest.…”
Section: :12mentioning
confidence: 99%
“…CLL, mantle cell lymphoma, B-cell ALL) and numerous types of solid tumors (37)(38)(39)(40). Due to its high-level surface expression as well as to its crucial role in tumor cell proliferation, survival, and metastasis, a number of pharmacological agents targeting ROR1 are under development, such as humanized monoclonal antibodies, small molecule inhibitors, bispecific T-cell engagers (BiTE) and anti-ROR1 CAR T cells (41)(42)(43). ROR1-targeted T cells have demonstrated to generate cytotoxicity against human ROR1 positive B cell malignancies in preclinical studies (39), without causing overt cytotoxicity in nonhuman primates (44).…”
Section: Novel T-cell Targets For B-cell Malignanciesmentioning
confidence: 99%