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. 2021 Jan 12;10(1):142. doi: 10.3390/cells10010142

Figure 4.

Figure 4

Targeting ROR1 with small molecules and immunotherapy—a selection of agents. While KAN0441571C functions as a tyrosine kinase inhibitor and already meets clinical evaluation, the inhibitor ARI-1, binding to the CRD of ROR1, is still in preclinical development. The most advanced monoclonal antibody (mAb) targeting ROR1 is cirmtuzumab. Other antibody-based targeting options comprise VLS-101, an antibody drug conjugate linking cirmtuzumab to MMAE, or bispecific antibodies such as ROR1 × CD3 or NBE-002. ROR1 is also an attractive target for chimeric antigen receptor-engineered (CAR) T cells since it does not lead to B cell depletion. Strictinin is a newly discovered, plant-derived tannin, which seemingly interacts with ROR1 and inhibits PI3K/AKT/GSK-3 activity.