Table 2 Evolving compounds and reagents regulating or inhibiting mTOR signaling, and its associated components, in various cancers
From: Recent advances and limitations of mTOR inhibitors in the treatment of cancer
Tested compounds | Preclinical study/mechanisms | Refs. |
|---|---|---|
RMC-4627 | In vitro models of B-cell acute lymphoblastic leukemia RMC-4627 BCR-ABL ↓4E-BP1 phosphorylation ↓ cancer cells progression ↓viability ↓ cancer cell survival | [55] |
1,4-O-diferuloylsecoisolariciresinol (IM-1) | In vitro mice embryonic fibroblast cells ↑nuclear translocation ↑S6K kinase ↑4E-BP1 ↑cytotoxicity ↑apoptosis | [116] |
Pierreione B (IM-2) | ||
DL001 | In vitro PC3 cells MEFs mice embryonic fibroblasts ↓hyperactive mTORC1 In vivo C57BL/6J mice ↓side effects of rapalogs | [85] |
DHM25 | In vitro triple-negative breast cancer cells ↓Akt phosphorylation | [35] |
3HOI-BA-01 | In vitro non-small cell lung cancer cells ↓mTOR kinase In vivo mice ↓tumor growth | [113] |
PF-5212384 PD-901 | In vitro 14 HNSCC cell lines ↑ cells in G0-/G1 phase ↓PI3K/mTOR ↓NF-κB, ↓AP-1, ↓IL8 ↓cells proliferation, ↓apoptosis, ↓angiogenesis | [63] |
P529 | In vitro GBM cells ↓AKT (Ser-473),↓NDRG1 (Thr-346) ↓PKCα (Ser-657) ↓cancer cells growth, ↓invasiveness In vivo Mice GBM xenograft ↓Tumor groth | [18] |
JR-AB2-011 (Palomid 529) | In vitro LLC-PK1, LLC-Mdr1a, LLC-MDR1 ↓ cancer cells’ growth In vivo WT and KO mice with gliomas ↑ blood brain passage | [56] |
W922 | In vitro HCT116, MCF-7, A549 ↓cancer cells viability In vivo mice xenograft model ↑ cell cycle arrest in G0-G1 phase ↑ apoptosis | [111] |