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Tumor Discovery RNA-protein complexes deregulated in cancer

Table 6. Molecules acting on intrinsically disordered proteins and biomolecular condensates (BCs)
Compound Target Application References
AC1Q3QWB HOTAIR-EZH2 binding Various cancers, BC favors euchromatin 206
RK33 inhibits ATPase DDX3, resulting in the block of CRC, head/neck cancer, PC, brain cancer, drug 173
16D inhibits helicase SGs assembly resistance
G3BP inhibitor G3Ia Block the interaction of G3BP with VCP multisystem proteinopathy 168,176
nSP3 peptide caprin 1 and USP10 and dissolves
the preformed SG
ZW-115 Stress-inducible NUPR1 Induces apoptosis, K-RAS tumors, PDAC 259,260
TAT-SIP-C1/2, TAT-SIP-U1-Antp Inhibitory peptides (SIPs) derived Induce sensitivity to sorafenib 265
from Caprin 1 and USP10
Ralaniten, EPI-7170 Blocks AR binding to DNA Prostate cancer, androgen resistant 266
ReACp53 peptides Bind p53 intrinsically disordered High-grade serous ovarian carcinoma 267
region
Aminothiazole BAY 249716, BAY Stabilize p53 variants R175H, Dissolution of the nuclear condensates 11,268
1892005 R282W and Y220C
PRIMA-1, ADH-6 Reactivates mutated p53 Induce apoptosis in normoxia and hypoxia 268
Nutlin-3 p Prevents the MDM2-p53 Increases the p53 shelf-life 268
interaction
Dyphenylfurans (DPF) Triple helix containing MALAT1 Degradation of MALAT1 in overexpressing cancers 269
Dovitinib Multiple RTK inhibitors Blocks miR-21 biogenesis 270
Small molecule DB1273 RNA G-quadruplexes targets K-RAS and N-RAS-bearing cancer 271
Verteporfin Blocks TRIM28 interaction with Inhibits IRF-induced PD-L1 expression and 274,275
IRF1 Golgi-related autophagy mechanisms
Psammaplysin F Decreases the levels of Improves chemotherapy, increases the efficacy of 276
phosphorylated eIF2α, inhibits bortezomib sorafenib
SG formation after eIF2
phosphorylation
Cannabidiol, lipoamide Attenuates the formation of SGs GBM; reduce FUS-linked stress granules induced by 277,278
and BCs arsenate
Trisenox/Tretinoin Inhibit PML bodies Induce PML-RARa degradation HCC, MM 278,281
VTP50469 Disrupts the interactions between Therapy for NUP98-rearranged leukemia 282
the NUP98 fusion proteins and
chromatin
Emodin, MLN4924, and TSA Increase the levels of PML protein Restore PML body activity 282
MLN4924 NEDDylation inhibitor Suppresses APL 282
SU056, fisetin, CX-5461 Y-box-binding protein 1 (YB1) CRC, melanoma, block invasiveness in BC 184
PI3K/mTOR dual inhibitors: Inhibit NEAT1_2 and paraspeckle CLL therapy 96
GSK1059615, CAY10626, samotolisib,
4Torin 1, PP242, PI-103, LY3023414,
INK128
Dual PI3K/TOR inhibitor BEZ235 Inhibit YB-1 expression Favors radiotherapy cytotoxicity in CRC, blocks 184
EMT, and invasiveness in melanoma
YK-4-279 Targets the IDR of EWS-FLI1 Ewing sarcoma tumors 280,281
SHP2 inhibitors AB-3068, TNO155, Therapy of SHP2 mutations Trials in solid cancers 282
RMC-4630, and RLY-1971 inducing BC formation and
promoting MAPK signaling,
leading to ERK1/2 activation
Elvitegravir Disrupts SRC-1 condensates, Suppresses the growth of YAP-dependent tumors, 282
P bodies, YAP/TEAD/SRC-1 BCs favors anti-PD-1 immunotherapy
(Cont’d...)

Volume 3 Issue 4 (2024) 21 doi: 10.36922/td.4657