Review
Copyright ©The Author(s) 2021.
World J Gastrointest Oncol. Oct 15, 2021; 13(10): 1229-1243
Published online Oct 15, 2021. doi: 10.4251/wjgo.v13.i10.1229
Table 1 Small molecules able to induce autophagic activity
Agents
Mechanism of action
GDC-0941Inhibitor of class I PI3K
GDC-0980Dual inhibitor of PI3K and mTORC1
EverolimusmTORC1 inhibitor
TemsirolimusmTORC1 inhibitor
RapamycinmTORC1 inhibitor
Tat–beclin 1 peptideReleases beclin-1 into cytoplasm-regulate autophagosome formation
MetforminAMPK activator
FluspirileneAntagonists of L-type Ca2+ channels
LoperamideAntagonists of L-type Ca2+ channels
AmiodaroneAntagonists of L-type Ca2+ channels
IsoliensinineNatural alkaloid
CepharanthineNatural alkaloid
Table 2 Small molecules able to inhibit autophagic activity
Agents
Mechanism of action
3-Methyladenine (3-MA)Inhibitor of class III PI3K
LY294002PI3K inhibitor
WortmanninPI3K inhibitor
SB202190Cross-inhibition of the PI3K/mTOR and MAPKs pathway
MHY1485Activator of mTOR
AzithromycinInhibitor of v-ATPase, inhibition of lysosomal acidification
Bafilomycin A1Inhibitor of v-ATPase, inhibition of lysosomal acidification
Concanamycin AInhibitor of v-ATPase, inhibition of lysosomal acidification
Chloroquine (CQ)Autophagosome-lysosome fusion
Hydroxy-chloroquine (HCQ)Autophagosome-lysosome fusion
ClomipramineAlter acidification of lysosomes
VerteporfinAlter acidification of lysosomes
PaclitaxelMicrotubule stabilizer- inhibit phosphorylation of VPS34 at T159
Spain-1Inhibits the activity of ubiquitin-specific peptidases, USP10 and USP13
MonensinInhibit autophagosome-lysosome fusion