Table 2.

Distinct metabolism of and response to drugs by LSCs

Metabolic targetDescriptionTherapy, if applicableActive and recruiting trials
Hsp90 Heat shock protein; protective under cell stress conditions47  AT13387 N/A for AML 
AUY922 (luminespib) 
BIIB028 
STA-9090 (ganetespib) 
MPC-3100 
IPI-493 
SNX-5422 
NF-κB Nuclear factor κB; regulates stress response pathways7,48  Bortezomib NCT01736943 
NCT01534260 
   Choline magnesium trisalicylate N/A for AML 
   Pentoxifylline N/A for AML 
Glutathione Redox balance regulator51  Buthionine sulfoximine N/A for AML 
   CB-839 NCT02071927 
Bcl-2 B-cell lymphoma 2; regulator of mitochondrial activity and antiapoptotic factor52  Venetoclax NCT02670044 
NCT02203773 
   S 055746 NCT02920541 
   Oblimersen N/A for AML 
IDH1/2 Isocitrate dehydrogenase; susceptible to perturbations in oxidative phosphorlyation53  AG221 (IDH2 inhibitor) NCT02632708 
NCT02677922 
NCT02577406 
   AG120 (IDH1 inhibitor) NCT02632708 
NCT02074839 
   AG881 (dual IDH1 and IDH2 inhibitor) NCT02492737 
   IDH305 (IDH1 inhibitor) NCT02826642 
NCT02381886 
   FT-2102 (IDH1 inhibitor) NCT02719574 
ALOX-5 Arachidonate 5-lipoxygenase; potential LSC regulator54  VIA-2291 N/A for AML 
PF-04191834 
GSK2190915 
Metabolic targetDescriptionTherapy, if applicableActive and recruiting trials
Hsp90 Heat shock protein; protective under cell stress conditions47  AT13387 N/A for AML 
AUY922 (luminespib) 
BIIB028 
STA-9090 (ganetespib) 
MPC-3100 
IPI-493 
SNX-5422 
NF-κB Nuclear factor κB; regulates stress response pathways7,48  Bortezomib NCT01736943 
NCT01534260 
   Choline magnesium trisalicylate N/A for AML 
   Pentoxifylline N/A for AML 
Glutathione Redox balance regulator51  Buthionine sulfoximine N/A for AML 
   CB-839 NCT02071927 
Bcl-2 B-cell lymphoma 2; regulator of mitochondrial activity and antiapoptotic factor52  Venetoclax NCT02670044 
NCT02203773 
   S 055746 NCT02920541 
   Oblimersen N/A for AML 
IDH1/2 Isocitrate dehydrogenase; susceptible to perturbations in oxidative phosphorlyation53  AG221 (IDH2 inhibitor) NCT02632708 
NCT02677922 
NCT02577406 
   AG120 (IDH1 inhibitor) NCT02632708 
NCT02074839 
   AG881 (dual IDH1 and IDH2 inhibitor) NCT02492737 
   IDH305 (IDH1 inhibitor) NCT02826642 
NCT02381886 
   FT-2102 (IDH1 inhibitor) NCT02719574 
ALOX-5 Arachidonate 5-lipoxygenase; potential LSC regulator54  VIA-2291 N/A for AML 
PF-04191834 
GSK2190915 

N/A, not applicable.

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