Preferred Label : DNA Polymerase Theta Inhibitor MOMA-313;
NCIt synonyms : Polymerase Theta Helicase Inhibitor MOMA-313; Pol Theta Inhibitor MOMA-313;
NCIt definition : An orally bioavailable inhibitor of DNA polymerase (pol) theta helicase, with potential
antineoplastic activity. Upon oral administration, DNA polymerase theta inhibitor
MOMA-313 specifically targets, binds to and inhibits the pol theta helicase domain
and thereby inhibits the activity of pol theta. This prevents pol theta-mediated repair
of DNA double-strand breaks (DSBs) via the theta-mediated end joining (TMEJ) process.
This causes apoptosis and inhibits proliferation in homologous recombination (HR)-deficient
cancer cells. MOMA-313 may have a synergistic effect if administered in combination
with a poly (adenosine diphosphate ribose) polymerase (PARP) inhibitor. Pol theta,
a DNA helicase-polymerase protein, plays a key role in repair of DNA DSBs through
TMEJ and is highly expressed in cancer cells while nearly absent in most healthy tissues.
It plays a key role in cancer cell survival. In HR-deficient cancers, DNA DSB repair
is impaired and is dependent on pol theta for repair and survival.;
Molecule name : MOMA 313; MOMA-313;
Origin ID : C211936;
concept_is_in_subset
- has_target
