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- NCIT_C175542 IAO_0000115 "An orally available inhibitor of mutant form of the isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1 [NADP+] soluble), including the substitution mutation at arginine (R) in position 132, IDH1(R132), with potential antineoplastic activity. Upon oral administration, IDH1 mutant inhibitor LY3410738 specifically and covalently binds to and modifies a single cysteine (Cys269) in the allosteric binding pocket of mutant forms of IDH1, thereby inactivating IDH1. This inhibits the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This depletes 2-HG levels, prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing mutant forms of IDH1. In addition, LY3410738 has the ability to cross the blood-brain barrier (BBB). IDH1 mutations, including IDH1(R132) mutations, are highly expressed in certain malignancies, including gliomas; they initiate and drive cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG." @default.
- NCIT_C175542 NCIT_A32 NCIT_C1909 @default.
- NCIT_C175542 NCIT_A7 NCIT_C117280 @default.
- NCIT_C175542 NCIT_NHC0 "C175542" @default.
- NCIT_C175542 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C175542 NCIT_P107 "IDH1 Mutant Inhibitor LY3410738" @default.
- NCIT_C175542 NCIT_P108 "IDH1 Mutant Inhibitor LY3410738" @default.
- NCIT_C175542 NCIT_P208 "CL1412892" @default.
- NCIT_C175542 NCIT_P322 "CTRP" @default.
- NCIT_C175542 NCIT_P322 "GDC" @default.
- NCIT_C175542 NCIT_P329 "803295" @default.
- NCIT_C175542 NCIT_P330 "803295" @default.
- NCIT_C175542 NCIT_P375 "IDH1 Mutant Inhibitor LY3410738" @default.
- NCIT_C175542 NCIT_P399 "803295" @default.
- NCIT_C175542 normalizedInformationContent "100" @default.
- NCIT_C175542 referenceCount "1" @default.
- NCIT_C175542 hasExactSynonym "IDH1 Inhibitor LY3410738" @default.
- NCIT_C175542 hasExactSynonym "IDH1 Mutant Inhibitor LY3410738" @default.
- NCIT_C175542 hasExactSynonym "LY 3410738" @default.
- NCIT_C175542 hasExactSynonym "LY-3410738" @default.
- NCIT_C175542 hasExactSynonym "LY3410738" @default.
- NCIT_C175542 inSubset NCIT_C116977 @default.
- NCIT_C175542 inSubset NCIT_C116978 @default.
- NCIT_C175542 inSubset NCIT_C128784 @default.
- NCIT_C175542 inSubset NCIT_C157711 @default.
- NCIT_C175542 inSubset NCIT_C157712 @default.
- NCIT_C175542 inSubset NCIT_C176424 @default.
- NCIT_C175542 inSubset NCIT_C177537 @default.
- NCIT_C175542 type Class @default.
- NCIT_C175542 isDefinedBy ncit.owl @default.
- NCIT_C175542 label "IDH1 Mutant Inhibitor LY3410738" @default.
- NCIT_C175542 subClassOf NCIT_C129824 @default.
- NCIT_C175542 subClassOf NCIT_C129825 @default.
- NCIT_C175542 subClassOf NCIT_C137826 @default.
- NCIT_C175542 subClassOf NCIT_C163758 @default.
- NCIT_C175542 subClassOf NCIT_C168618 @default.
- NCIT_C175542 subClassOf NCIT_C175542 @default.
- NCIT_C175542 subClassOf NCIT_C1908 @default.
- NCIT_C175542 subClassOf NCIT_C1909 @default.
- NCIT_C175542 subClassOf NCIT_C2189 @default.
- NCIT_C175542 subClassOf NCIT_C274 @default.
- NCIT_C175542 subClassOf NCIT_C471 @default.