Publication

Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation.

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Nature2015PMID 25686603stubpubmedPublished

Abstract

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Linked entities

Linked entities (36)

How each link was made (MeSH, dictionary, registry reference, curation…) and whether it has been validated. Candidate links are not counted in entity statistics.

Validated 36

cancerAcute Lymphoblastic Leukemiacivic_curation1.00
cancerChronic Myeloid Leukemia, BCR-ABL1 Positivecivic_curation1.00
drugAxitinibcivic_curation1.00
drugDasatinibcivic_curation1.00
drugImatinibcivic_curation1.00
drugNilotinibcivic_curation1.00
drugPonatinibcivic_curation1.00
geneABL1civic_curation1.00
variantABL1 D276Gcivic_curation1.00
variantABL1 E255Kcivic_curation1.00
variantABL1 E255Vcivic_curation1.00
variantABL1 E279Kcivic_curation1.00
variantABL1 E292Lcivic_curation1.00
variantABL1 F317Lcivic_curation1.00
variantABL1 F317Rcivic_curation1.00
variantABL1 F317Vcivic_curation1.00
variantABL1 F359Icivic_curation1.00
variantABL1 F359Vcivic_curation1.00
variantABL1 F486Scivic_curation1.00
variantABL1 Fusioncivic_curation1.00
variantABL1 G250Ecivic_curation1.00
variantABL1 H396Pcivic_curation1.00
variantABL1 H396Rcivic_curation1.00
variantABL1 L248Rcivic_curation1.00
variantABL1 L248Vcivic_curation1.00
variantABL1 L384Mcivic_curation1.00
variantABL1 M244Vcivic_curation1.00
variantABL1 M343Tcivic_curation1.00
variantABL1 M351Tcivic_curation1.00
variantABL1 Q252Hcivic_curation1.00
variantABL1 T315Acivic_curation1.00
variantABL1 T315Icivic_curation1.00
variantABL1 T315Vcivic_curation1.00
variantABL1 V299Lcivic_curation1.00
variantABL1 Y253Fcivic_curation1.00
variantABL1 Y253Hcivic_curation1.00

Curated evidence

Evidence citing this paper (33)

civicCuratedShowing 1–33 of 33 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
ABL1 T315I + ABL1 Fusion5
Axitinib + PonatinibSubstitutes	Acute Lymphoblastic Leukemia	Predictive	D	Does Not Support Resistance	3	accepted	EID7777 Bone marrow mononuclear cells (BM MNCs) were isolated from three acute lymphoblastic leukemia patients with the BCR-ABL1 T315I variant who were pretreated with various chemotherapeutics and dasatinib.… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
Dasatinib + Imatinib + NilotinibSubstitutes	Acute Lymphoblastic Leukemia	Predictive	D	Supports Resistance	3	accepted	EID7778 Bone marrow mononuclear cells (BM MNCs) isolated from three acute lymphoblastic leukemia patients with the BCR-ABL1 T315I variant. Patients were pretreated with various chemotherapeutics and dasatinib… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	C	Supports Sensitivity Response	4	accepted	EID4369 In this study, enzymatic profiling, crystal structures, and proliferation assays using Ba/F3 with the BCR-ABL1 variant showed higher sensitivity to axitinib in fusions with the T315I variant of ABL1 c… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
Dasatinib + Imatinib + NilotinibSubstitutes	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	3	accepted	EID7780 Bone marrow mononuclear cells (BM MNCs) were isolated from a chronic myeloid leukemia patients with the BCR-ABL1 T315I variant who was pretreated with imatinib, dasatinib, and chemotherapy. The patien… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
Ponatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID7779 Bone marrow mononuclear cells (BM MNCs) were isolated from a chronic myeloid leukemia patient with the BCR-ABL1 T315I variant. The patient was pretreated with imatinib, dasatinib, and chemotherapy. Th… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 D276G + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4360 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed increased incorporations when harboring fusions with … (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 E255K + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4355 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed increased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 E255K + ABL1 V299L + ABL1 Fusion1
Dasatinib + PonatinibSubstitutes	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	accepted	EID7781 Bone marrow mononuclear cells isolated from a chronic myeloid leukemia patient with the BCR-ABL1 fusion and E255K and V299L secondary variants in ABL1 showed a high drug sensitivity score to ponatinib… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 E255V + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4441 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed increased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 E279K + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	accepted	EID7772 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed similar incorporation when harboring fusions with the… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 E292L + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	2	accepted	EID7773 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed similar incorporation when harboring fusions with the… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 F317L + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4390 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed increased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 F317R + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID7774 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed higher incorporation when harboring fusions with the … (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 F317V + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4535 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed increased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 F359I + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	2	accepted	EID4529 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed similar incorporation when harboring fusions with the… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 F359V + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	2	accepted	EID3822 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed similar incorporation when harboring fusions with the… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 F486S + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	2	accepted	EID4438 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed similar incorporation when harboring fusions with the… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 G250E + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4320 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed higher incorporation when harboring fusions with the … (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 H396P + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	2	accepted	EID7770 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed lower incorporation when harboring fusions with the H… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 H396R + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4417 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed increased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 L248R + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID7776 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed increased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 F359I + ABL1 L248R + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID7775 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed similar sensitivity to axitinib in fusions with the L… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 L248V + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4311 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed decreased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 L384M + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	2	accepted	EID4525 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed similar incorporation when harboring fusions with the… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 M244V + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	2	accepted	EID7771 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed similar incorporation when harboring fusions with the… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 M343T + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4534 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed increased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 M351T + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	2	accepted	EID7769 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed decreased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 Q252H + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4323 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed increased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 T315A + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	accepted	EID7768 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed decreased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 T315V + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	accepted	EID7766 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed reduced incorporation when treated with axitinib in f… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 V299L + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	accepted	EID7767 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed decreased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 Y253F + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID4345 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed increased incorporation when harboring fusions with t… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic
ABL1 Y253H + ABL1 Fusion1
Axitinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	2	accepted	EID4329 In a proliferation assay measuring tritiated thymidine incorporation in the presence of axitinib, Ba/F3 cells carrying the BCR-ABL1 variant showed similar incorporation when harboring fusions with the… (full text at CIViC) PMID 25686603 · Pemovska et al., 2015 · Open in CIViC	civic