Target General Information
Target ID T63505
Target Name Tyrosine-protein kinase ABL1(ABL1) Target Info
Gene Name ABL1
Species Homo sapiens
Uniprot ID ABL1_HUMAN
Sequence MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSE
NDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVN
SLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTAS
DGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERT
DITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQ
LLGVCTREPPFYIITEFMTYGNLLDYLRECNRQEVNAVVLLYMATQISSAMEYLEKKNFI
HRDLAARNCLVGENHLVKVADFGLSRLMTGDTYTAHAGAKFPIKWTAPESLAYNKFSIKS
DVWAFGVLLWEIATYGMSPYPGIDLSQVYELLEKDYRMERPEGCPEKVYELMRACWQWNP
SDRPSFAEIHQAFETMFQESSISDEVEKELGKQGVRGAVSTLLQAPELPTKTRTSRRAAE
HRDTTDVPEMPHSKGQGESDPLDHEPAVSPLLPRKERGPPEGGLNEDERLLPKDKKTNLF
SALIKKKKKTAPTPPKRSSSFREMDGQPERRGAGEEEGRDISNGALAFTPLDTADPAKSP
KPSNGAGVPNGALRESGGSGFRSPHLWKKSSTLTSSRLATGEEEGGGSSSKRFLRSCSAS
CVPHGAKDTEWRSVTLPRDLQSTGRQFDSSTFGGHKSEKPALPRKRAGENRSDQVTRGTV
TPPPRLVKKNEEAADEVFKDIMESSPGSSPPNLTPKPLRRQVTVAPASGLPHKEEAGKGS
ALGTPAAAEPVTPTSKAGSGAPGGTSKGPAEESRVRRHKHSSESPGRDKGKLSRLKPAPP
PPPAASAGKAGGKPSQSPSQEAAGEAVLGAKTKATSLVDAVNSDAAKPSQPGEGLKKPVL
PATPKPQSAKPSGTPISPAPVPSTLPSASSALAGDQPSSTAFIPLISTRVSLRKTRQPPE
RIASGAITKGVVLDSTEALCLAISRNSEQMASHSAVLEAGKNLYTFCVSYVDSIQQMRNK
FAFREAINKLENNLRELQICPATAGSGPAATQDFSKLLSSVKEISDIVQR [Homo sap
iens]
Drug Resistance Mutation and Corresponding Drugs
Ref 536500Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.
Ref 539183(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1882).
Ref 536294Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
Ref 541030(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5687).
Ref 5287152006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
Ref 536577Dasatinib: a tyrosine kinase inhibitor for the treatment of chronic myelogenous leukemia and philadelphia chromosome-positive acute lymphoblastic leukemia. Clin Ther. 2007 Nov;29(11):2289-308.
Ref 541021(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5678).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 5292822007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
Ref 541038(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5697).
Ref 525021ClinicalTrials.gov (NCT02311998) Phase I/II Study of Bosutinib in Combination With Inotuzumab Ozogamicin in CD22-positive Philadelphia-Chromosome (PC) Positive Acute Lymphoblastic Leukemia (ALL) and Chronic Myeloid Leukemia (CML). U.S. National Institutes of Health.
Ref 541049(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5710).
Ref 1572605The ChEMBL database in 2017.
Mutation Info Missense: A344V
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: A350V
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: A365V
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: A366G
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: A380T
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: A397P
Drugs
Drug Name Imatinib Drug Info [555788]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 77 patients
Mutation Info Missense: A399T
Drugs
Drug Name Imatinib Drug Info [555893]
Targeted Disease Leukemia
Drug Name Type I TKIs Drug Info [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: A433T
Drugs
Drug Name Imatinib Drug Info [555715], [555785], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 94 patients
Mutation Info Missense: D276A
Drugs
Drug Name Imatinib Drug Info [555923]
Targeted Disease Leukemia
Mutation Prevalence 38 out of 45 patients
Mutation Info Missense: D276G
Drugs
Drug Name Imatinib Drug Info [555534]
Targeted Disease Leukemia
Mutation Prevalence 16 out of 49 patients in all ABL mutations
Drug Name Type I TKIs Drug Info [555813]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: D276N
Drugs
Drug Name Imatinib Drug Info [555945]
Targeted Disease Leukemia
Mutation Info Missense: D363Y
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: D444Y
Drugs
Drug Name Dasatinib Drug Info [555765]
Targeted Disease Leukemia
Mutation Info Missense: D482V
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 4 out of 53 patients
Mutation Info Missense: E255K
Drugs
Drug Name Dasatinib Drug Info [555765], [555785], [555817]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 21 patients
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 4 out of 94 patients
Drug Name Nilotinib Drug Info [555785], [555806]
Targeted Disease Leukemia
Mutation Prevalence 2 out of 21 patients
Mutation Info Missense: E255V
Drugs
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 3 out of 94 patients
Drug Name Nilotinib Drug Info [555785], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 21 patients
Drug Name Type I TKIs Drug Info [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: E258D
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: E275K
Drugs
Drug Name Imatinib Drug Info [555806], [555955]
Targeted Disease Leukemia
Mutation Info Missense: E275Q
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: E279A
Drugs
Drug Name Imatinib Drug Info [555945]
Targeted Disease Leukemia
Mutation Info Missense: E279K
Drugs
Drug Name Imatinib Drug Info [555806], [555882]
Targeted Disease Leukemia
Mutation Info Missense: E279Y
Drugs
Drug Name Imatinib Drug Info [555769]
Targeted Disease Leukemia
Mutation Info Missense: E279Z
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 53 patients
Mutation Info Missense: E282G
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 2 out of 53 patients
Mutation Info Missense: E282K
Drugs
Drug Name Type I TKIs Drug Info [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: E292Q
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: E292V
Drugs
Drug Name Imatinib Drug Info [555715], [555719], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 94 patients
Mutation Info Missense: E352D
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 53 patients
Mutation Info Missense: E352G
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 53 patients
Mutation Info Missense: E355?
Drugs
Drug Name Imatinib Drug Info [555769]
Targeted Disease Leukemia
Mutation Info Missense: E355A
Drugs
Drug Name Imatinib Drug Info [555715], [555806], [555990]
Targeted Disease Leukemia
Mutation Prevalence 2 out of 94 patients
Mutation Info Missense: E355D
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: E355G
Drugs
Drug Name Imatinib Drug Info [556211]
Targeted Disease Leukemia
Mutation Prevalence 7 out of 17 patients
Drug Name Dasatinib Drug Info [555699], [555765]
Targeted Disease Leukemia
Mutation Info Missense: E373K
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: E450?
Drugs
Drug Name Imatinib Drug Info [555769]
Targeted Disease Leukemia
Mutation Info Missense: E450A
Drugs
Drug Name Imatinib Drug Info [555758], [555769], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 62 patients
Mutation Info Missense: E450G
Drugs
Drug Name Imatinib Drug Info [555758]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 62 patients
Mutation Info Missense: E450K
Drugs
Drug Name Imatinib Drug Info [555730], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 55 patients
Mutation Info Missense: E450V
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: E453A
Drugs
Drug Name Imatinib Drug Info [555806], [555945]
Targeted Disease Leukemia
Mutation Info Missense: E453D
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 53 patients
Mutation Info Missense: E453G
Drugs
Drug Name Imatinib Drug Info [555806], [555955]
Targeted Disease Leukemia
Mutation Info Missense: E453K
Drugs
Drug Name Imatinib Drug Info [555715], [555719], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 94 patients
Mutation Info Missense: E453L
Drugs
Drug Name Imatinib Drug Info [555769]
Targeted Disease Leukemia
Mutation Info Missense: E453V
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: E459A
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: E459G
Drugs
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 2 out of 94 patients
Mutation Info Missense: E459K
Drugs
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 2 out of 94 patients
Mutation Info Missense: E459Q
Drugs
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 94 patients
Mutation Info Missense: E459V
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: E494G
Drugs
Drug Name Imatinib Drug Info [555893]
Targeted Disease Leukemia
Mutation Info Missense: E507G
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: F311I
Drugs
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 2 out of 94 patients
Mutation Info Missense: F311L
Drugs
Drug Name Imatinib Drug Info [555923]
Targeted Disease Leukemia
Mutation Prevalence 38 out of 45 patients
Drug Name Type I TKIs Drug Info [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: F317C
Drugs
Drug Name Imatinib Drug Info [555806], [555909]
Targeted Disease Leukemia
Drug Name Dasatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: F317I
Drugs
Drug Name Imatinib Drug Info [555806], [555909]
Targeted Disease Leukemia
Drug Name Dasatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: F317L
Drugs
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 9 out of 94 patients
Drug Name Dasatinib Drug Info [555789]
Targeted Disease Leukemia
Mutation Prevalence 4 out of 60 patients
Drug Name Type I TKIs Drug Info [555813], [555819], [555881]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: F317R
Drugs
Drug Name Dasatinib Drug Info [555892]
Targeted Disease Leukemia
Mutation Info Missense: F317V
Drugs
Drug Name Imatinib Drug Info [555754], [555806], [555909]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 40 patients
Drug Name Dasatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: F359*
Drugs
Drug Name Imatinib Drug Info [555769]
Targeted Disease Leukemia
Mutation Info Missense: F359?
Drugs
Drug Name Imatinib Drug Info [555769]
Targeted Disease Leukemia
Mutation Info Missense: F359A
Drugs
Drug Name Imatinib Drug Info [555534]
Targeted Disease Leukemia
Mutation Prevalence 16 out of 49 patients in all ABL mutations
Mutation Info Missense: F359C
Drugs
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 2 out of 94 patients
Drug Name Nilotinib Drug Info [555785], [555806]
Targeted Disease Leukemia
Mutation Prevalence 2 out of 21 patients
Mutation Info Missense: F359I
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 2 out of 53 patients
Drug Name Nilotinib Drug Info [555806]
Targeted Disease Leukemia
Drug Name Bosutinib Drug Info [555892]
Targeted Disease Chronic Myeloid Leukaemia
Drug Name Dasatinib Drug Info [555699]
Targeted Disease Leukemia
Drug Name Type I TKIs Drug Info [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: F359L
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: F359V
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 4 out of 53 patients
Drug Name Nilotinib Drug Info [555806]
Targeted Disease Leukemia
Drug Name Dasatinib Drug Info [556073]
Targeted Disease Leukemia
Drug Name Bosutinib Drug Info [555796]
Targeted Disease Chronic Myeloid Leukaemia
Drug Name Type I TKIs Drug Info [555813]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: F382L
Drugs
Drug Name Imatinib Drug Info [555502], [555719], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 53 patients
Mutation Info Missense: F486S
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 3 out of 53 patients
Mutation Info Missense: G250E
Drugs
Drug Name Imatinib Drug Info [555810]
Targeted Disease Leukemia
Mutation Prevalence 6 out of 36 patients
Drug Name Nilotinib Drug Info [555796]
Targeted Disease Leukemia
Drug Name Dasatinib Drug Info [555699], [555765], [555791]
Targeted Disease Leukemia
Drug Name Type I TKIs Drug Info [555813], [555819], [555881]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: G250R
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: G251D
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 53 patients
Mutation Info Missense: G251E
Drugs
Drug Name Imatinib Drug Info [555990]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 125 patients
Mutation Info Missense: G398R
Drugs
Drug Name Imatinib Drug Info [556052]
Targeted Disease Leukemia
Mutation Prevalence 33% of the patients
Mutation Info Missense: H396A
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: H396P
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 53 patients
Mutation Info Missense: H396R
Drugs
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 3 out of 94 patients
Drug Name Nilotinib Drug Info [555882]
Targeted Disease Leukemia
Drug Name Type I TKIs Drug Info [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: I242T
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: I293V
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: I418S
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: I418V
Drugs
Drug Name Imatinib Drug Info [555719], [555769], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 53 patients
Mutation Info Missense: K247R
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: K294 > RGG
Drugs
Drug Name Imatinib Drug Info [555791]
Targeted Disease Leukemia
Mutation Info Missense: K378R
Drugs
Drug Name Imatinib Drug Info [555893]
Targeted Disease Leukemia
Mutation Info Missense: K419E
Drugs
Drug Name Imatinib Drug Info [555882]
Targeted Disease Leukemia
Mutation Info Missense: L248R
Drugs
Drug Name Bosutinib Drug Info [555892]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: L248V
Drugs
Drug Name Imatinib Drug Info [555513]
Targeted Disease Leukemia
Mutation Prevalence 27 out of 144 patients
Mutation Info Missense: L273M
Drugs
Drug Name Imatinib Drug Info [555719], [555735], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 53 patients
Drug Name Dasatinib Drug Info [555765]
Targeted Disease Leukemia
Mutation Info Missense: L298V
Drugs
Drug Name Imatinib Drug Info [555810]
Targeted Disease Leukemia
Mutation Prevalence 2 out of 36 patients
Mutation Info Missense: L324Q
Drugs
Drug Name Imatinib Drug Info [555806], [556031]
Targeted Disease Leukemia
Mutation Info Missense: L340L
Drugs
Drug Name Imatinib Drug Info [555923]
Targeted Disease Leukemia
Mutation Prevalence 38 out of 45 patients
Mutation Info Missense: L364I
Drugs
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 94 patients
Mutation Info Missense: L370P
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: L384M
Drugs
Drug Name Imatinib Drug Info [555981]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 4 patients
Drug Name Type I TKIs Drug Info [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: L387F
Drugs
Drug Name Imatinib Drug Info [555806], [555945]
Targeted Disease Leukemia
Mutation Info Missense: L387M
Drugs
Drug Name Imatinib Drug Info [555754]
Targeted Disease Leukemia
Mutation Prevalence 3 out of 40 patients
Drug Name Type I TKIs Drug Info [555813]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: L387V
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: M237V
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: M244V
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 8 out of 53 patients
Drug Name Type I TKIs Drug Info [555813], [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: M343T
Drugs
Drug Name Imatinib Drug Info [555502], [555806]
Targeted Disease Leukemia
Mutation Info Missense: M351K
Drugs
Drug Name Imatinib Drug Info [555893]
Targeted Disease Leukemia
Mutation Info Missense: M351T
Drugs
Drug Name Imatinib Drug Info [555788]
Targeted Disease Leukemia
Mutation Prevalence 7 out of 77 patients
Drug Name Nilotinib Drug Info [555696]
Targeted Disease Leukemia
Drug Name Bosutinib Drug Info [555796]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: M388L
Drugs
Drug Name Imatinib Drug Info [555715], [555719], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 94 patients
Drug Name Type I TKIs Drug Info [555813]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: M472I
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: N368S
Drugs
Drug Name Imatinib Drug Info [555990]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 125 patients
Mutation Info Missense: N374Y
Drugs
Drug Name Imatinib Drug Info [555745]
Targeted Disease Leukemia
Mutation Info Missense: P480L
Drugs
Drug Name Imatinib Drug Info [555730], [555806]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 55 patients
Mutation Info Missense: Q252E
Drugs
Drug Name Imatinib Drug Info [555547]
Targeted Disease Leukemia
Mutation Prevalence 30% of the patients
Mutation Info Missense: Q252H
Drugs
Drug Name Imatinib Drug Info [555505]
Targeted Disease Leukemia
Mutation Prevalence 23 out of 66 patients in all ABL mutations
Drug Name Type I TKIs Drug Info [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: Q252K
Drugs
Drug Name Imatinib Drug Info [555785]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 21 patients
Mutation Info Missense: Q252R
Drugs
Drug Name Imatinib Drug Info [555502], [555806]
Targeted Disease Leukemia
Mutation Info Missense: R220H
Drugs
Drug Name Type I TKIs Drug Info [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: R328M
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 53 patients
Mutation Info Missense: S417F
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: S417Y
Drugs
Drug Name Imatinib Drug Info [555923]
Targeted Disease Leukemia
Mutation Prevalence 38 out of 45 patients
Mutation Info Missense: S438C
Drugs
Drug Name Imatinib Drug Info [555806], [555893], [555945]
Targeted Disease Leukemia
Mutation Info Missense: T277A
Drugs
Drug Name Imatinib Drug Info [555806], [555893], [555923]
Targeted Disease Leukemia
Mutation Prevalence 38 out of 45 patients
Mutation Info Missense: T315A
Drugs
Drug Name Dasatinib Drug Info [555806], [555892]
Targeted Disease Leukemia
Drug Name Imatinib Drug Info [555909]
Targeted Disease Leukemia
Mutation Info Missense: T315I
Drugs
Drug Name Dasatinib Drug Info [555817]
Targeted Disease Leukemia
Mutation Prevalence 12 out of 17 patients
Drug Name Imatinib Drug Info [555715]
Targeted Disease Leukemia
Mutation Prevalence 9 out of 94 patients
Drug Name Nilotinib Drug Info [555854]
Targeted Disease Leukemia
Drug Name Bosutinib Drug Info [555806]
Targeted Disease Chronic Myeloid Leukaemia
Drug Name Type I TKIs Drug Info [555813], [555819], [555881]
Targeted Disease Chronic Myeloid Leukaemia
Drug Name Nilotinib + Dasatinib Drug Info [555806]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: T315N
Drugs
Drug Name Imatinib Drug Info [555534]
Targeted Disease Leukemia
Mutation Prevalence 16 out of 49 patients in all ABL mutations
Mutation Info Missense: T315V
Drugs
Drug Name Nilotinib Drug Info [555892]
Targeted Disease Leukemia
Mutation Info Missense: T495R
Drugs
Drug Name Dasatinib Drug Info [555699]
Targeted Disease Leukemia
Mutation Info Missense: V256L
Drugs
Drug Name Imatinib Drug Info [555893]
Targeted Disease Leukemia
Mutation Info Missense: V280A
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: V289A
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Drug Name Type I TKIs Drug Info [555819]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: V289F
Drugs
Drug Name Imatinib Drug Info [555810], [555918], [555990]
Targeted Disease Leukemia
Mutation Prevalence 1 out of 40 patients
Mutation Info Missense: V289I
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: V299L
Drugs
Drug Name Dasatinib Drug Info [555699], [555765], [555806], [555898], [556073]
Targeted Disease Leukemia
Drug Name Imatinib Drug Info [555806], [555893], [555898], [555909]
Targeted Disease Leukemia
Drug Name Bosutinib Drug Info [555898]
Targeted Disease Chronic Myeloid Leukaemia
Drug Name Type I TKIs Drug Info [555819], [555881]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: V371A
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: V379I
Drugs
Drug Name Imatinib Drug Info [555923]
Targeted Disease Leukemia
Mutation Prevalence 38 out of 45 patients
Drug Name Dasatinib Drug Info [555765]
Targeted Disease Leukemia
Mutation Info Missense: W261L
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: Y253F
Drugs
Drug Name Imatinib Drug Info [555719]
Targeted Disease Leukemia
Mutation Prevalence 3 out of 53 patients
Drug Name Dasatinib Drug Info [555765]
Targeted Disease Leukemia
Mutation Info Missense: Y253H
Drugs
Drug Name Imatinib Drug Info [555789]
Targeted Disease Leukemia
Mutation Prevalence 6 out of 60 patients
Drug Name Dasatinib Drug Info [555765], [555791], [555796]
Targeted Disease Leukemia
Drug Name Nilotinib Drug Info [555806], [555882]
Targeted Disease Leukemia
Drug Name Type I TKIs Drug Info [555813]
Targeted Disease Chronic Myeloid Leukaemia
Mutation Info Missense: Y320C
Drugs
Drug Name Imatinib Drug Info [555806], [555893]
Targeted Disease Leukemia
Mutation Info Missense: Y342H
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Mutation Info Missense: Y353H
Drugs
Drug Name Imatinib Drug Info [555810]
Targeted Disease Leukemia
Mutation Prevalence 4 out of 36 patients
Drug Name Dasatinib Drug Info [555765]
Targeted Disease Leukemia
Mutation Info Missense: Y393C
Drugs
Drug Name Imatinib Drug Info [555806]
Targeted Disease Leukemia
Reference
Ref 555502Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell. 2002 Aug;2(2):117-25.
Ref 555505Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy. Leukemia. 2002 Nov;16(11):2190-6.
Ref 555513Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis. Blood. 2003 Jul 1;102(1):276-83. Epub 2003 Mar 6.
Ref 555534High incidence of BCR-ABL kinase domain mutations and absence of mutations of the PDGFR and KIT activation loops in CML patients with secondary resistance to imatinib. Hematol J. 2004;5(1):55-60.
Ref 555547Evidence of ABL-kinase domain mutations in highly purified primitive stem cell populations of patients with chronic myelogenous leukemia. Biochem Biophys Res Commun. 2004 Oct 22;323(3):728-30.
Ref 555696Sequential development of mutant clones in an imatinib resistant chronic myeloid leukaemia patient following sequential treatment with multiple tyrosine kinase inhibitors: an emerging problem? Cancer Chemother Pharmacol. 2009 Jun;64(1):195-7. doi: 10.1007/s00280-008-0905-5. Epub 2009 Jan 21.
Ref 555699Complexity of BCR-ABL kinase domain mutations during the course of therapy with tyrosine kinase inhibitors in chronic myeloid leukemia. Am J Hematol. 2009 Apr;84(4):256-7. doi: 10.1002/ajh.21366.
Ref 555715Long-term outcome of patients with chronic myeloid leukemia treated with second-generation tyrosine kinase inhibitors after imatinib failure is predicted by the in vitro sensitivity of BCR-ABL kinase domain mutations. Blood. 2009 Sep 3;114(10):2037-43. doi: 10.1182/blood-2009-01-197715. Epub 2009 Jun 30.
Ref 555719Determining the rise in BCR-ABL RNA that optimally predicts a kinase domain mutation in patients with chronic myeloid leukemia on imatinib. Blood. 2009 Sep 24;114(13):2598-605. doi: 10.1182/blood-2008-08-173674. Epub 2009 Jul 22.
Ref 555730Dynamic change of T315I BCR-ABL kinase domain mutation in Korean chronic myeloid leukaemia patients during treatment with Abl tyrosine kinase inhibitors. Hematol Oncol. 2010 Jun;28(2):82-8. doi: 10.1002/hon.918.
Ref 555735Spectrum of BCR-ABL kinase domain mutations in patients with chronic myeloid leukemia from India with suspected resistance to imatinib-mutations are rare and have different distributions. Leuk Lymphoma. 2009 Dec;50(12):2092-5. doi: 10.3109/10428190903332486.
Ref 555745Kinase domain mutations and responses to dose escalation in chronic myeloid leukemia resistant to standard dose imatinib mesylate. Leuk Lymphoma. 2010 Jan;51(1):79-84. doi: 10.3109/10428190903437629.
Ref 555754Mutations in ABL kinase domain are associated with inferior progression-free survival. Leuk Lymphoma. 2010 Jun;51(6):1072-8. doi: 10.3109/10428191003729741.
Ref 555758Rapid and sensitive allele-specific (AS)-RT-PCR assay for detection of T315I mutation in chronic myeloid leukemia patients treated with tyrosine-kinase inhibitors. Clin Exp Med. 2011 Mar;11(1):55-9. doi: 10.1007/s10238-010-0101-x. Epub 2010 May 29.
Ref 555765Longitudinal studies of SRC family kinases in imatinib- and dasatinib-resistant chronic myelogenous leukemia patients. Leuk Res. 2011 Jan;35(1):38-43. doi: 10.1016/j.leukres.2010.06.030. Epub 2010 Jul 29.
Ref 555769Characteristics of BCR-ABL kinase domain point mutations in Chinese imatinib-resistant chronic myeloid leukemia patients. Ann Hematol. 2011 Jan;90(1):47-52. doi: 10.1007/s00277-010-1039-5. Epub 2010 Aug 10.
Ref 555785Results of allogeneic hematopoietic stem cell transplantation for chronic myelogenous leukemia patients who failed tyrosine kinase inhibitors after developing BCR-ABL1 kinase domain mutations. Blood. 2011 Mar 31;117(13):3641-7. doi: 10.1182/blood-2010-08-302679. Epub 2010 Dec 14.
Ref 555788BCR-ABL isoforms associated with intrinsic or acquired resistance to imatinib: more heterogeneous than just ABL kinase domain point mutations? Med Oncol. 2012 Mar;29(1):219-26. doi: 10.1007/s12032-010-9781-z. Epub 2011 Jan 8.
Ref 555789BCR-ABL1 mutations in patients with imatinib-resistant Philadelphia chromosome-positive leukemia by use of the PCR-Invader assay. Leuk Res. 2011 May;35(5):598-603. doi: 10.1016/j.leukres.2010.12.006. Epub 2011 Jan 15.
Ref 555791A novel insertion mutation of K294RGG within BCR-ABL kinase domain confers imatinib resistance: sequential analysis of the clonal evolution in a patient with chronic myeloid leukemia in blast crisis. Int J Hematol. 2011 Feb;93(2):237-42. doi: 10.1007/s12185-011-0766-2. Epub 2011 Jan 25.
Ref 555796Outcome of patients with chronic myeloid leukemia with multiple ABL1 kinase domain mutations receiving tyrosine kinase inhibitor therapy. Haematologica. 2011 Jun;96(6):918-21. doi: 10.3324/haematol.2010.039321. Epub 2011 Feb 28.
Ref 555806BCR-ABL kinase domain mutation analysis in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors: recommendations from an expert panel on behalf of European LeukemiaNet. Blood. 2011 Aug 4;118(5):1208-15. doi: 10.1182/blood-2010-12-326405. Epub 2011 May 11.
Ref 555810Clinical outcome of chronic myeloid leukemia imatinib-resistant patients: do BCR-ABL kinase domain mutations affect patient survival? First multicenter Argentinean study. Leuk Lymphoma. 2011 Sep;52(9):1720-6. doi: 10.3109/10428194.2011.578310. Epub 2011 Jun 12.
Ref 555813Use of direct sequencing for detection of mutations in the BCR-ABL kinase domain in Slovak patients with chronic myeloid leukemia. Neoplasma. 2011;58(6):548-53.
Ref 555817Dasatinib as first-line treatment for adult patients with Philadelphia chromosome-positive acute lymphoblastic leukemia. Blood. 2011 Dec 15;118(25):6521-8. doi: 10.1182/blood-2011-05-351403. Epub 2011 Sep 19.
Ref 555819ABL domain kinase point mutations as a cause of resistance to therapy of patients with chronic myeloid leukemia with tyrosine kinase inhibitors
Ref 555854Analysis of mutations in the BCR-ABL1 kinase domain, using direct sequencing: detection of the T315I mutation in bone marrow CD34+ cells of a patient with chronic myelogenous leukemia 6 months prior to its emergence in peripheral blood. Mol Diagn Ther. 2012 Jun 1;16(3):163-6. doi: 10.2165/11632420-000000000-00000.
Ref 555881Early detection and quantification of mutations in the tyrosine kinase domain of chimerical BCR-ABL1 gene combining high-resolution melting analysis and mutant-allele specific quantitative polymerase chain reaction. Leuk Lymphoma. 2013 Mar;54(3):598-606. doi: 10.3109/10428194.2012.718767. Epub 2012 Aug 31.
Ref 555882Role of treatment in the appearance and selection of BCR-ABL1 kinase domain mutations. Mol Diagn Ther. 2012 Aug 1;16(4):251-9. doi: 10.2165/11635340-000000000-00000.
Ref 555892Three novel patient-derived BCR/ABL mutants show different sensitivity to second and third generation tyrosine kinase inhibitors. Am J Hematol. 2012 Nov;87(11):E125-8. doi: 10.1002/ajh.23338. Epub 2012 Oct 9.
Ref 555893Impact of BCR-ABL mutations on response to dasatinib after imatinib failure in elderly patients with chronic-phase chronic myeloid leukemia. Ann Hematol. 2013 Jan;92(2):179-83. doi: 10.1007/s00277-012-1591-2. Epub 2012 Oct 10.
Ref 555898Characteristics and outcomes of patients with V299L BCR-ABL kinase domain mutation after therapy with tyrosine kinase inhibitors. Blood. 2012 Oct 18;120(16):3382-3. doi: 10.1182/blood-2012-04-424192.
Ref 555909BCR-ABL1 compound mutations in tyrosine kinase inhibitor-resistant CML: frequency and clonal relationships. Blood. 2013 Jan 17;121(3):489-98. doi: 10.1182/blood-2012-05-431379. Epub 2012 Dec 5.
Ref 555918Contribution of BCR-ABL kinase domain mutations to imatinib mesylate resistance in Philadelphia chromosome positive Malaysian chronic myeloid leukemia patients. Hematol Rep. 2012 Nov 19;4(4):e23. doi: 10.4081/hr.2012.e23. Epub 2012 Nov 23.
Ref 555923Frequency of ABL gene mutations in chronic myeloid leukemia patients resistant to imatinib and results of treatment switch to second-generation tyrosine kinase inhibitors. Med Clin (Barc). 2013 Aug 4;141(3):95-9. doi: 10.1016/j.medcli.2012.10.028. Epub 2013 Feb 22.
Ref 555945Detection of BCR-ABL kinase domain mutations in patients with chronic myeloid leukemia on imatinib. Hematology. 2013 Nov;18(6):328-33. doi: 10.1179/1607845413Y.0000000095. Epub 2013 May 8.
Ref 555955BCR-ABL1 kinase domain mutations may persist at very low levels for many years and lead to subsequent TKI resistance. Br J Cancer. 2013 Sep 17;109(6):1593-8. doi: 10.1038/bjc.2013.318. Epub 2013 Jun 25.
Ref 555981The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma. Cancer Discov. 2014 Jan;4(1):94-109. doi: 10.1158/2159-8290.CD-13-0617. Epub 2013 Nov 21.
Ref 555990BCR-ABL kinase domain mutations, including 2 novel mutations in imatinib resistant Malaysian chronic myeloid leukemia patients-Frequency and clinical outcome. Leuk Res. 2014 Apr;38(4):454-9. doi: 10.1016/j.leukres.2013.12.025. Epub 2014 Jan 6.
Ref 556031Increased genomic instability may contribute to the development of kinase domain mutations in chronic myeloid leukemia. Int J Hematol. 2014 Dec;100(6):567-74. doi: 10.1007/s12185-014-1685-9. Epub 2014 Oct 4.
Ref 556052Incidence and clinical importance of BCR-ABL1 mutations in Iranian patients with chronic myeloid leukemia on imatinib. J Hum Genet. 2015 May;60(5):253-8. doi: 10.1038/jhg.2015.11. Epub 2015 Mar 5.
Ref 556073Long-term follow-up of a phase 2 study of chemotherapy plus dasatinib for the initial treatment of patients with Philadelphia chromosome-positive acute lymphoblastic leukemia. Cancer. 2015 Dec 1;121(23):4158-64. doi: 10.1002/cncr.29646. Epub 2015 Aug 26.
Ref 556211Characterization of the rpsL and rrs genes of streptomycin-resistant clinical isolates of Mycobacterium tuberculosis in Japan. J Appl Microbiol. 1997 Nov;83(5):634-40.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.