Resistance mutation info of target

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 524819ClinicalTrials.gov (NCT02181023) Acute Effect of Aclidinium on Hyperinflation and Ventilation Inhomogeneity in Severe COPD Patients. U.S. National Institutes of Health.
Ref 551969Clinical pipeline report, company report or official report of Novartis.
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
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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.

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