Drug Information

Drug (ID: DG00439) and It's Reported Resistant Information

Name	Thiopurine
Synonyms	2-Mercaptopurine; 2-Thiopurine; 28128-19-0; 5-Mercaptopurine; Purine-2-thiol; 3,7-dihydropurine-2-thione; Thiopurine; UNII-81XK02929C; 81XK02929C; 2-Purinethiol; 7H-purine-2-thiol; 1,3-Dihydro-2H-purine-2-thione; 2-MP; 3,7-dihydro-2H-purine-2-thione; EINECS 248-855-0; NSC 23720; 2H-Purine-2-thione, 1,3-dihydro-; SCHEMBL3896; DTXSID60878767; NSC23720; MFCD00047145; NSC-23720; ZINC12955987; AKOS006275100; 2-Mercaptopurine, >=95%, crystalline; 2H-Purine-2-thione, 1,3-dihydro- (9CI); FT-0694524; W-202176; Q27269279 Click to Show/Hide
Structure
Drug Resistance Disease(s)	Disease(s) with Clinically Reported Resistance for This Drug (1 diseases) Acute lymphocytic leukemia [ICD-11: 2B33] [1]
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Formula	C5H4N4S
IsoSMILES	C1=NC(=S)NC2=C1NC=N2
InChI	1S/C5H4N4S/c10-5-6-1-3-4(9-5)8-2-7-3/h1-2H,(H2,6,7,8,9,10)
InChIKey	HDBQZGJWHMCXIL-UHFFFAOYSA-N
PubChem CID	3015569

Type(s) of Resistant Mechanism of This Drug

UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

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Acute lymphocytic leukemia [ICD-11: 2B33]

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Drug Resistance Data Categorized by Their Corresponding Mechanisms
Unusual Activation of Pro-survival Pathway (UAPP)		Click to Show/Hide
Key Molecule: Cytosolic purine 5'-nucleotidase (NT5C2)			[1]
Molecule Alteration	Missense mutation	p.R238W	Molecule Info
Resistant Disease	Acute lymphocytic leukemia [ICD-11: 2B33.0]		Disease Info
Experimental Note	Identified from the Human Clinical Data
Experiment for Molecule Alteration	Whole-exome sequencing assay; Whole-genome sequencing assay
Experiment for Drug Resistance	Flow cytometric analysis assay; MTT assay
Mechanism Description	Finally, genomic profiling of diagnostic and relapsed leukemias has identified relapse-associated mutations in the 5'-nucleotidase, cytosolic II(NT5C2) gene as drivers of resistance to thiopurine chemotherapy in about 20% of T-ALL and 5% of B-precursor ALL cases at relapse.

References

Ref 1	Mutational landscape, clonal evolution patterns, and role of RAS mutations in relapsed acute lymphoblastic leukemia. Proc Natl Acad Sci U S A. 2016 Oct 4;113(40):11306-11311. doi: 10.1073/pnas.1608420113. Epub 2016 Sep 21.