Resistance mutation info of drug

Drug General Information

Drug ID

D01XYJ

Drug Name

Zidovudine

Synonyms

zidovudine; Azidothymidine; 30516-87-1; 3'-Azido-3'-deoxythymidine; Retrovir; AZT; Zidovudinum; Compound S; Thymidine, 3'-azido-3'-deoxy-; ZIDOVUDINE [AZT]; zidovudin; BW A509U; Zidovudinum [Latin]; Zidovudina [Spanish]; BWA509U; DRG-0004; 3'-Azido-2',3'-Dideoxythymidine; ZDV; UNII-4B9XT59T7S; 3'-Deoxy-3'-azidothymidine; CCRIS 105; Aztec; BW-A509U; BW-A-509U; HSDB 6515; 3'-Azido-3'-deoxythymidine (AIDS); CHEMBL129; NSC 602670; BW-A 509U; MLS000028548; 4B9XT59T7S; AZT; Antiviral; Azidodeoxythymidine; ZVD; Zidovudin; Zidovudina; AZT Antiviral; AZT TRANSPLACENTAL CARCINOGENESIS STUDY; Antiviral AZT; Cpd S; Racemic Liposomal AZT; Zidovudine EP III; BWA 509U; K7 [P Ti2 W10 O40]; AZT & EPO; AZT & HPA; AZT & Lymphoblastoid Interferon; AZT & SST; AZT & rsT4; AZT & sCD4; AZT & srCD4; AZT (Antiviral); AZT+PRO 140; AZT, Antiviral; Apo-Zidovudine; BWA-509U; Intron A & AZT; Novo-Azt; Propolis+AZT; Retrovir (TN); Retrovir(TM); Retrovis (TN); Zidovudine+PRO 140; AZT & Colony-stimulating factor 2; AZT & Concanavalin A (ConA); AZT & GM-CSF; AZT & IFN-alpha; AZT & IL-1; AZT & IL-2; AZT & IL-6; AZT & Li & EPO; AZT & NP (from PHCA or HSA); AZT & PM-19; DS-4152 & AZT; Liposomal AZT-SN-1; Liposomal AZT-SN-3; PC-SOD+AZT;RIFN-beta seron & AZT; AZT & CD4(178)-PE 40; AZT & Li & GM-CSF; AZT & Li & IL-1; AZT & Li & IL-6; AZT & rIFNalpha2; Racemic-dipalmitoylglycerophospho-AZT (in a lipid vesicle); Zidovudine (JAN/USP/INN); Zidovudine [USAN:INN:BAN:JAN]; AZT & rsCD4 & rIFNalphaA; SN-1-dipalmitoylglycerophospho-AZT (in a lipid vesicle); SN-3-dipalmitoylglycerophospho-AZT (in a lipid vesicle); AZT & Interferon-alpha-2; Met-SDF-1beta & AZT; Met-SDF-1beta & Zidovudine; Interferon AD + 3'-azido-3'-deoxythymidine; 1-(3-Azido-2,3-dideoxy-beta-D-ribofuranosyl)thymine; 3′-Azido-3′-deoxythymidine; 3' Azido 2',3' Dideoxythymidine; 3' Azido 3' deoxythymidine; 3'-Azido-3'-deoxythymidine & Concanavalin A; 3'-Azido-3'-deoxythymidine & Erythropoietin; 3'-Azido-3'-deoxythymidine & Heteropolyoxotungstate PM-19; 3'-Azido-3'-deoxythymidine & Interleukin-1; 3'-Azido-3'-deoxythymidine & Interleukin-2; 3'-Azido-3'-deoxythymidine & Interleukin-6; 3'-Azido-3'-deoxythymidine & Lithium & Erythropoietin; 3'-Azido-3'-deoxythymidine & Lithium & Interleukin-1; 3'-Azido-3'-deoxythymidine & Lithium & Interleukin-6; 3'-Azido-3'-deoxythymidine & Lymphoblastoid Interferon; 3'-Azido-3'-deoxythymidine & Sho-Saiko-To; 3'-Azido-3'deoxythymidine & Interferon-alpha; 3'-Azidothymidine; 3'-azido-3'-deoxythymidine, AZT; 3-Azido-3-deoxythymidine; Dendrigen; CTCE-0422

Drug Type

Small molecular drug

Therapeutic Class

Anti-HIV Agents

Company

GlaxoSmithKline

Structure

Drug Resistance Mutations

Target Name

HIV Non-Nucleoside reverse transcriptase

Target Info

Uniprot ID

POL_HV1B1(600-1159)

Species

Human immunodeficiency virus type 1 (HIV-1)

Reference Sequence

PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI
YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNKGRQKVVPLTNTTNQKTELQ
AIYLALQDSGLEVNIVTDSQYALGIIQAQPDKSESELVNQIIEQLIKKEKVYLAWVPAHK
GIGGNEQVDKLVSAGIRKIL [Human immunodeficiency virus type 1 (H
IV-1)]

Targeted Disease

HIV infection

Drug Resistance Mutations

Mutation info	Deletion: D67				[1], [2]
Level of Resistance	Intermediate resistance

Mutation info	Insertion: T69				[1], [2]
Level of Resistance	High-level resistance

Target Name

HIV Nucleoside reverse transcriptase

Target Info

Uniprot ID

POL_HV1B1(600-1159)

Species

Human immunodeficiency virus type 1 (HIV-1)

Reference Sequence

Targeted Disease

HIV infection

Drug Resistance Mutations

Mutation info	Missense: T215Y				[1], [2]
Level of Resistance	Intermediate resistance

Mutation info	Missense: D67N				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: K219E				[2], [3]

Mutation info	Missense: K219Q				[2], [3]

Mutation info	Missense: K65*				[2], [3]

Mutation info	Missense: K70*				[2], [3]

Mutation info	Missense: K70R				[2], [3]
Level of Resistance	Intermediate resistance

Mutation info	Missense: L210W				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: L74*				[2], [3]

Mutation info	Missense: M184*				[2], [3]

Mutation info	Missense: M41L				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: Q151L				[2], [3]
Level of Resistance	Intermediate resistance

Mutation info	Missense: Q151M				[2], [3]
Level of Resistance	High-level resistance

Mutation info	Missense: T210W				[2], [3]

Mutation info	Missense: T215A				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: T215C				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: T215D				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: T215E				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: T215F				[2], [3]
Level of Resistance	Intermediate resistance

Mutation info	Missense: T215I				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: T215L				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: T215N				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: T215S				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: T215V				[2], [3]
Level of Resistance	Low-level resistance

Mutation info	Missense: L74I				[3]
Mutation Frequency	3-20% of the samples

Target Name

ATP-binding cassette sub-family G member 2 (ABCG2)

Target Info

Gene Name

ABCG2

Uniprot ID

ABCG2_HUMAN

Species

Homo sapiens

Reference Sequence

MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVE
KEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCN
SGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGT
QFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIF
SIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIING
DSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKK
ITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDS
TGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLP
MRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLL
MTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGN
NPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS [Hom
o sapiens]

Targeted Disease

HIV infection

Drug Resistance Mutations

Mutation info	Missense: R482M				[4]

References

REF 1

HIV drug development: the next 25 years. Nat Rev Drug Discov. 2007 Dec;6(12):959-66.

REF 2

The HIVdb system for HIV-1 genotypic resistance interpretation. Intervirology. 2012;55(2):98-101.

REF 3

Mechanisms of anti-retroviral drug resistance: implications for novel drug discovery and development. Infect Disord Drug Targets. 2013 Oct;13(5):330-6.

REF 4

Induction of cellular resistance to nucleoside reverse transcriptase inhibitors by the wild-type breast cancer resistance protein. Biochem Pharmacol. 2004 Oct 1;68(7):1363-70.

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

Prof. Feng ZHU

Prof. Yuzong CHEN