Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM5KXFI)

Drug Name

NUTLIN-3 Drug Info

Synonyms

Nutlin-3; 548472-68-0; 890090-75-2; nutlin-3A; nutlin 3; (+/-)-Nutlin3; CHEMBL211045; Nutlin 3(Random Configuration); MDM2 Antagonist, Nutlin-3, Racemic; 4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one; 4-({4,5-bis(4-chlorophenyl)-2-[4-methoxy-2-(propan-2-yloxy)phenyl]-4,5-dihydro-1H-imidazol-1-yl}carbonyl)piperazin-2-one; 4-[4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

Cross-matching ID

PubChem CID: 216345
ChEBI ID: CHEBI:93777
CAS Number: CAS 548472-68-0
TTD Drug ID: DM5KXFI

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Investigative Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting Mdm2 messenger RNA (MDM2 mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
NU-8231	DMEUV5R	Discovery agent	N.A.	Investigative	[3]
ISIS 16518	DM24L0S	Solid tumour/cancer	2A00-2F9Z	Investigative	[4]
PLSQETFSDLWKLLPEN-NH2	DMBN4V6	Discovery agent	N.A.	Investigative	[5]
NSC-66811	DMRVMA5	Discovery agent	N.A.	Investigative	[6]
ISIS 16507	DMK69ZR	Solid tumour/cancer	2A00-2F9Z	Investigative	[4]
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Drug(s) Targeting Cellular tumor antigen p53 (TP53)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Contusugene ladenovec	DMN9ETB	Oral cancer	2B6E	Phase 3	[7]
QPI-1002	DMDU5Y2	Renal transplantation	NE84	Phase 3	[8]
Thymoquinone	DMVDTR2	Polycystic ovarian syndrome	5A80.1	Phase 2/3	[9]
APG-115	DMIFA0L	Prolymphocytic leukaemia	2A82.1	Phase 2	[10]
SGT-53	DMLYIPA	Pancreatic cancer	2C10	Phase 2	[11]
APR-246	DMNFADH	Ovarian cancer	2C73	Phase 2	[12]
Ad-p53	DMJSWXL	Solid tumour/cancer	2A00-2F9Z	Phase 2	[13]
Kevetrin	DMFO6MH	Ovarian cancer	2C73	Phase 2	[10]
INGN-225	DMF7J6D	Head and neck cancer	2D42	Phase 2	[14]
ALT-801	DM9KL7P	Acute myeloid leukaemia	2A60	Phase 2	[15]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cellular tumor antigen p53 (TP53)	TT7SBF5	P53_HUMAN	Inhibitor	[1]
Mdm2 messenger RNA (MDM2 mRNA)	TT9TE0O	MDM2_HUMAN	Inhibitor	[2]

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References

1	Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein intera... J Med Chem. 2009 Nov 26;52(22):7044-53.
2	Reaching for high-hanging fruit in drug discovery at protein-protein interfaces. Nature. 2007 Dec 13;450(7172):1001-9.
3	Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold. J Med Chem. 2006 Oct 19;49(21):6209-21.
4	US patent application no. 6,238,921, Antisense oligonucleotide modulation of human mdm2 expression.
5	Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction. J Med Chem. 2006 Jun 15;49(12):3432-5.
6	Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening str... J Med Chem. 2006 Jun 29;49(13):3759-62.
7	A review of contusugene ladenovec (Advexin) p53 therapy. Curr Opin Mol Ther. 2009 Feb;11(1):54-61.
8	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
9	Apoptosis as a mechanism for the treatment of adult T cell leukemia: promising drugs from benchside to bedside. Drug Discov Today. 2020 Jul;25(7):1189-1197.
10	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
11	Transferrin receptor targeting nanomedicine delivering wild-type p53 gene sensitizes pancreatic cancer to gemcitabine therapy. Cancer Gene Ther. 2013 Apr;20(4):222-8.
12	APR-246/PRIMA-1MET inhibits thioredoxin reductase 1 and converts the enzyme to a dedicated NADPH oxidase. Cell Death Dis. 2013 Oct 24;4:e881.
13	Assessment of p53 gene transfer and biological activities in a clinical study of adenovirus-p53 gene therapy for recurrent ovarian cancer. Cancer Gene Ther. 2003 Mar;10(3):224-38.
14	INGN-225: a dendritic cell-based p53 vaccine (Ad.p53-DC) in small cell lung cancer: observed association between immune response and enhanced chemotherapy effect. Expert Opin Biol Ther. 2010 Jun;10(6):983-91.
15	Phase I trial of ALT-801, an interleukin-2/T-cell receptor fusion protein targeting p53 (aa264-272)/HLA-A*0201 complex, in patients with advanced malignancies. Clin Cancer Res. 2011 Dec 15;17(24):7765-75.