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

General Information of Drug (ID: DMGMC8H)

Drug Name
LY333531 Drug Info
Synonyms
Ruboxistaurin; 169939-94-0; LY-333531; Ruboxistaurin [INN]; LY 333531; UNII-721809WQCP; 721809WQCP; K00587a; 13-((Dimethylamino)methyl)-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H,13H-dibenzo(e,k)pyrrolo(3,4-h)(1,4,13)oxadiazacyclohexadecene-1,3(2H)-dione; CHEMBL432130; (9S)-9-[(dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-di(metheno)dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione; Br-WR99210
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 2 [1]
Cross-matching ID
PubChem CID
153999
CAS Number
CAS 169939-94-0
TTD Drug ID
DMGMC8H
INTEDE Drug ID
DR1860

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Polypeptide deformylase (PDF) TT9SL3Q DEFM_HUMAN Inhibitor [2]
Protein kinase C beta (PRKCB) TTYPXQF KPCB_HUMAN Inhibitor [3] , [4] , [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Phase 2 [6]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Solid tumour/cancer
ICD Disease Classification 2A00-2F9Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Polypeptide deformylase (PDF) DTT PDF 8.87E-16 -0.54 -0.86
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 7.29E-03 -3.47E-02 -1.80E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 ClinicalTrials.gov (NCT00482976) Effect of LY333531 on Vascular and Neural Functions. U.S. National Institutes of Health.
2 Three-dimensional structure of M. tuberculosis dihydrofolate reductase reveals opportunities for the design of novel tuberculosis drugs. J Mol Biol. 2000 Jan 14;295(2):307-23.
3 Protein kinase C beta inhibition attenuates the progression of experimental diabetic nephropathy in the presence of continued hypertension. Diabetes. 2003 Feb;52(2):512-8.
4 Protein kinase C activation and its pharmacological inhibition in vascular disease. Vasc Med. 2000;5(3):173-85.
5 Characterization of protein kinase C beta isoform activation on the gene expression of transforming growth factor-beta, extracellular matrix components, and prostanoids in the glomeruli of diabetic rats. J Clin Invest. 1997 Jul 1;100(1):115-26.
6 The interactions of a selective protein kinase C beta inhibitor with the human cytochromes P450. Drug Metab Dispos. 2002 Sep;30(9):957-61.