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Substrate Report for: CHR-2863

The aminopeptidase inhibitor CHR-2863 is an orally bioavailable inhibitor of murine malaria. It is an orally available hydrophobic inhibitor prodrug used as chemotherapeutic agents for the treatment of refractory acute myeloid leukemia. It is hydrolyzed by CES1


General
Type Drug
Chemical_Nomenclature cyclopentyl (2S)-2-[[(2R)-2-[(1S)-2-(hydroxyamino)-1-methoxy-2-oxoethyl]-4-methylpentanoyl]amino]-2-phenylacetate
Canonical SMILES CC(C)CC(C(C(=O)NO)OC)C(=O)NC(C1=CC=CC=C1)C(=O)OC2CCCC2
InChI InChI=1S/C22H32N2O6/c1-14(2)13-17(19(29-3)21(26)24-28)20(25)23-18(15-9-5-4-6-10-15)22(27)30-16-11-7-8-12-16/h4-6,9-10,14,16-19,28H,7-8,11-13H2,1-3H3,(H,23,25)(H,24,26)/t17-,18+,19+/m1/s1
InChIKey NYGGUGZLUBNLTJ-QYZOEREBSA-N
Other name(s) CHR 2863 ; CHR2863 ; Cyclopentyl (2S)-2-[[(2R)-2-[(1S)-2-(hydroxyamino)-1-methoxy-2-oxo-ethyl]-4-methyl-pentanoyl]amino]-2-phenyl-acetate
________________________________________________________________________________________________
MW|420.49
Formula|C22H32N2O6
CAS_number|
PubChem|15547707
UniChem|NYGGUGZLUBNLTJ-QYZOEREBSA-N
IUPHAR|
Wikipedia|

Target
Families | CHR-2863 ligand of proteins in family: Carb_B_Chordata

References:
Search PubMed for references concerning: CHR-2863
    Title: Multifactorial resistance to aminopeptidase inhibitor prodrug CHR2863 in myeloid leukemia cells: down-regulation of carboxylesterase 1, drug sequestration in lipid droplets and pro-survival activation ERK/Akt/mTOR
    Verbrugge SE, Al M, Assaraf YG, Kammerer S, Chandrupatla DM, Honeywell R, Musters RP, Giovannetti E, O'Toole T and Jansen G <10 more author(s)>
    Ref: Oncotarget, 7:5240, 2016 : PubMed

            

    Title: The aminopeptidase inhibitor CHR-2863 is an orally bioavailable inhibitor of murine malaria
    Skinner-Adams TS, Peatey CL, Anderson K, Trenholme KR, Krige D, Brown CL, Stack C, Nsangou DM, Mathews RT and Gardiner DL <2 more author(s)>
    Ref: Antimicrobial Agents & Chemotherapy, 56:3244, 2012 : PubMed