Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T89515 Target Info
Target Name Polypeptide deformylase (PDF)
Synonyms
PDF
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Target Type Successful Target
Gene Name PDF
Biochemical Class CH-NH donor oxidoreductase
UniProt ID
DEFM_HUMAN
Co-Targets of This Target  Top
Co-Target Name Solute carrier family 19 member 1 (SLC19A1) Successful Target
UniProt ID S19A1_HUMAN
Gene Name SLC19A1
Synonyms
Reduced folate carrier protein; RFC1; RFC; Placental folate transporter; Intestinal folate carrier 1; IFC-1; Folate transporter 1; FOLT; FLOT1
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Representative Drug(s) Pralatrexate Drug Info IC50 = 0.69 nM [1]
Co-Target Name Dihydrofolate reductase (DHFR) Successful Target
UniProt ID DYR_HUMAN
Gene Name DHFR
Synonyms
DYR; DHFRP1
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Representative Drug(s) Trimetrexate Drug Info IC50 < 1 nM [2]
Co-Target Name Proton-coupled folate transporter (SLC46A1) Successful Target
UniProt ID PCFT_HUMAN
Gene Name SLC46A1
Synonyms
Solute carrier family 46 member 1; PCFT/HCP1; PCFT; Heme carrier protein 1; HCP1; G21
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Representative Drug(s) Pralatrexate Drug Info IC50 = 57 nM [1]
Co-Target Name Folate receptor alpha (FOLR1) Successful Target
UniProt ID FOLR1_HUMAN
Gene Name FOLR1
Synonyms
Ovarian tumorassociated antigen MOv18; KB cells FBP; Folate receptor, adult; Folate receptor 1; FRalpha; FOLR1; Adult folatebinding protein
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Representative Drug(s) Pralatrexate Drug Info IC50 = 168 nM [1]
Co-Target Name Protein kinase C gamma (PRKCG) Successful Target
UniProt ID KPCG_HUMAN
Gene Name PRKCG
Synonyms
PRKCG; PKCG; PKC-gamma
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Representative Drug(s) LY333531 Drug Info IC50 = 300 nM Click to Show More [3]
2 LY333531 Drug Info IC50 = 300 nM [4]
Co-Target Name Protein kinase C alpha (PRKCA) Successful Target
UniProt ID KPCA_HUMAN
Gene Name PRKCA
Synonyms
Protein kinase C alpha type; PRKACA; PKCalpha; PKCA; PKC-alpha; PKC-A
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Representative Drug(s) LY333531 Drug Info IC50 = 360 nM Click to Show More [3]
2 LY333531 Drug Info IC50 = 360 nM [5]
Co-Target Name Protein kinase C epsilon (PRKCE) Successful Target
UniProt ID KPCE_HUMAN
Gene Name PRKCE
Synonyms
Protein kinase C epsilon type; PKCE; PKC epsilon; NPKC-epsilon
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Representative Drug(s) LY333531 Drug Info IC50 = 600 nM Click to Show More [6]
2 LY333531 Drug Info IC50 = 600 nM [3]
Co-Target Name Protein kinase C beta (PRKCB) Clinical trial Target
UniProt ID KPCB_HUMAN
Gene Name PRKCB
Synonyms
Protein kinase C beta type; PRKCB1; PKCB; PKC-beta; PKC-B
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Representative Drug(s) LY333531 Drug Info IC50 = 4.7 nM Click to Show More [3]
2 LY333531 Drug Info IC50 = 4.7 nM [4]
Co-Target Name Serine/threonine-protein kinase pim-1 (PIM1) Clinical trial Target
UniProt ID PIM1_HUMAN
Gene Name PIM1
Synonyms
Pim-1 proto-oncogene, serine/threonine kinase; PIM
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Representative Drug(s) LY333531 Drug Info IC50 = 200 nM [7]
Co-Target Name Protein kinase C delta (PRKCD) Clinical trial Target
UniProt ID KPCD_HUMAN
Gene Name PRKCD
Synonyms
nPKC-delta; Tyrosine-protein kinase PRKCD; SDK1; Protein kinase C delta type catalytic subunit; Protein kinase C delta type; PKC-delta
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Representative Drug(s) LY333531 Drug Info IC50 = 250 nM Click to Show More [6]
2 LY333531 Drug Info IC50 = 250 nM [3]
Co-Target Name Phosphoinositide dependent protein kinase-1 (PDPK1) Clinical trial Target
UniProt ID PDPK1_HUMAN
Gene Name PDPK1
Synonyms
PDK1; HPDK1; 3-phosphoinositide-dependent protein kinase 1; 3-Phosphoinositide-dependent kinase-1; 3'-phosphoinositide dependent kinase 1
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Representative Drug(s) LY333531 Drug Info IC50 = 750 nM [4]
Co-Target Name Protein kinase C eta (PRKCH) Co-Target
UniProt ID KPCL_HUMAN
Gene Name PRKCH
Synonyms
Protein kinase C eta type; PKC-L; nPKC-eta
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Representative Drug(s) LY333531 Drug Info IC50 = 52 nM Click to Show More [6]
2 LY333531 Drug Info IC50 = 52 nM [3]
References  Top
REF 1 Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor alpha and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis. J Med Chem. 2018 Mar 8;61(5):2027-40.
REF 2 Selective inhibitors of Candida albicans dihydrofolate reductase: activity and selectivity of 5-(arylthio)-2,4-diaminoquinazolines. J Med Chem. 1995 Sep 1;38(18):3608-16.
REF 3 Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. Bioorg Med Chem Lett. 2003 Jun 2;13(11):1857-9.
REF 4 Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition. Bioorg Med Chem. 2018 Aug 7;26(14):4209-24.
REF 5 Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors. J Med Chem. 2003 Sep 11;46(19):4021-31.
REF 6 (S)-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... J Med Chem. 1996 Jul 5;39(14):2664-71.
REF 7 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.

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