Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T70508 Target Info
Target Name Cyclin-dependent kinase (CDK)
Synonyms
Cyclin dependent kinase
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Target Type Clinical trial Target
Gene Name NO-GeName
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
Co-Target Name Fms-like tyrosine kinase 3 (FLT-3) Successful Target
UniProt ID FLT3_HUMAN
Gene Name FLT3
Synonyms
Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
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Representative Drug(s) TG02 Drug Info IC50 = 21 nM [1]
Co-Target Name Janus kinase 2 (JAK-2) Successful Target
UniProt ID JAK2_HUMAN
Gene Name JAK2
Synonyms
Tyrosine-protein kinase JAK2
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Representative Drug(s) TG02 Drug Info IC50 = 73 nM [1]
Co-Target Name Glycogen synthase kinase-3 alpha (GSK-3A) Successful Target
UniProt ID GSK3A_HUMAN
Gene Name GSK3A
Synonyms
Serine/threonineprotein kinase GSK3A; Serine/threonine-protein kinase GSK3A; Glycogen synthase kinase3 alpha; Glycogen synthase kinase 3; GSK3 alpha; GSK-3 alpha; GSK-3
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Representative Drug(s) Flavopiridol Drug Info IC50 = 280 nM [2]
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) Flavopiridol Drug Info IC50 = 480 nM [3]
Co-Target Name Debrisoquine 4-hydroxylase (CYP2D6) Successful Target
UniProt ID CP2D6_HUMAN
Gene Name CYP2D6
Synonyms
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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Representative Drug(s) TG02 Drug Info IC50 = 950 nM [4]
Co-Target Name Glycogen synthase kinase-3 beta (GSK-3B) Clinical trial Target
UniProt ID GSK3B_HUMAN
Gene Name GSK3B
Synonyms
Serine/threonine-protein kinase GSK3B; GSK-3 beta
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Representative Drug(s) Flavopiridol Drug Info IC50 = 280 nM [2]
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) Flavopiridol Drug Info IC50 = 890 nM [3]
Co-Target Name Glycogen phosphorylase muscle form (GP) Patented-recorded Target
UniProt ID PYGM_HUMAN
Gene Name PYGM
Synonyms
Muscle glycogen phosphorylase; Glycogen phosphorylase, muscle form; Glycogen phosphorylase b
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Representative Drug(s) Flavopiridol Drug Info IC50 = 1000 nM [5]
Co-Target Name La-related protein 7 (LARP7) Co-Target
UniProt ID LARP7_HUMAN
Gene Name LARP7
Synonyms
La ribonucleoprotein domain family member 7; hLARP7; P-TEFb-interaction protein for 7SK stability; PIP7S
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Representative Drug(s) Flavopiridol Drug Info Ki = 3 nM [6]
Co-Target Name Cyclin dependent kinase 2-G1/S specific cyclin E complex (CDK2-CCNE) Co-Target
UniProt ID CDK2_HUMAN-CCNE1_HUMAN/CCNE2_HUMAN
Gene Name CDK2-CCNE1/CCNE2
Representative Drug(s) R-roscovitine Drug Info IC50 = 100 nM Click to Show More [7]
2 Flavopiridol Drug Info IC50 = 170 nM [8]
References  Top
REF 1 Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. J Med Chem. 2016 Oct 13;59(19):8667-84.
REF 2 Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. J Med Chem. 2005 Feb 10;48(3):737-43.
REF 3 Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem. 2002 Aug 29;45(18):3905-27.
REF 4 Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer. J Med Chem. 2012 Jan 12;55(1):169-96.
REF 5 Identification, synthesis, and characterization of new glycogen phosphorylase inhibitors binding to the allosteric AMP site. J Med Chem. 2004 Jul 1;47(14):3537-45.
REF 6 A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. Bioorg Med Chem. 2019 Mar 1;27(5):677-685.
REF 7 Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1. Cancer Res. 2005 Jun 15;65(12):5399-407.
REF 8 Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2973-7.

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