Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T52227 Target Info
Target Name Candida Thymidylate synthase (Candi TMP1)
Synonyms
Tsase of Candida albicans; TS of Candida albicans; TMP1; Human recombinant thymidylate synthase; HrTS
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Target Type Successful Target
Gene Name Candi TMP1
Biochemical Class Methyltransferase
UniProt ID
TYSY_CANAL
Co-Targets of This Target  Top
Co-Target Name DNA topoisomerase II beta (TOP2B) Successful Target
UniProt ID TOP2B_HUMAN
Gene Name TOP2B
Synonyms
Topo IIbeta; TOP2beta; TOP2B
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Representative Drug(s) Ciprofloxacin XR Drug Info IC50 = 0.3 ug.mL-1 [1]
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) Raltitrexed Drug Info IC50 = 6.3 nM Click to Show More [2]
2 Drug Info IC50 = 23.8 nM [4]
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) Drug Info Ki = 7 nM [3]
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) Drug Info IC50 = 8.3 nM Click to Show More [4]
2 Raltitrexed Drug Info IC50 = 99.5 nM [2]
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) Raltitrexed Drug Info IC50 = 15 nM Click to Show More [5]
2 Drug Info IC50 = 42 nM [4]
Co-Target Name DNA topoisomerase II (TOP2) Successful Target
UniProt ID TOP2A_HUMAN; TOP2B_HUMAN
Gene Name TOP2A; TOP2B
Synonyms
TOP2; DNA topoisomerase 2
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Representative Drug(s) Ciprofloxacin XR Drug Info EC50 = 30 nM [6]
Co-Target Name Glycinamide ribonucleotide formyltransferase (GART) Clinical trial Target
UniProt ID PUR2_HUMAN
Gene Name GART
Synonyms
Trifunctional purine biosynthetic protein adenosine-3; PRGS; PGFT
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Representative Drug(s) Drug Info IC50 = 11.74 nM [7]
Co-Target Name Thymidylate synthase (TYMS) Literature-reported Target
UniProt ID TYSY_HUMAN
Gene Name TYMS
Synonyms
TSase; TS
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Representative Drug(s) Drug Info Ki = 1.3 nM Click to Show More [8]
2 Nolatrexed Drug Info Ki = 15 nM [9]
3 Raltitrexed Drug Info IC50 = 260 nM [10]
Co-Target Name Folate receptor beta (FOLR2) Literature-reported Target
UniProt ID FOLR2_HUMAN
Gene Name FOLR2
Synonyms
Placental folate-binding protein; Folate receptor, fetal/placental; Folate receptor type-beta; Folate receptor 2; FR-beta; FOLR2
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Representative Drug(s) Raltitrexed Drug Info IC50 = 22 nM Click to Show More [2]
2 Drug Info IC50 = 60 nM [4]
Co-Target Name Thymidylate synthase/GAR transformylase/AICAR transformylase (TYMS/GAR/TATIC) Co-Target
UniProt ID TYSY_HUMAN; PUR2_HUMAN; PUR9_HUMAN
Gene Name TYMS; GART; ATIC
Synonyms
Tsase; PRGS; PURH
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Representative Drug(s) Drug Info IC50 = 70 nM [11]
References  Top
REF 1 Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative. J Med Chem. 1988 Sep;31(9):1694-7.
REF 2 Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors alpha and beta and the proton-coupled folate transporter. J Med Chem. 2014 Oct 9;57(19):8152-66.
REF 3 Synthesis of classical, four-carbon bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates. J Med Chem. 2005 Aug 11;48(16):5329-36.
REF 4 Fluorine-Substituted Pyrrolo[2,3- d]Pyrimidine Analogues with Tumor Targeting 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 May 10;61(9):4228-4248.
REF 5 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 6 3-benzyl-quinolones: Novel, potent inhibitors of mammalian topoisomerase II. Bioorg Med Chem Lett. 1995 May 4;5(9):1021-6.
REF 7 Novel 5-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase and as potential antitumor agents. J Med Chem. 2015 Feb 12;58(3):1479-93.
REF 8 Novel approaches for targeting thymidylate synthase to overcome the resistance and toxicity of anticancer drugs. J Med Chem. 2010 Sep 23;53(18):6539-49.
REF 9 Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones. J Med Chem. 1993 Mar 19;36(6):733-46.
REF 10 Synthesis and antiproliferative activity of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline. Eur J Med Chem. 2013 Jun;64:401-9.
REF 11 Novel 6-substituted benzoyl and non-benzoyl straight chain pyrrolo[2,3-d]pyrimidines as potential antitumor agents with multitargeted inhibition of TS, GARFTase and AICARFTase. Eur J Med Chem. 2017 Oct 20;139:531-541.

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