Co-Target(s) Information
Target General Information | Top | ||||
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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 |
Co-Targets of This Target | Top | |||||
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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 | Pemetrexed | 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) | Pemetrexed | 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) | Pemetrexed | 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 | Pemetrexed | 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) | Pemetrexed | 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) | Pemetrexed | 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 | Pemetrexed | 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) | Pemetrexed | Drug Info | IC50 = 70 nM | [11] |
References | Top | ||||
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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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