Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T94309 | Target Info | |||
| Target Name | Pancreatic triacylglycerol lipase (PNLIP) | ||||
| Synonyms |
Pancreatic lipase; PTL; PL
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| Target Type | Successful Target | ||||
| Gene Name | PNLIP | ||||
| Biochemical Class | Carboxylic ester hydrolase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Lipoprotein lipase (LPL) | Successful Target | ||||
| UniProt ID | LIPL_HUMAN | |||||
| Gene Name | LPL | |||||
| Synonyms |
LIPD
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| Representative Drug(s) | Orlistat | Drug Info | IC50 = 66 nM | [1] | ||
| Co-Target Name | Cannabinoid receptor 1 (CB1) | Successful Target | ||||
| UniProt ID | CNR1_HUMAN | |||||
| Gene Name | CNR1 | |||||
| Synonyms |
Cannabinoid CB1 receptor; CNR; CB-R; CANN6
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| Representative Drug(s) | Orlistat | Drug Info | IC50 <= 100 nM | [2] | ||
| Co-Target Name | Fatty acid synthase (FASN) | Successful Target | ||||
| UniProt ID | FAS_HUMAN | |||||
| Gene Name | FASN | |||||
| Synonyms |
Yeast fatty acid synthase; Fatty-acyl-CoA synthase; Fatty acyl-CoA synthetase enzyme; FAS
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| Representative Drug(s) | Orlistat | Drug Info | Ki = 280 nM | [3] | ||
| Co-Target Name | Endothelial lipase (LIPG) | Clinical trial Target | ||||
| UniProt ID | LIPE_HUMAN | |||||
| Gene Name | LIPG | |||||
| Synonyms |
Endothelial cell-derived lipase; EL; EDL
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| Representative Drug(s) | Orlistat | Drug Info | IC50 = 6 nM | [1] | ||
| Co-Target Name | Platelet-activating factor acetylhydrolase (PLA2G7) | Clinical trial Target | ||||
| UniProt ID | PAFA_HUMAN | |||||
| Gene Name | PLA2G7 | |||||
| Synonyms |
gVIIA-PLA2; PAFAH; PAF acetylhydrolase; PAF 2-acylhydrolase; Lipoprotein-associated phospholipase A2; LDL-associated phospholipase A2; LDL-PLA(2); Group-VIIA phospholipase A2; 2-acetyl-1-alkylglycerophosphocholine esterase; 1-alkyl-2-acetylglycerophosphocholine esterase
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| Representative Drug(s) | Orlistat | Drug Info | IC50 = 50 nM | [4] | ||
| Co-Target Name | Diacylglycerol lipase alpha (DAGLA) | Patented-recorded Target | ||||
| UniProt ID | DGLA_HUMAN | |||||
| Gene Name | DAGLA | |||||
| Synonyms |
Sn1-specific diacylglycerol lipase alpha; Neural stem cell-derived dendrite regulator; NSDDR; KIAA0659; DGL-alpha; C11orf11
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| Representative Drug(s) | Orlistat | Drug Info | IC50 = 1 nM | [5] | ||
| Co-Target Name | Monoacylglycerol lipase ABHD6 (ABHD6) | Patented-recorded Target | ||||
| UniProt ID | ABHD6_HUMAN | |||||
| Gene Name | ABHD6 | |||||
| Synonyms |
Abhydrolase domain-containing protein 6; 2-arachidonoylglycerol hydrolase
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| Representative Drug(s) | Orlistat | Drug Info | IC50 = 13.18 nM | [6] | ||
| Co-Target Name | Diacylglycerol lipase beta (DAGLB) | Literature-reported Target | ||||
| UniProt ID | DGLB_HUMAN | |||||
| Gene Name | DAGLB | |||||
| Synonyms |
Sn1-specific diacylglycerol lipase beta; KCCR13L; DGL-beta
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| Representative Drug(s) | Orlistat | Drug Info | IC50 = 60 nM | [4] | ||
| Co-Target Name | Hepatic lipase (LIPC) | Co-Target | ||||
| UniProt ID | LIPC_HUMAN | |||||
| Gene Name | LIPC | |||||
| Synonyms |
Hepatic triacylglycerol lipase; HL; Lipase member C; Lysophospholipase; Phospholipase A1
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| Representative Drug(s) | Orlistat | Drug Info | IC50 = 3 nM | [1] | ||
| Co-Target Name | Phosphatidylserine lipase ABHD16A (ABHD16A) | Co-Target | ||||
| UniProt ID | ABHGA_HUMAN | |||||
| Gene Name | ABHD16A | |||||
| Synonyms |
Alpha/beta hydrolase domain-containing protein 16A; Abhydrolase domain-containing protein 16A; HLA-B-associated transcript 5; hBAT5; Monoacylglycerol lipase ABHD16A; Protein G5
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| Representative Drug(s) | Orlistat | Drug Info | IC50 = 30 nM | [4] | ||
| Co-Target Name | Monoacylglycerol lipase ABHD12 (ABHD12) | Co-Target | ||||
| UniProt ID | ABD12_HUMAN | |||||
| Gene Name | ABHD12 | |||||
| Synonyms |
Lysophosphatidylserine lipase ABHD12; 2-arachidonoylglycerol hydrolase ABHD12; Abhydrolase domain-containing protein 12; hABHD12; Oxidized phosphatidylserine lipase ABHD12
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| Representative Drug(s) | Orlistat | Drug Info | IC50 = 80 nM | [4] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Sulfonylated Benzothiazoles as Inhibitors of Endothelial Lipase. ACS Med Chem Lett. 2018 Nov 21;9(12):1263-1268. | ||||
| REF 2 | The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications. J Med Chem. 2005 Aug 11;48(16):5059-87. | ||||
| REF 3 | The lipogenesis pathway as a cancer target. J Med Chem. 2011 Aug 25;54(16):5615-38. | ||||
| REF 4 | Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5838-41. | ||||
| REF 5 | Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase. Bioorg Med Chem. 2016 Apr 1;24(7):1455-68. | ||||
| REF 6 | Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors. Bioorg Med Chem. 2015 Oct 1;23(19):6335-45. | ||||
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