Target Information
| Target General Information | Top | |||||
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| Target ID |
T01943
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| Target Name |
Plasmodium Beta-hydroxyacyl-ACP dehydratase (Malaria FabZ)
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| Synonyms |
fabZ; Fatty acid synthesis protein; Beta-hydroxyacyl-ACP dehydratase; 17 kDa actomyosin component; (3R)-hydroxymyristoyl-[acyl-carrier-protein] dehydratase; (3R)-hydroxymyristoyl-ACP dehydrase
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| Gene Name |
Malaria FabZ
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Hepatic fibrosis/cirrhosis [ICD-11: DB93] | |||||
| Function |
Involved in unsaturated fatty acids biosynthesis. Catalyzes the dehydration of short chain beta-hydroxyacyl-ACPs and long chain saturated and unsaturated beta-hydroxyacyl-ACPs.
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| UniProt ID | ||||||
| Sequence |
MRFLIIHIAVIVLPFVLMIDVKRENSFFLRHSPKRLYKKADYNNMYDKIIKKQQNRIYDV
SSQINQDNINGQNISFNLTFPNYDTSIDIEDIKKILPHRYPFLLVDKVIYMQPNKTIIGL KQVSTNEPFFNGHFPQKQIMPGVLQIEALAQLAGILCLKSDDSQKNNLFLFAGVDGVRWK KPVLPGDTLTMQANLISFKSSLGIAKLSGVGYVNGKVVINISEMTFALSK Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | Epigallocatechin gallate | Drug Info | Phase 3 | Hepatic fibrosis | [2], [3], [4], [5] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 7 Inhibitor drugs | + | ||||
| 1 | Epigallocatechin gallate | Drug Info | [6] | |||
| 2 | (-)-CATECHINGALLATE | Drug Info | [6] | |||
| 3 | 2-Hexadecynoic acid | Drug Info | [7] | |||
| 4 | 3,7,3',4'-TETRAHYDROXYFLAVONE | Drug Info | [6] | |||
| 5 | biochanin A | Drug Info | [6] | |||
| 6 | GALLOCATECHIN GALLATE | Drug Info | [6] | |||
| 7 | MORIN | Drug Info | [6] | |||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Similarity Proteins
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There is no similarity protein (E value < 0.005) for this target
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| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Fatty acid biosynthesis | |||||
| 2 | Biotin metabolism | |||||
| 3 | Metabolic pathways | |||||
| 4 | Fatty acid metabolism | |||||
| References | Top | |||||
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| REF 1 | Antiplasmodial drug targets: a patent review (2000 - 2013).Expert Opin Ther Pat. 2016;26(1):107-30. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7002). | |||||
| REF 3 | The green tea polyphenol (2)-epigallocatechin-3-gallate (EGCG) is not a beta-secretase inhibitor. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1408-14. | |||||
| REF 4 | Epigallocatechin gallate modulates CYP450 isoforms in the female Swiss-Webster mouse. Toxicol Sci. 2003 Dec;76(2):262-70. | |||||
| REF 5 | Prolyl endopeptidase inhibitors from green tea. Arch Pharm Res. 2001 Aug;24(4):292-6. | |||||
| REF 6 | Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. J Med Chem. 2006 Jun 1;49(11):3345-53. | |||||
| REF 7 | 2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections. Bioorg Med Chem. 2010 Nov 1;18(21):7475-85. | |||||
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