Target General Infomation
Target ID
T72335
Former ID
TTDR01027
Target Name
Lethal factor
Gene Name
lef
Synonyms
ALF; Anthrax lethal factor; Anthrax lethal toxin endopeptidase component; LF; lef
Target Type
Clinical Trial
Disease Bacillus anthracis infection [ICD10: A22]
Function
One of the three proteins composing the anthrax toxin, the agent which infects many mammalian species and that may cause death. LF is the lethal factor that, when associated with PA, causes death. LF is not toxic by itself. It is a protease that cleaves the N-terminal of most dual specificity mitogen-activated protein kinase kinases (MAPKKs or MAP2Ks) (except for MAP2K5). Cleavage invariably occurs within the N-terminal proline-rich region preceding the kinase domain, thus disrupting a sequence involved in directing specific protein-protein interactions necessary for the assembly of signaling complexes. There may be other cytosolic targets of LF involved in cytotoxicity. The proteasome may mediate a toxic process initiated by LF in the cell cytosol involving degradation of unidentified molecules that are essential for macrophage homeostasis. This is an early step in LeTx intoxication, but it is downstream of the cleavage by LF of MEK1 or other putative substrates.
BioChemical Class
Peptidase
Target Validation
T72335
UniProt ID
EC Number
EC 3.4.24.83
Sequence
MNIKKEFIKVISMSCLVTAITLSGPVFIPLVQGAGGHGDVGMHVKEKEKNKDENKRKDEE
RNKTQEEHLKEIMKHIVKIEVKGEEAVKKEAAEKLLEKVPSDVLEMYKAIGGKIYIVDGD
ITKHISLEALSEDKKKIKDIYGKDALLHEHYVYAKEGYEPVLVIQSSEDYVENTEKALNV
YYEIGKILSRDILSKINQPYQKFLDVLNTIKNASDSDGQDLLFTNQLKEHPTDFSVEFLE
QNSNEVQEVFAKAFAYYIEPQHRDVLQLYAPEAFNYMDKFNEQEINLSLEELKDQRMLAR
YEKWEKIKQHYQHWSDSLSEEGRGLLKKLQIPIEPKKDDIIHSLSQEEKELLKRIQIDSS
DFLSTEEKEFLKKLQIDIRDSLSEEEKELLNRIQVDSSNPLSEKEKEFLKKLKLDIQPYD
INQRLQDTGGLIDSPSINLDVRKQYKRDIQNIDALLHQSIGSTLYNKIYLYENMNINNLT
ATLGADLVDSTDNTKINRGIFNEFKKNFKYSISSNYMIVDINERPALDNERLKWRIQLSP
DTRAGYLENGKLILQRNIGLEIKDVQIIKQSEKEYIRIDAKVVPKSKIDTKIQEAQLNIN
QEWNKALGLPKYTKLITFNVHNRYASNIVESAYLILNEWKNNIQSDLIKKVTNYLVDGNG
RFVFTDITLPNIAEQYTHQDEIYEQVHSKGLYVPESRSILLHGPSKGVELRNDSEGFIHE
FGHAVDDYAGYLLDKNQSDLVTNSKKFIDIFKEEGSNLTSYGRTNEAEFFAEAFRLMHST
DHAERLKVQKNAPKTFQFINDQIKFIINS
Drugs and Mode of Action
Drug(s) IQ-DAA Drug Info Phase 1 Bacillus anthracis infection [547984]
GM6001 Drug Info Preclinical Discovery agent [544872]
Inhibitor 3-(2,5-dimethyl-1H-pyrrol-1-yl)benzoic acid Drug Info [528374]
GF-109203 Drug Info [528823]
GM6001 Drug Info [551393]
GNF-PF-600 Drug Info [527949]
MMI270 Drug Info [527922]
N,N'-Bis(4-Amino-2-Methylquinolin-6-Yl)Urea Drug Info [551393]
N,N-Dimethylsphingosine Drug Info [528823]
N-(3,4,5-trihydroxyphenethyl)oleamide Drug Info [528901]
N-(3,4-dihydroxybenzyl)oleamide Drug Info [529351]
N-(Sulfanylacetyl)Tyrosylprolylmethioninamide Drug Info [551393]
N-hydroxy-4-(2-oleamidoethyl)benzamide Drug Info [528901]
N-hydroxy-4-(oleamidomethyl)benzamide Drug Info [529351]
N-oleoyl-dopamine Drug Info [528901]
NSC-622445 Drug Info [528374]
Modulator IQ-DAA Drug Info
Pathways
Pathway Interaction Database Cellular roles of Anthrax toxin
Reactome Uptake and function of anthrax toxins
References
Ref 544872Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001387)
Ref 547984Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020942)
Ref 527922Bioorg Med Chem Lett. 2006 Feb 15;16(4):964-8. Epub 2005 Dec 9.The discovery of a potent and selective lethal factor inhibitor for adjunct therapy of anthrax infection.
Ref 527949J Med Chem. 2006 Jan 12;49(1):27-30.Anthrax lethal factor protease inhibitors: synthesis, SAR, and structure-based 3D QSAR studies.
Ref 528374J Med Chem. 2006 Aug 24;49(17):5232-44.Novel small-molecule inhibitors of anthrax lethal factor identified by high-throughput screening.
Ref 528823Antimicrob Agents Chemother. 2007 Jul;51(7):2403-11. Epub 2007 May 7.Amiodarone and bepridil inhibit anthrax toxin entry into host cells.
Ref 528901Bioorg Med Chem Lett. 2007 Aug 15;17(16):4575-8. Epub 2007 Jun 6.Inhibitors of anthrax lethal factor.
Ref 529351Bioorg Med Chem Lett. 2008 Apr 1;18(7):2467-70. Epub 2008 Feb 20.Inhibitors of anthrax lethal factor based upon N-oleoyldopamine.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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