AON_AZEFE
ID AON_AZEFE Reviewed; 21 AA.
AC B3EWH2;
DT 09-JAN-2013, integrated into UniProtKB/Swiss-Prot.
DT 09-JAN-2013, sequence version 1.
DT 25-MAY-2022, entry version 17.
DE RecName: Full=Azemiopsin {ECO:0000303|PubMed:22613724};
OS Azemiops feae (Fea's viper).
OC Eukaryota; Metazoa; Chordata; Craniata; Vertebrata; Euteleostomi;
OC Lepidosauria; Squamata; Bifurcata; Unidentata; Episquamata; Toxicofera;
OC Serpentes; Colubroidea; Viperidae; Azemiopinae; Azemiops.
OX NCBI_TaxID=8773;
RN [1] {ECO:0000305}
RP PROTEIN SEQUENCE, FUNCTION, SUBUNIT, MASS SPECTROMETRY, TOXIC DOSE, AND
RP MUTAGENESIS OF ASP-1; ASN-2; TRP-3; TRP-4; PRO-5; LYS-6; PRO-7; PRO-8;
RP HIS-9; GLN-10; GLY-11; PRO-12; ARG-13; PRO-14; PRO-15; ARG-16; PRO-17;
RP ARG-18; PRO-19; LYS-20 AND PRO-21.
RC TISSUE=Venom {ECO:0000269|PubMed:22613724};
RX PubMed=22613724; DOI=10.1074/jbc.m112.363051;
RA Utkin Y.N., Weise C., Kasheverov I.E., Andreeva T.V., Kryukova E.V.,
RA Zhmak M.N., Starkov V.G., Hoang N.A., Bertrand D., Ramerstorfer J.,
RA Sieghart W., Thompson A.J., Lummis S.C., Tsetlin V.I.;
RT "Azemiopsin from Azemiops feae viper venom, a novel polypeptide ligand of
RT nicotinic acetylcholine receptor.";
RL J. Biol. Chem. 287:27079-27086(2012).
CC -!- FUNCTION: In vitro, reversibly blocks human muscle-type nicotinic
CC acetylcholine receptors (nAChR) alpha-1-beta-1-epsilon-delta/CHRNA1-
CC CHRNB1-CHRNE-CHRND (EC(50)=0.44 uM) and alpha-1-beta-1-gamma-
CC delta/CHRNA1-CHRNB1-CHRNG-CHRND (EC(50)=1.56 uM). Binds to nAChR from
CC T.californica (IC(50)=0.03-0.18 uM), human neuronal nAChR alpha-
CC 7/CHRNA7 (IC(50)=22 uM) and acetylcholine-binding proteins (AChBP) from
CC L.stagnalis (IC(50)=63 uM) and A.californica (IC(50)=230 uM).
CC {ECO:0000269|PubMed:22613724}.
CC -!- SUBUNIT: Monomer. {ECO:0000269|PubMed:22613724}.
CC -!- SUBCELLULAR LOCATION: Secreted {ECO:0000305}.
CC -!- TISSUE SPECIFICITY: Expressed by the venom gland. {ECO:0000305}.
CC -!- MASS SPECTROMETRY: Mass=2540.3; Method=MALDI;
CC Evidence={ECO:0000269|PubMed:22613724};
CC -!- TOXIC DOSE: LD(50) is 2.6 mg/kg by intraperitoneal injection in mice.
CC {ECO:0000269|PubMed:22613724}.
CC -!- MISCELLANEOUS: Has no effect on GABA(A) receptors alpha-1-beta-3-gamma-
CC 2/GABRA1-GABRB3-GABRG2 and alpha-2-beta-3-gamma-2/GABRA2-GABRB3-GABRG2
CC or on receptors HTR3A and HTR3A-HTR3B. {ECO:0000305|PubMed:22613724}.
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DR AlphaFoldDB; B3EWH2; -.
DR GO; GO:0005576; C:extracellular region; IEA:UniProtKB-SubCell.
DR GO; GO:0030550; F:acetylcholine receptor inhibitor activity; IEA:UniProtKB-KW.
DR GO; GO:0099106; F:ion channel regulator activity; IEA:UniProtKB-KW.
DR GO; GO:0090729; F:toxin activity; IEA:UniProtKB-KW.
PE 1: Evidence at protein level;
KW Acetylcholine receptor inhibiting toxin; Direct protein sequencing;
KW Ion channel impairing toxin; Neurotoxin; Postsynaptic neurotoxin; Secreted;
KW Toxin.
FT PEPTIDE 1..21
FT /note="Azemiopsin"
FT /evidence="ECO:0000269|PubMed:22613724"
FT /id="PRO_0000420621"
FT REGION 1..21
FT /note="Disordered"
FT /evidence="ECO:0000256|SAM:MobiDB-lite"
FT REGION 3..6
FT /note="Implicated in receptor binding"
FT /evidence="ECO:0000269|PubMed:22613724"
FT REGION 8..11
FT /note="Implicated in receptor binding"
FT /evidence="ECO:0000269|PubMed:22613724"
FT REGION 13..14
FT /note="Implicated in receptor binding"
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 1
FT /note="D->A: No effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 2
FT /note="N->A: No effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 3
FT /note="W->A: Moderate effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 4
FT /note="W->A: Severe effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 5
FT /note="P->A: Severe effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 6
FT /note="K->A: Severe effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 7
FT /note="P->A: No effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 8
FT /note="P->A: Complete loss of binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 9
FT /note="H->A: Complete loss of binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 10
FT /note="Q->A: Severe effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 11
FT /note="G->A: Severe effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 12
FT /note="P->A: No effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 13
FT /note="R->A: Severe effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 14
FT /note="P->A: Moderate effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 15
FT /note="P->A: No effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 16
FT /note="R->A: Moderate effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 17
FT /note="P->A: No effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 18
FT /note="R->A: No effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 19
FT /note="P->A: No effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 20
FT /note="K->A: No effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
FT MUTAGEN 21
FT /note="P->A: No effect on binding to nAChR from
FT T.californica."
FT /evidence="ECO:0000269|PubMed:22613724"
SQ SEQUENCE 21 AA; 2541 MW; B1A965ECE448823F CRC64;
DNWWPKPPHQ GPRPPRPRPK P