Site-directed mutagenesis of the toxin from the Chinese scorpion Buthus martensii Karsch (BmKAS): insight into sites related to analgesic activity.
This study utilized the E. coli expression system to investigate the role of amino acid residues in toxin from the Chinese scorpion--Buthus martensii Karsch (BmKAS). To evaluate the extent to which residues of the toxin core contribute to its analgesic activity, ten mutants of BmKAS were obtained by PCR. Using site-directed mutagenesis, all of these residues were substituted with different amino acids. This study represents a thorough mapping and elucidation of the epitopes that form the molecular basis of the toxin's analgesic activity. Our results showed large mutant-dependent differences that emphasize the important roles of the studied residues.
School of Life Science and Bio-Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, Liaoning Province, China.
Yong
Y
Cui
Yong-Bo
YB
Song
Lin
L
Ma
Yan-Feng
YF
Liu
Guo-Dong
GD
Li
Chun-Fu
CF
Wu
Jing-Hai
JH
Zhang
D018712:Analgesics, Non-Narcotic / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D019476:Insect Proteins / Q000737:chemistry* / Q000235:genetics / Q000494:pharmacology*; D051379:Mice; D008958:Models, Molecular; D016297:Mutagenesis, Site-Directed; D050505:Mutant Proteins / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D009498:Neurotoxins / Q000737:chemistry / Q000235:genetics / Q000494:pharmacology; D010147:Pain Measurement; D010455:Peptides / Q000737:chemistry* / Q000235:genetics / Q000494:pharmacology*; D011487:Protein Conformation; D025941:Protein Interaction Mapping; D017434:Protein Structure, Tertiary; D011994:Recombinant Proteins / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D012604:Scorpion Venoms / Q000737:chemistry* / Q000235:genetics / Q000494:pharmacology*; D012605:Scorpions / Q000378:metabolism*; D016415:Sequence Alignment; D017386:Sequence Homology, Amino Acid; D013329:Structure-Activity Relationship
D018712:Analgesics, Non-Narcotic; D019476:Insect Proteins; C556310:KAS toxin, Buthus martensi Karsch; C076349:LqhIT2 insect toxin; D050505:Mutant Proteins; D009498:Neurotoxins; D010455:Peptides; D011994:Recombinant Proteins; D012604:Scorpion Venoms