Loop2 Size Modification Reveals Significant Impacts on the Potency of α-Conotoxin TxID [PDF]
α4/6-conotoxin TxID, which was identified from Conus textile, simultaneously blocks rat (r) α3β4 and rα6/α3β4 nicotinic acetylcholine receptors (nAChRs) with IC50 values of 3.6 nM and 33.9 nM, respectively.
Jianying Dong +7 more
doaj +2 more sources
α-Conotoxin TxIB Inhibits Development of Morphine-Induced Conditioned Place Preference in Mice via Blocking α6β2* Nicotinic Acetylcholine Receptors [PDF]
Morphine, the main component of opium, is a commonly used analgesic in clinical practice, but its abuse potential limits its clinical application. Nicotinic acetylcholine receptors (nAChRs) in the mesolimbic circuitry play an important role in the ...
Xiaodan Li +6 more
doaj +2 more sources
Synthesis, Structural and Pharmacological Characterizations of CIC, a Novel α-Conotoxin with an Extended N-Terminal Tail [PDF]
Cone snails are venomous marine predators that rely on fast-acting venom to subdue their prey and defend against aggressors. The conotoxins produced in the venom gland are small disulfide-rich peptides with high affinity and selectivity for their ...
Julien Giribaldi +7 more
doaj +2 more sources
A 4/8 Subtype α-Conotoxin Vt1.27 Inhibits N-Type Calcium Channels With Potent Anti-Allodynic Effect [PDF]
A novel 4/8 subtype α-conotoxin, Vt1.27 (NCCMFHTCPIDYSRFNC-NH2), was identified from Conus vitulinus in the South China Sea by RACE methods. The peptide was synthesized and structurally characterized.
Shuo Wang +16 more
doaj +2 more sources
Stapling Cysteine[2,4] Disulfide Bond of α-Conotoxin LsIA and Its Potential in Target Delivery [PDF]
α-Conotoxins, as selective nAChR antagonists, can be valuable tools for targeted drug delivery and fluorescent labeling, while conotoxin-drug or conotoxin-fluorescent conjugates through the disulfide bond are rarely reported.
Xin Sun +6 more
doaj +2 more sources
Unique Pharmacological Properties of α-Conotoxin OmIA at α7 nAChRs [PDF]
OmIA, isolated from Conus omaria venom, is a potent antagonist at α7 nAChRs. We determined the co-crystal structure of OmIA with Lymnae stagnalis acetylcholine binding protein (Ls-AChBP) that identified His5, Val10 and Asn11 as key determinants for the ...
Thao N.T. Ho +2 more
doaj +2 more sources
Cysteine [2,4] Disulfide Bond as a New Modifiable Site of α-Conotoxin TxIB [PDF]
α-Conotoxin TxIB, a selective antagonist of α6/α3β2β3 nicotinic acetylcholine receptor, could be a potential therapeutic agent for addiction and Parkinson’s disease.
Baojian Zhang +8 more
doaj +2 more sources
Rigidity of loop 1 contributes to equipotency of globular and ribbon isomers of α-conotoxin AusIA [PDF]
α-Conotoxins are small disulfide-rich peptides targeting nicotinic acetylcholine receptors (nAChRs) characterised by a CICII-Xm-CIII-Xn-CIV framework that invariably adopt the native globular conformations which is typically most potent. α-Conotoxins are
Thao N. T. Ho +2 more
doaj +2 more sources
Programmed Aptamer Screening, Characterization, and Rapid Detection for α-Conotoxin MI [PDF]
Conotoxins (CTXs) are a variety of mixed polypeptide toxins, among which α-conotoxin MI (CTX-MI) is the most toxic. Serious toxic symptoms, a lack of counteracting drugs, and cumbersome detection processes have made CTX-MI a hidden danger for humans. One
Han Guo +10 more
doaj +2 more sources
Degradation kinetics of α‐conotoxin TxID [PDF]
α‐Conotoxin (CTx) TxID is a potent α3β4 nicotinic acetylcholine receptor (nAChR) antagonist that has been suggested as a potential drug candidate to treat addiction and small cell lung cancer.
Pan Xu +6 more
doaj +2 more sources

