Results 1 to 10 of about 467 (80)
Side-chain dynamics of the α1B -adrenergic receptor determined by NMR via methyl relaxation. [PDF]
Protein Sci, 2023 Abstract G protein‐coupled receptors (GPCRs) are medically important membrane proteins that sample inactive, intermediate, and active conformational states characterized by relatively slow interconversions (~μs–ms). On a faster timescale (~ps–ns), the conformational landscape of GPCRs is governed by the rapid dynamics of amino acid side chains.
Baumann C +8 more
europepmc +2 more sources
The macrocycle inhibitor landscape of SLC-transporter. [PDF]
Mol InformAbstract In the past years the interest in Solute Carrier Transporters (SLC) has increased due to their potential as drug targets. At the same time, macrocycles demonstrated promising activities as therapeutic agents. However, the overall macrocycle/SLC‐transporter interaction landscape has not been fully revealed yet.
Granulo N, Sosnin S, Digles D, Ecker GF.
europepmc +2 more sources
Usage of Cell-Free Protein Synthesis in Post-Translational Modification of μ-Conopeptide PIIIA [PDF]
Marine Drugs, 2023 Liu Y +5 more
exaly +2 more sources
Single-Disulfide Conopeptide Czon1107, an Allosteric Antagonist of the Human α3β4 Nicotinic Acetylcholine Receptor [PDF]
Marine Drugs, 2022 Mengke Yang +2 more
exaly +2 more sources
The Conopeptide αD-FrXXA, an Inhibitor of Voltage-Gated Potassium Channels [PDF]
Marine DrugsEstuardo Lopez-Vera
exaly +2 more sources
A Chemoenzymatic Approach To Produce a Cyclic Analogue of the Analgesic Drug MVIIA (Ziconotide)
Angewandte Chemie, Volume 135, Issue 29, July 17, 2023., 2023 A chemoenzymatic method has been developed to prepare backbone cyclic analogues of the ω‐conotoxin MVIIA. The most potent cyclic analogue, cM‐7, shows highly improved stability and maintains the activity of the native peptide. Abstract Ziconotide (ω‐conotoxin MVIIA) is an approved analgesic for the treatment of chronic pain.
Yan Zhou +8 more
wiley +2 more sources
High‐resolution crystal structure of the Mu8.1 conotoxin from Conus mucronatus
Acta Crystallographica Section F, Volume 79, Issue 9, Page 240-246, September 2023., 2023 The crystal structure of the Mu8.1 conotoxin was determined in the high‐symmetry space group I4122 at 1.67 Å resolution. This crystal structure reveals a surface‐exposed Zn2+‐binding site and establishes a hydrogen‐bonding network around Lys55 buried at the dimer interface.Marine cone snails produce a wealth of peptide toxins (conotoxins) that bind ...
Emilie Müller +3 more
wiley +1 more source
Journal of Cellular and Molecular Medicine, Volume 26, Issue 20, Page 5330-5334, October 2022., 2022 Abstract Conotoxins are promising neuropharmacological tools and drug candidates due to their high efficiency and specificity in targeting ion channels or neurotransmitter receptors. In this study, a novel O2‐superfamily conotoxin, Lt7b, was synthesized and its pharmacological functions were evaluated.
Yun Wu +4 more
wiley +1 more source
Discovery of KV1.3 ion channel inhibitors: Medicinal chemistry approaches and challenges
Medicinal Research Reviews, Volume 41, Issue 4, Page 2423-2473, July 2021., 2021 Abstract The KV1.3 voltage‐gated potassium ion channel is involved in many physiological processes both at the plasma membrane and in the mitochondria, chiefly in the immune and nervous systems. Therapeutic targeting KV1.3 with specific peptides and small molecule inhibitors shows great potential for treating cancers and autoimmune diseases, such as ...
Špela Gubič +9 more
wiley +1 more source
Engineered biosynthesis of cyclotides
New Zealand Journal of Botany, Volume 58, Issue 4, Page 358-377, December 2020., 2020 ABSTRACT A system based on cyanobacterial split inteins, SICLOPPs (Split Intein Circular Ligation of Proteins and Peptides), has been used to synthesise a small natively cyclic plant protein, kalata B1, and cyclised versions of the natively linear therapeutic peptides ziconotide and leconotide.
Thomas N. G. Handley +8 more
wiley +1 more source