Ligand-based peptide design and combinatorial peptide libraries to target G protein-coupled receptors. Curr Pharm Des. 16(28):3071-88 (2010).Gruber CW, Muttenthaler M, Freissmuth M 2010. Ligand-based peptide design and combinatorial peptide libraries to target G protein-coupled receptors . Curr...
Synthesis and pharmacokinetic characterisation of a fluorine-18 labelled brain shuttle peptide fusion dimeric affibody Article Open access 28 January 2021 Human biodistribution and radiation dosimetry of two novel α-synuclein PET tracers, 18F-SPAL-T-06 and 18F-C05-05 Article Open access 13 March...
Subsequently, we introduced a 10-aa peptide derived from Myc (EQKLISEEDL) at the N- or C-terminus of the extracellular domains of APRIL and BAFF, creating four constructs: Myc-APRIL, ARPIL-Myc, Myc-BAFF and BAFF-Myc (Fig. 1a). These proteins were purified to greater than 95% purity,...
(Supplementary Fig.1and Supplementary Table1). Subsequently, we introduced a 10-aa peptide derived from Myc (EQKLISEEDL) at the N- or C-terminus of the extracellular domains of APRIL and BAFF, creating four constructs: Myc-APRIL, ARPIL-Myc, Myc-BAFF and BAFF-Myc (Fig.1a). These ...
(+)-7-iso-jasmonoyl-L-isoleucine (JA-Ile) is a plant hormone involved in plant development and stress response that signals through a COI1–JAZ co-receptor complex. Structure-guided design led to the identification of a coronatine derivative that antagon
validation and analysis. The platform uses the open-source cheminformatics toolkit RDKit to calculate fingerprints and similarities, but through the three-stage design data generated by other sources can easily be fed in at the validation or analysis stages. The platform with its compound and traini...
Fig. 1: Rational crystallography-guided design of small-molecule ligands targeting the SH2 domain of SOCS2. a Crystal structure of SOCS2 in complex with bound EpoR peptide (yellow carbons, PDB: 6I4X). SOCS2 residues participating in hydrophobic interactions with the substrate peptide are highligh...
(Bio Basic Inc.) and subcloned into a modified pLVX lentiviral expression vector (Addgene) using the SpeI and NdeI restriction enzyme sites. The pLVX vector backbone was modified to co-express GFP downstream of the BAFF-CAR construct, separated by a tandem P2A/T2A self-cleaving peptide ...
as experimentally co-crystallized in ligand–protein complexes from the Protein Data Bank (PDB) [49] and were therefore selected to compile a training set (TR, Table1, Supporting Information Table SI1). All TR compounds were reported as covalent inhibitors characterized by either a peptide or a...
The recently discovered fourth member of the opioid receptor family, the nociceptin receptor (NOP) and its endogenous ligand, the heptadecapeptide nociceptin, are involved in several central nervous system pathways, such as nociception, reward, tolerance, and feeding. The discovery of small-molecule ...