Piotr Kossoń
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View article: Chirality and Rigidity in Triazole-Modified Peptidomimetics Interacting with Neuropilin-1
Chirality and Rigidity in Triazole-Modified Peptidomimetics Interacting with Neuropilin-1 Open
The interaction of Neuropilin-1 (NRP-1) with vascular endothelial growth factor (VEGF) has been shown to promote angiogenesis under physiological and pathological conditions. Angiogenesis around tumors is a major factor allowing for their …
View article: Stapling of leu-enkephalin analogs with bifunctional reagents for prolonged analgesic activity
Stapling of leu-enkephalin analogs with bifunctional reagents for prolonged analgesic activity Open
The design and synthesis of leu-enkephalin analogs by replacing the glycine residues with N -(2-thioethyl)glycines and opening the cyclisation potential is presented.
View article: Gαi-derived peptide binds the µ-opioid receptor
Gαi-derived peptide binds the µ-opioid receptor Open
Background G protein-coupled receptors (GPCRs) transduce external stimuli into the cell by G proteins via an allosteric mechanism. Agonist binding to the receptor stimulates GDP/GTP exchange within the heterotrimeric G protein complex, whe…
View article: In Vivo, In Vitro and In Silico Studies of the Hybrid Compound AA3266, an Opioid Agonist/NK1R Antagonist with Selective Cytotoxicity
In Vivo, In Vitro and In Silico Studies of the Hybrid Compound AA3266, an Opioid Agonist/NK1R Antagonist with Selective Cytotoxicity Open
AA3266 is a hybrid compound consisting of opioid receptor agonist and neurokinin-1 receptor (NK1R) antagonist pharmacophores. It was designed with the desire to have an analgesic molecule with improved properties and auxiliary anticancer a…
View article: Antinociceptive and Cytotoxic Activity of Opioid Peptides with Hydrazone and Hydrazide Moieties at the C-Terminus
Antinociceptive and Cytotoxic Activity of Opioid Peptides with Hydrazone and Hydrazide Moieties at the C-Terminus Open
In the present contribution, we analyze the influence that C-terminal extension of short opioid peptide sequences by organic fragments has on receptor affinity, in vivo analgesic activity, and antimelanoma properties. The considered fragme…
View article: β2-Homo-Amino Acid Scan of µ-Selective Opioid Tetrapeptide TAPP
β2-Homo-Amino Acid Scan of µ-Selective Opioid Tetrapeptide TAPP Open
TAPP (H-Tyr-d-Ala-Phe-Phe-NH2) is a potent, µ-selective opioid ligand. In order to gain further insights into pharmacophoric features of this tetrapeptide, we have performed a β2-Homo-amino acid (β2hAA) scan of the TAPP sequence. To this a…
View article: Evaluation of Receptor Affinity, Analgesic Activity and Cytotoxicity of a Hybrid Peptide, AWL3020
Evaluation of Receptor Affinity, Analgesic Activity and Cytotoxicity of a Hybrid Peptide, AWL3020 Open
In the present contribution we report design, synthesis and evaluation of receptor affinity, analgesic activity and cytotoxicity of a hybrid peptide, AWL3020. The peptide includes two pharmacophores, one of δ-opioid receptor (δOR) agonists…
View article: Can keratin scaffolds be used for creating three-dimensional cell cultures?
Can keratin scaffolds be used for creating three-dimensional cell cultures? Open
Three-dimensional (3D) cell cultures were created with the use of fur keratin associated proteins (F-KAPs) as scaffolds. The procedure of preparation F-KAP involves combinations of chemical activation and enzymatic digestion. The best resu…
View article: Gα<sub>i</sub>-derived peptide binds the µ-opioid receptor
Gα<sub>i</sub>-derived peptide binds the µ-opioid receptor Open
G protein-coupled receptors (GPCRs) transduce external stimuli into the cell by G proteins via an allosteric mechanism. Agonist binding to the receptor stimulates GDP/GTP exchange within the heterotrimeric G protein complex. Whereas recent…
View article: Fentanyl Family at the Mu-Opioid Receptor: Uniform Assessment of Binding and Computational Analysis
Fentanyl Family at the Mu-Opioid Receptor: Uniform Assessment of Binding and Computational Analysis Open
Interactions of 21 fentanyl derivatives with μ-opioid receptor (μOR) were studied using experimental and theoretical methods. Their binding to μOR was assessed with radioligand competitive binding assay. A uniform set of binding affinity d…
View article: High-Titre Neutralizing Antibodies to H1N1 Influenza Virus after Mouse Immunization with Yeast Expressed H1 Antigen: A Promising Influenza Vaccine Candidate
High-Titre Neutralizing Antibodies to H1N1 Influenza Virus after Mouse Immunization with Yeast Expressed H1 Antigen: A Promising Influenza Vaccine Candidate Open
H1N1 influenza virus is still regarded as a serious pandemic threat. The most effective method of protection against influenza virus and the way to reduce the risk of epidemic or pandemic spread is vaccination. Influenza vaccine manufactur…
View article: Affinity of fentanyl and its derivatives for the σ<sub>1</sub>-receptor
Affinity of fentanyl and its derivatives for the σ<sub>1</sub>-receptor Open
Fentanyl has been found to only weakly bind the σ1-receptor, and its close derivatives have submicromolar affinities.
View article: Immunogenicity of DNA Vaccine against H5N1 Containing Extended Kappa B Site: In Vivo Study in Mice and Chickens
Immunogenicity of DNA Vaccine against H5N1 Containing Extended Kappa B Site: In Vivo Study in Mice and Chickens Open
Influenza is one of the most important illnesses in the modern world, causing great public health losses each year due to the lack of medication and broadly protective, long-lasting vaccines. The development of highly immunogenic and safe …
View article: Physicochemical properties and in vitro cytotoxicity of iron oxide-based nanoparticles modified with antiangiogenic and antitumor peptide A7R
Physicochemical properties and in vitro cytotoxicity of iron oxide-based nanoparticles modified with antiangiogenic and antitumor peptide A7R Open
Superparamagnetic iron oxide-based nanoparticles (SPIONs) are promising carriers as targeted drug delivery vehicles, because they can be guided to their target with the help of an external magnetic field. Functionalization of nanoparticles…
View article: The Length of N-Glycans of Recombinant H5N1 Hemagglutinin Influences the Oligomerization and Immunogenicity of Vaccine Antigen
The Length of N-Glycans of Recombinant H5N1 Hemagglutinin Influences the Oligomerization and Immunogenicity of Vaccine Antigen Open
Hemagglutinin glycoprotein (HA) is a principle influenza vaccine antigen. Recombinant HA-based vaccines become a potential alternative for traditional approach. Complexity and variation of HA N-glycosylation are considered as the im…
View article: Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds
Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds Open
The area of multitarget compounds, joining two pharmacophores within one molecule, is a vivid field of research in medicinal chemistry. Not only pharmacophoric elements are essential for the design and activity of such compounds, but the t…
View article: Codon optimization of antigen coding sequences improves the immune potential of DNA vaccines against avian influenza virus H5N1 in mice and chickens
Codon optimization of antigen coding sequences improves the immune potential of DNA vaccines against avian influenza virus H5N1 in mice and chickens Open
View article: Bifunctional Peptide-Based Opioid Agonist–Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain
Bifunctional Peptide-Based Opioid Agonist–Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain Open
Herein, the opioid pharmacophore H-Dmt-d-Arg-Aba-β-Ala-NH2 (7) was linked to peptide ligands for the nociceptin receptor. Combination of 7 and NOP ligands (e.g., H-Arg-Tyr-Tyr-Arg-Ile-Lys-NH2) led to binding affinities in the low nanomolar…
View article: Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics
Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics Open
Herein, the synthesis and biological evaluation of dual opioid agonists-neurokinin 1 receptor (NK1R) antagonists is described. In these multitarget ligands, the two pharmacophores do not overlap, and this allowed maintaining high NK1R affi…
View article: Dimeric Dermorphin Analogues Containing β3-Homo-Amino Acids: Synthesis, Binding Affinities and Metabolic Stability
Dimeric Dermorphin Analogues Containing β3-Homo-Amino Acids: Synthesis, Binding Affinities and Metabolic Stability Open
Oliwia Frączak, Anika Lasota, Adriana Muchowska, Piotr Kosson, Dagmara Tymecka, Aleksandra Misicka and Aleksandra Olma Institute of Organic Chemistry, Lodz University of Technology, Zeromskiego 116, Lodz 90-924, Poland; Mossakowski Medical…
View article: Neuroprotective effect of fingolimod and pramipexole in Parkinson's disease animal model
Neuroprotective effect of fingolimod and pramipexole in Parkinson's disease animal model Open