Pacifico et al., 2019 - Google Patents
Tetrabranched hetero-conjugated peptides as bifunctional agonists of the NOP and mu opioid receptorsPacifico et al., 2019
View PDF- Document ID
- 17793294471028127216
- Author
- Pacifico S
- Albanese V
- Illuminati D
- Fantinati A
- Marzola E
- Ferrari F
- Neto J
- Sturaro C
- Ruzza C
- Calò G
- Preti D
- Guerrini R
- Publication year
- Publication venue
- Bioconjugate Chemistry
External Links
Snippet
The general aim of the work was the validation of a new synthetic methodology designed for obtaining bifunctional heterotetrabranched peptide ligands. Applying an easily accessible synthetic route, we provided a small series of heteromultimeric peptide conjugates targeting …
- 102000037275 μ-opioid receptors 0 title abstract description 85
Classifications
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
- G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
- G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
- G01N33/502—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
- G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
- G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
- G01N33/5044—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving specific cell types
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
- A61K47/48—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
- A61K47/48238—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates the modifying agent being a protein, peptide, polyamino acid
- A61K47/48246—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates the modifying agent being a protein, peptide, polyamino acid drug-peptide, protein or polyamino acid conjugates, i.e. the modifying agent being a protein, peptide, polyamino acid which being linked/complexed to a molecule that being the pharmacologically or therapeutically active agent
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
- G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
- G01N33/6872—Intracellular protein regulatory factors and their receptors, e.g. including ion channels
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
- G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2500/00—Screening for compounds of potential therapeutic value
- G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
- G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
- G01N2333/72—Assays involving receptors, cell surface antigens or cell surface determinants for hormones
- G01N2333/726—G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH
Similar Documents
Publication | Publication Date | Title |
---|---|---|
Portoghese | From models to molecules: opioid receptor dimers, bivalent ligands, and selective opioid receptor probes | |
Mosberg et al. | Development of a bioavailable μ opioid receptor (MOPr) agonist, δ opioid receptor (DOPr) antagonist peptide that evokes antinociception without development of acute tolerance | |
Ballet et al. | Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist | |
Yamamoto et al. | A structure–activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are δ/μ opioid receptor agonists and neurokinin 1 receptor antagonists | |
Guillemyn et al. | Bifunctional peptide-based opioid agonist–nociceptin antagonist ligands for dual treatment of acute and neuropathic pain | |
Liu et al. | Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potent μ-opioid agonists | |
Yamamoto et al. | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for δ/μ opioid receptor agonists and neurokinin-1 receptor antagonists | |
Nguyen et al. | Neuropeptide FF and its receptors: therapeutic applications and ligand development | |
Mollica et al. | Novel cyclic biphalin analogue with improved antinociceptive properties | |
Yekkirala et al. | Standard opioid agonists activate heteromeric opioid receptors: Evidence for morphine and [D-Ala2-MePhe4-Glyol5] enkephalin as selective μ− δ agonists | |
Mollica et al. | Biological active analogues of the opioid peptide biphalin: Mixed α/β3-peptides | |
Gonzalez et al. | Optimized opioid-neurotensin multitarget peptides: from design to structure–activity relationship studies | |
Lee et al. | Discovery of amphipathic dynorphin A analogues to inhibit the neuroexcitatory effects of dynorphin A through bradykinin receptors in the spinal cord | |
Singh et al. | Synthesis and pharmacology of α/β3-peptides based on the melanocortin agonist Ac-His-DPhe-Arg-Trp-NH2 sequence | |
Muratspahić et al. | Design of a stable cyclic peptide analgesic derived from sunflower seeds that targets the κ-opioid receptor for the treatment of chronic abdominal pain | |
Nishizawa et al. | Design and synthesis of an investigational nonapeptide KISS1 receptor (KISS1R) agonist, Ac-d-Tyr-hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg (Me)-Trp-NH2 (TAK-448), with highly potent testosterone-suppressive activity and excellent water solubility | |
Liu et al. | MEL-N16: a series of novel endomorphin analogs with good analgesic activity and a favorable side effect profile | |
Lensing et al. | Developing a biased unmatched bivalent ligand (BUmBL) design strategy to target the GPCR homodimer allosteric signaling (cAMP over β-arrestin 2 recruitment) within the melanocortin receptors | |
Jinsmaa et al. | Novel 2′, 6′-dimethyl-l-tyrosine-containing pyrazinone opioid mimetic μ-agonists with potent antinociceptive activity in mice | |
Stefanucci et al. | Potent, efficacious, and stable cyclic opioid peptides with long lasting antinociceptive effect after peripheral administration | |
Zhang et al. | Synthesis and biological characterization of cyclic disulfide-containing peptide analogs of the multifunctional opioid/neuropeptide FF receptor agonists that produce long-lasting and nontolerant antinociception | |
Lensing et al. | A direct in vivo comparison of the melanocortin monovalent agonist Ac-His-DPhe-Arg-Trp-NH2 versus the bivalent agonist Ac-His-DPhe-Arg-Trp-PEDG20-His-DPhe-Arg-Trp-NH2: a bivalent advantage | |
Beaudeau et al. | N-Guanidyl and C-tetrazole Leu-enkephalin derivatives: Efficient mu and delta opioid receptor agonists with improved pharmacological properties | |
Halab et al. | Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist | |
Pescatore et al. | Synthesis and pharmacology of halogenated δ-opioid-selective [D-Ala2] deltorphin II peptide analogues |