Fatty acid acylated peptide therapeutics: discovery of omega-n oxidation of the lipid chain as a novel metabolic pathway in preclinical species

Autor: Simone Esposito, Alain Krick, Olivier Pasquier, Fabrice Bonche, Raffaele Ingenito, Paola Magotti, Elisabetta Bianchi, Edith Monteagudo, Mariana Gallo, Daniel Oscar Cicero, Laura Orsatti, Maria Veneziano, Fulvia Caretti, Riccardo Mele, Daniela Roversi, Nadia Gennari, Denis Brasseur, Laurence Gauzy-Lazo, Olivier Duclos, Christine Mauriac, Stephane Illiano, Sergio Mallart

Publikováno v: Journal of Pharmaceutical and Biomedical Analysis
Journal of Pharmaceutical and Biomedical Analysis, 2023, 227, pp.115256. ⟨10.1016/j.jpba.2023.115256⟩

International audience; We recently described C18 fatty acid acylated peptides as a new class of potent long-lasting single-chain RXFP1 agonists that displayed relaxin-like activities in vivo. Early pharmacokinetics and toxicological studies of these

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe48f7e018f9c4ba38832ba51bf5e8f5
https://hdl.handle.net/2108/313607

Advances in Antibody–Drug Conjugate Design: Current Clinical Landscape and Future Innovations

Autor: Marie-Priscille Brun, Ingrid Sassoon, Laurence Gauzy-Lazo

Publikováno v: SLAS Discovery. 25:843-868

The targeted delivery of potent cytotoxic molecules into cancer cells is considered a promising anticancer strategy. The design of clinically effective antibody-drug conjugates (ADCs), in which biologically active drugs are coupled through chemical l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d708dd0ecd1be88cfa48de2a1d515e2a
https://doi.org/10.1177/2472555220912955

Synthesis of C 2 -symmetric guanidino-sugars as potent inhibitors of glycosidases

Autor: Jean-Claude Depezay, Christine Gravier-Pelletier, Yves Le Merrer, Laurence Gauzy

Publikováno v: Bioorganic & Medicinal Chemistry. 8:307-320

A series of enantiomerically pure C2-Symmetric guanidino-sugars was synthesized from d -mannitol. The first method described involves direct opening of a bis-epoxide by guanidine, whereas the second one deals with a mercury-catalyzed transformation o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ff0456c0fae894bdf50e357ffc27656
https://doi.org/10.1016/s0968-0896(99)00294-1

Protocols for lysine conjugation

Autor: Marie-Priscille, Brun, Laurence, Gauzy-Lazo

Publikováno v: Methods in molecular biology (Clifton, N.J.). 1045

Currently, the most widely used chemical methodology for the conjugation of drugs to monoclonal antibodies involves either lysine or cysteine residues. In this chapter, several methods for the preparation of antibody-drug conjugates (ADCs) through co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::3a8359c162b2c90ff91b3a3a8461a7dd
https://pubmed.ncbi.nlm.nih.gov/23913147

Abstract LB-053: Towards new cryptophycins as promising payloads for ADC

Autor: Céline Nicolazzi, François Clerc, Alain Krick, Marie-Helene Pascual, Céline Amara, Herve Bouchard, Olivier Pasquier, Nathalie Karst, Pierre-Yves Abecassis, Anne-Marie Lefebvre, Zhang Jidong, Christophe Henry, Ingrid Sassoon, Eric Beys, Florence Efremenko, Marie-Priscille Brun, Pierre-François Berne, Laurence Gauzy, Sylvain Huille

Publikováno v: Cancer Research. 76:LB-053

Cryptophycins are a class of macrocyclic depsipeptides produced as secondary metabolites by cyanobacteria of the genus Nostoc and were found to bind to microtubules at the vinca site. The natural product C-1 isolated in 1990 and the synthetic derivat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a9f16176e854a07f354fafb50371995b
https://doi.org/10.1158/1538-7445.am2016-lb-053