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Pregled bibliografske jedinice broj: 1131519

Macrolide Inspired Macrocycles as Modulators of the IL-17A/IL-17RA Interaction


Koštrun, Sanja; Fajdetić, Andrea; Pešić, Dijana; Brajša, Karmen; Bencetić Mihaljević, Vlatka; Jelić, Dubravko; Petrinić Grba, Adriana; Elenkov, Ivaylo; Rupčić, Renata; Kapić, Sandra et al.
Macrolide Inspired Macrocycles as Modulators of the IL-17A/IL-17RA Interaction // Journal of medicinal chemistry (2021) doi:10.1021/acs.jmedchem.1c00327 (znanstveni, online first)


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Naslov
Macrolide Inspired Macrocycles as Modulators of the IL-17A/IL-17RA Interaction

Autori
Koštrun, Sanja ; Fajdetić, Andrea ; Pešić, Dijana ; Brajša, Karmen ; Bencetić Mihaljević, Vlatka ; Jelić, Dubravko ; Petrinić Grba, Adriana ; Elenkov, Ivaylo ; Rupčić, Renata ; Kapić, Sandra ; Ozimec Landek, Ivana ; Butković, Kristina ; Grgičević, Ana ; Žiher, Dinko ; Čikoš, Ana ; Padovan, Jasna ; Saxty, Gordon ; Duck, Kevin ; Bladh, Haakan ; Skak- Nielsen, Tine ; Feldbaek Nielsen, Simon ; Lambert, Maja ; Stahlhud, Martin

Vrsta, podvrsta
Radovi u časopisima, znanstveni

Izvornik
Journal of medicinal chemistry (2021)

Status rada
Online first

Ključne riječi
proteins ; macrocycles ; IL 17AM ; Il 17RA ; chemical structure inhibitors

Sažetak
Interleukin 17 (IL-17) cytokines promote inflammatory pathophysiology in many autoimmune diseases, including psoriasis, multiple sclerosis, rheumatoid arthritis, and inflammatory bowel disease. Such broad involvement of IL-17 in various autoimmune diseases makes it an ideal target for drug discovery. Psoriasis is a chronic inflammatory disease characterized by numerous defective components of the immune system. Significantly higher levels of IL-17A have been noticed in lesions of psoriatic patients, if compared to non-lesion parts. Therefore, this paper is focused on the macrolide inspired macrocycles as potential IL-17A/IL-17RA modulators and covers the molecular design, synthesis, and in vitro profiling. Macrocycles are designed to diversify and enrich chemical space through different ring sizes and a variety of three-dimensional shapes. Inhibitors in the nM range were identified in both target-based and phenotypic assays. In vitro ADME as well as in vivo PK properties are reported.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Interdisciplinarne biotehničke znanosti



POVEZANOST RADA


Poveznice na cjeloviti tekst rada:

doi pubs.acs.org

Citiraj ovu publikaciju:

Koštrun, Sanja; Fajdetić, Andrea; Pešić, Dijana; Brajša, Karmen; Bencetić Mihaljević, Vlatka; Jelić, Dubravko; Petrinić Grba, Adriana; Elenkov, Ivaylo; Rupčić, Renata; Kapić, Sandra et al.
Macrolide Inspired Macrocycles as Modulators of the IL-17A/IL-17RA Interaction // Journal of medicinal chemistry (2021) doi:10.1021/acs.jmedchem.1c00327 (znanstveni, online first)
Koštrun, S., Fajdetić, A., Pešić, D., Brajša, K., Bencetić Mihaljević, V., Jelić, D., Petrinić Grba, A., Elenkov, I., Rupčić, R. & Kapić, S. (2021) Macrolide Inspired Macrocycles as Modulators of the IL-17A/IL-17RA Interaction. Prihvaćen za objavljivanje u Journal of medicinal chemistry. [Preprint] doi:10.1021/acs.jmedchem.1c00327.
@unknown{unknown, year = {2021}, DOI = {10.1021/acs.jmedchem.1c00327}, keywords = {proteins, macrocycles, IL 17AM, Il 17RA, chemical structure inhibitors}, journal = {Journal of medicinal chemistry}, doi = {10.1021/acs.jmedchem.1c00327}, title = {Macrolide Inspired Macrocycles as Modulators of the IL-17A/IL-17RA Interaction}, keyword = {proteins, macrocycles, IL 17AM, Il 17RA, chemical structure inhibitors} }
@unknown{unknown, year = {2021}, DOI = {10.1021/acs.jmedchem.1c00327}, keywords = {proteins, macrocycles, IL 17AM, Il 17RA, chemical structure inhibitors}, journal = {Journal of medicinal chemistry}, doi = {10.1021/acs.jmedchem.1c00327}, title = {Macrolide Inspired Macrocycles as Modulators of the IL-17A/IL-17RA Interaction}, keyword = {proteins, macrocycles, IL 17AM, Il 17RA, chemical structure inhibitors} }

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