By Brown Zachary Z; Mapelli Claudio; McCracken Amy Bittner; Chen Kuanchang; Zhu Xiaohong; Garbaccio Robert M; Walji Abbas; Farasat Iman; Shoultz Alycia V; Canada Keith A; et al From The Journal of organic chemistry (2020), 85(3), 1466-1475, Language: English, Database:…
By Mattioni Anna; Castagnoli Luisa; Cesareni Gianni; Santonico Elena; Boldt Karsten; Ueffing Marius; Auciello Giulio; Komada Masayuki; Rappoport Joshua Z; Cesareni Gianni From The FEBS journal (2020), , Language: English, Database: MEDLINE RING finger protein 11 (RNF11) is an evolutionary…
By Borgini Matteo; Zamperini Claudio; Poggialini Federica; Botta Maurizio; Zamperini Claudio; Botta Maurizio; Ferrante Luca; Fabio Romano Di; Summa Vincenzo; Fabio Romano Di; et al From ACS medicinal chemistry letters (2020), 11(5), 846-851, Language: English, Database: MEDLINE The marine natural…
By Varrone Francesca; Caputo Emilia From International journal of molecular sciences (2020), 21(3), , Language: English, Database: MEDLINE Melanoma is the less common but the most malignant skin cancer. Since the survival rate of melanoma metastasis is about 10-15%, many…
By Cariulo, Cristina; Verani, Margherita; Martufi, Paola; Ingenito, Raffaele; Finotto, Marco; Deguire, Sean M.; Lavery, Daniel J.; Toledo-Sherman, Leticia; Lee, Ramee; Doherty, Elizabeth M.; et al From Biochemical and Biophysical Research Communications (2020), 521(3), 549-554. Language: English, Database: CAPLUS, DOI:10.1016/j.bbrc.2019.09.097…
In the last few years macrocyclic peptides have emerged as a better class of lead candidates for inhibition of protein-protein interactions with respect to conventional small molecules. The IRBM peptide chemistry team collaborated with the teams at Merck & co. and RaPharma to develop potent macrocyclic peptide inhibitors of PCSK9 a key regulator of plasma LDL-cholesterol.
Nowadays, there is a strong drive to explore new areas of chemical space in search of innovative ways to bind and modulate challenging biological targets. At IRBM our peptide chemistry team has extensive expertise in peptide and macrocyclic drug discovery in various therapeutic areas.
IRBM used liquid chromatography-high resolution mass spectrometry to explore different methods for the study of catabolism (breakdown) which is a key driver in the design of more stable peptides.
Trypanosoma brucei is a parasite responsible for human African trypanosomiasis, also known as sleeping sickness, a disease endemic in sub-Saharan Africa, with 70 million people at risk of infection. Current treatments are limited by their toxicity, administration in endemic countries and treatment resistance.
Human African trypanosomiasis (HAT), also known as sleeping sickness, is a parasitic disease that causes significant mortality in sub- Saharan Africa. A previous publication from IRBM laboratory reported the identification of 2-(1H-imidazo-2-yl)piperazines as a new series of potent T. brucei growth inhibitors.
