Phenotypic screening platform identifies statins as enhancers of immune cell-induced cancer cell death

Autor: Tove Selvin, Malin Berglund, Lena Lenhammar, Malin Jarvius, Peter Nygren, Mårten Fryknäs, Rolf Larsson, Claes R Andersson

Publikováno v: BMC Cancer, Vol 23, Iss 1, Pp 1-10 (2023)

Abstract Background High-throughput screening (HTS) of small molecule drug libraries has greatly facilitated the discovery of new cancer drugs. However, most phenotypic screening platforms used in the field of oncology are based solely on cancer cell

Externí odkaz: https://doaj.org/article/6a001318eb47461bbdbb33b4e9a1a25b

Discovery and hit-to-lead optimization of benzothiazole scaffold-based DNA gyrase inhibitors with potent activity against Acinetobacter baumannii and Pseudomonas aeruginosa

Autor: Andrej Emanuel Cotman, Martina Durcik, Davide Benedetto Tiz, Federica Fulgheri, Daniela Secci, Maša Sterle, Štefan Možina, Žiga Skok, Nace Zidar, Anamarija Zega, Janez Ilaš, Lucija Peterlin Mašič, Tihomir Tomašič, Diarmaid Hughes, Douglas L. Huseby, Sha Cao, Linnéa Garoff, Talía Berruga Fernández, Paraskevi Giachou, Lisa Crone, Ivailo Simoff, Richard Svensson, Bryndis Birnir, Sergiy V. Korol, Zhe Jin, Francisca Vicente, Maria C. Ramos, Mercedes de la Cruz, Björn Glinghammar, Lena Lenhammar, Sara R. Henderson, Julia E. A. Mundy, Anthony Maxwell, Clare E. M. Stevenson, David M. Lawson, Guido V. Janssen, Geert Jan Sterk, Danijel Kikelj

Publikováno v: Journal of medicinal chemistry, vol. 66, no. 2, 2023.
Journal of medicinal chemistry, str. 1380-1425 : Ilustr., Vol. 66, no. 2, 2023
COBISS-ID: 512806681
Journal of medicinal chemistry, 66(2), 1380-1425. American Chemical Society
Cotman, A E, Durcik, M, Benedetto Tiz, D, Fulgheri, F, Secci, D, Sterle, M, Možina, Š, Skok, Ž, Zidar, N, Zega, A, Ilaš, J, Peterlin Mašič, L, Tomašič, T, Hughes, D, Huseby, D L, Cao, S, Garoff, L, Berruga Fernández, T, Giachou, P, Crone, L, Simoff, I, Svensson, R, Birnir, B, Korol, S V, Jin, Z, Vicente, F, Ramos, M C, De La Cruz, M, Glinghammar, B, Lenhammar, L, Henderson, S R, Mundy, J E A, Maxwell, A, Stevenson, C E M, Lawson, D M, Janssen, G V, Sterk, G J & Kikelj, D 2023, ' Discovery and Hit-to-Lead Optimization of Benzothiazole Scaffold-Based DNA Gyrase Inhibitors with Potent Activity against Acinetobacter baumannii and Pseudomonas aeruginosa ', Journal of medicinal chemistry, vol. 66, no. 2, pp. 1380-1425 . https://doi.org/10.1021/acs.jmedchem.2c01597

We have developed compounds with a promising activity against Acinetobacter baumannii and Pseudomonas aeruginosa, which are both on the WHO priority list of antibiotic-resistant bacteria. Starting from DNA gyrase inhibitor 1, we identified compound 2

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b20d28e0e61c3b400f08f6903958d25f
https://repozitorij.uni-lj.si/Dokument.php?id=166579&dn=

Anti-Myeloma Drug Melflufen Inhibits RANKL-Stimulated Osteoclastogenesis By Suppressing Proliferation of CD14+ Precursor Cells

Autor: Claes Andersson, Annica J. Rasmusson, Mårten Fryknäs, Malin Berglund, Fredrik Lehmann, Joachim Gullbo, Konstantin Byrgazov, Lena Lenhammar, Ana Slipicevic, Håkan Melhus, Rolf Larsson, Thomas Lind

Publikováno v: Blood. 136:23-23

Background Melflufen (melphalan flufenamide) is a first-in-class peptide-drug conjugate (PDC) that targets aminopeptidases and rapidly releases alkylating agents into tumor cells. Osteolytic lesions are a hallmark of multiple myeloma and occur in alm

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e0fd5a16ba686c836c236e39b60d0bf4
https://doi.org/10.1182/blood-2020-136749

Design, synthesis and in vitro biological evaluation of oligopeptides targeting E. coli type I signal peptidase (LepB)

Autor: Per E. Andrén, Douglas L. Huseby, Lu Lu, Diarmaid Hughes, Natalia Szałaj, Sha Cao, Anders Karlén, Sherry L. Mowbray, Annette K. Roos, Maria Cristina De Rosa, Edouard Zamaratski, Johan Gising, Peter Brandt, Henrik Wadensten, Lena Lenhammar, Rolf Larsson

Publikováno v: Bioorganic & Medicinal Chemistry.

Type I signal peptidases are potential targets for the development of new antibacterial agents. Here we report finding potent inhibitors of E. coli type I signal peptidase (LepB), by optimizing a previously reported hit compound, decanoyl-PTANA-CHO,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa4ee0934c8337bec0e9ec618dd9920c