HER2-positive breast-cancer cell lines are sensitive to KDM5 inhibition: definition of a gene-expression model for the selection of sensitive cases

Autor: Gabriela Paroni, Marco Bolis, Mineko Terao, Maddalena Fratelli, Lars Ole Gerlach, Adriana Zanetti, Peter Staller, Enrico Garattini, Kristian Helin, Richard M. Neve, Paolo Ubezio

Publikováno v: Oncogene. 38(15)

Targeting of histone methylation has therapeutic potential in oncology. Here, we provide proof-of-principle that pharmacological inhibition of KDM5 histone-demethylases is a new strategy for the personalized treatment of HER2+ breast cancer. The anti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5ae3ad1e48c46845ccb244da9ab153c
https://pubmed.ncbi.nlm.nih.gov/30538297

Novel Selective Orally Active CRTH2 Antagonists for Allergic Inflammation Developed from in Silico Derived Hits

Autor: Jean-Marie Receveur, Lars-Ole Gerlach, Jesper Mosolff Mathiesen, Evi Kostenis, Thomas M. Frimurer, Thomas Högberg, Marie Grimstrup, Øystein Rist, Lena Uller, Trond Ulven

Publikováno v: University of Copenhagen
Ulven, T, Receveur, J-M, Grimstrup, M, Rist, Ø, Frimurer, T M, Gerlach, L-O, Mathiesen, J M, Kostenis, E, Uller, L & Högberg, T 2006, ' Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits ', Journal of Medicinal Chemistry, vol. 49, no. 23, pp. 6638-6641 . https://doi.org/10.1021/jm060657g

Hits from an in silico derived focused library for CRTH2 were transformed into highly selective antagonists with favorable ADME properties. Oral administration of 4-bromo-2-(1-phenyl-1H-pyrazole-4-carbonyl)phenoxyacetic acid (19) inhibited peribronch

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef8e3d0eef0b5dd8e1313da9e8171822
https://doi.org/10.1021/jm060657g

Molecular Mechanism of AMD3100 Antagonism in the CXCR4 Receptor

Autor: Mette M. Rosenkilde, Renato T. Skerlj, Gary Bridger, Lars-Ole Gerlach, Janus S. Jakobsen, Thue W. Schwartz

Publikováno v: Journal of Biological Chemistry. 279:3033-3041

AMD3100 is a symmetric bicyclam, prototype non-peptide antagonist of the CXCR4 chemokine receptor. Mutational substitutions at 16 positions located in TM-III, -IV, -V, -VI, and -VII lining the main ligand-binding pocket of the CXCR4 receptor identifi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6f26ac2d5526de11f70b48614d8db466
https://doi.org/10.1074/jbc.m309546200

Arylamide derivatives as allosteric inhibitors of the integrin α2β1/type I collagen interaction

Autor: Meredith W. Miller, Dahui Liu, Joel S. Bennett, William F. DeGrado, Hang Yin, Gaston Vilaire, David T. Moore, Lars Ole Gerlach

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:3380-3382

We herein report a group of allosteric inhibitors of integrin alpha(2)beta(1) based on an arylamide scaffold. Compound 4 showed an IC(50) of 4.80 microM in disrupting integrin I-domain/collagen binding in an ELISA. These arylamide compounds are able

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f1f3f5fc3fa3ede4b9383ad79701094
https://doi.org/10.1016/j.bmcl.2006.04.037

Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor

Autor: Mette M. Rosenkilde, Thue W. Schwartz, Lars Ole Gerlach, Renato T. Skerlj, Sigrid Hatse, Gary Bridger, Dominique Schols

Publikováno v: The Journal of biological chemistry. 282(37)

AMD3465 is a novel, nonpeptide CXCR4 antagonist and a potent inhibitor of HIV cell entry in that one of the four-nitrogen cyclam rings of the symmetrical, prototype bicyclam antagonist AMD3100 has been replaced by a two-nitrogen N-pyridinylmethylene

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fba09da642ad9856736a870a7a7ed72
https://pubmed.ncbi.nlm.nih.gov/17599916