Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Per Källblad"'
Autor:
Wei B. Emond, Rajiv Sawant, Matthis Geitmann, Johan Winquist, Peter Brandt, Ulf Bremberg, Per Källblad, Vendela Parrow, Claes Andersson, Kristin Blom, Nasrin Najafi, Tobias Bergström, Fredrik J. Swartling, Mats Hellström, Konrad F. Koehler
Publikováno v:
Cancer Research. 83:705-705
LSD1 has emerged as a potential therapeutic target to increase the effectiveness of cancer immunotherapy. We have developed a series of novel small molecules, exemplified by the lead substance BEA-17, that modulates LSD1 via binding to an allosteric
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f2c42493fb778b9176cfe3ea22922e02
https://doi.org/10.1158/1538-7445.am2023-705
https://doi.org/10.1158/1538-7445.am2023-705
Autor:
Ulf Bremberg, Vendela Parrow, Maria Sjöberg, Wei B. Emond, Malin Jarvius, Rajiv Sawant, Konrad Koehler, Anna Segerman, Mia Niklasson, Johan Winquist, Per Källblad, Matthis Geitmann
Publikováno v:
Cancer Research. 79:3843-3843
LSD1 has emerged as a potential therapeutic target for a number of cancer types (e.g. AML, SCLC, colorectal, breast, liver, prostate, glioblastoma, Ewing sarcoma), as well as sickle cell anaemia and Alzheimer’s disease. Irreversible LSD1 catalytic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::78460e6c49ba63cc9380711196b12703
https://doi.org/10.1158/1538-7445.am2019-3843
https://doi.org/10.1158/1538-7445.am2019-3843
Autor:
U. Helena Danielson, Rob Leurs, Jacqueline E. van Muijlwijk-Koezen, Gerdien E. de Kloe, Matthis Geitmann, Per Källblad, Tariq T. Nahar, Hubertus Irth, August B. Smit, Iwan J. P. de Esch, René van Elk, Kim Retra
Publikováno v:
Journal of Medicinal Chemistry, 53(19), 7192-7201. American Chemical Society
Journal of Medicinal Chemistry
de Kloe, G E, Retra, K, Geitmann, M, Kallblad, B, Nahar, T T, van Elk, R, Smit, A B, van Muijlwijk-Koezen, J E, Leurs, R, Irth, H, Danielson, U H & de Esch, I J P 2010, ' Surface Plasmon Resonance Biosensor Based Fragment Screening Using Acetylcholine Binding Protein Identifies Ligand Efficiency Hot Spots (LE Hot Spots) by Deconstruction of Nicotinic Acetylcholine Receptor α7 Ligands ', Journal of Medicinal Chemistry, vol. 53, no. 19, pp. 7192-7201 . https://doi.org/10.1021/jm100834y
Journal of Medicinal Chemistry
de Kloe, G E, Retra, K, Geitmann, M, Kallblad, B, Nahar, T T, van Elk, R, Smit, A B, van Muijlwijk-Koezen, J E, Leurs, R, Irth, H, Danielson, U H & de Esch, I J P 2010, ' Surface Plasmon Resonance Biosensor Based Fragment Screening Using Acetylcholine Binding Protein Identifies Ligand Efficiency Hot Spots (LE Hot Spots) by Deconstruction of Nicotinic Acetylcholine Receptor α7 Ligands ', Journal of Medicinal Chemistry, vol. 53, no. 19, pp. 7192-7201 . https://doi.org/10.1021/jm100834y
The soluble acetylcholine binding protein (AChBP) is a homologue of the ligand-binding domain of the nicotinic acetylcholine receptors (nAChR). To guide future fragment-screening using surface plasmon resonance (SPR) biosensor technology as a label-f
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69187fa16eaf4d0068d9eeacfca3d8ca
https://hdl.handle.net/1871/38696
https://hdl.handle.net/1871/38696
Autor:
Bernard T. Golding, Claire Hutton, Shafiq U. Ahmed, Rebecca J. Reid, Stefano Norbedo, Stuart J. Kemp, John Lunec, Kappusamy Saravanan, Julian S. Northen, Henriëtte M. G. Willems, Gillian Farnie, Roger J. Griffin, Martin S. Kitching, Helen Atkins, Ian R. Hardcastle, Per Källblad, Sabrina Guyenne, David R. Newell
Publikováno v:
Journal of Medicinal Chemistry. 49:6209-6221
From a set of weakly potent lead compounds, using in silico screening and small library synthesis, a series of 2-alkyl-3-aryl-3-alkoxyisoindolinones has been identified as inhibitors of the MDM2-p53 interaction. Two of the most potent compounds, 2-be
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43ed654b0d15101155e322b8953dfc6a
https://doi.org/10.1021/jm0601194
https://doi.org/10.1021/jm0601194
Publikováno v:
QSAR & Combinatorial Science. 24:503-507
Intrinsic protein flexibility is often ignored in the drug discovery process, however, there is increasing evidence suggesting that many therapeutic targets are flexible. In this work, we describe a method for incorporating receptor flexibility, base
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4f10b121da2509c062fad049e1128598
https://doi.org/10.1002/qsar.200430924
https://doi.org/10.1002/qsar.200430924
Autor:
Shafiq U. Ahmed, Rebecca J. Reid, Roger J. Griffin, Martin S. Kitching, Per Källblad, Stuart J. Kemp, John Lunec, Julian S. Northen, Gillian Farnie, Claire Hutton, Helen Atkins, Ian R. Hardcastle, Bernard T. Golding, Stefano Norbedo, David R. Newell, A. Hilary Calvert, Sabrina Guyenne, Nicola J. Curtin, Henriëtte M. G. Willems, Kappusamy Saravanan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1515-1520
A series of 2-N-alkyl-3-aryl-3-alkoxyisoindolinones has been synthesised and evaluated as inhibitors of the MDM2-p53 interaction. The most potent compound, 3-(4-chlorophenyl)-3-(4-hydroxy-3,5-dimethoxybenzyloxy)-2-propyl-2,3-dihydroisoindol-1-one (NU
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c6a7cb96a08326b0a364a28e3c377a22
https://doi.org/10.1016/j.bmcl.2004.12.061
https://doi.org/10.1016/j.bmcl.2004.12.061
Publikováno v:
Journal of Medicinal Chemistry. 47:3334-3337
Computational ligand-protein docking is routinely used for binding mode prediction. We have quantified the effect of considering multiple docking solutions on the success rate of obtaining the crystallographic binding mode. By selection of a small se
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e6f1c929cfecb8eed897d13dcb421681
https://doi.org/10.1021/jm0498147
https://doi.org/10.1021/jm0498147
Autor:
Per Källblad, Markkuu D. Hämäläinen, U. Helena Danielson, Helena Nordström, Johan Winquist, Malin Elinder, Thomas Gossas, Matthis Geitmann
Publikováno v:
Journal of biomolecular screening. 16(1)
A new fragment library for lead discovery has been designed and experimentally validated for use in surface plasmon resonance (SPR) biosensor-based screening. The 930 compounds in the library were selected from 4.6 million commercially available comp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee37d329e0091cf0c18d7e76a1b9f9f5
https://pubmed.ncbi.nlm.nih.gov/21149860
https://pubmed.ncbi.nlm.nih.gov/21149860
Autor:
Helena Nordström, Thomas Gossas, Hans Wallberg, Susanne Nyström, Markku Hämäläinen, Per Källblad, U. Helena Danielson
Publikováno v:
Journal of medicinal chemistry. 51(12)
Small inhibitors of matrix metalloproteinase 12 (MMP-12) have been identified with a biosensor-based screening strategy and a specifically designed fragment library. The interaction between fragments and three variants of the target and a reference p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9678eec0aabbec707db89ccdd05b5da0
https://pubmed.ncbi.nlm.nih.gov/18494455
https://pubmed.ncbi.nlm.nih.gov/18494455
Publikováno v:
Scopus-Elsevier
We have investigated the efficacy of generating multiple sidechain conformations using a rotamer library in order to find the experimentally observed ligand binding site conformation of a protein in the presence of a bound ligand. We made use of a re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99a5ba653e9072c2bcd9521379aa5a8e
https://pubmed.ncbi.nlm.nih.gov/15562988
https://pubmed.ncbi.nlm.nih.gov/15562988