[HTML][HTML] Structure of the ligand‐binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist
…, RE Hubbard, T Bonn, AG Thorsell… - The EMBO …, 1999 - embopress.org
Oestrogens exert their physiological effects through two receptor subtypes. Here we report
the three‐dimensional structure of the oestrogen receptor beta isoform (ERβ) ligand‐binding …
the three‐dimensional structure of the oestrogen receptor beta isoform (ERβ) ligand‐binding …
Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors
…, N Markova, A Macchiarulo, AG Thorsell… - Nature …, 2012 - nature.com
Inhibitors of poly-ADP-ribose polymerase (PARP) family proteins are currently in clinical trials
as cancer therapeutics, yet the specificity of many of these compounds is unknown. Here …
as cancer therapeutics, yet the specificity of many of these compounds is unknown. Here …
[PDF][PDF] Structural insights into the mode of action of a pure antiestrogen
…, AM Brzozowski, J Walton, RE Hubbard, AG Thorsell… - Structure, 2001 - cell.com
Background: Estrogens exert their effects on target tissues by binding to a nuclear transcription
factor termed the estrogen receptor (ER). Previous structural studies have demonstrated …
factor termed the estrogen receptor (ER). Previous structural studies have demonstrated …
Structural basis for potency and promiscuity in poly (ADP-ribose) polymerase (PARP) and tankyrase inhibitors
AG Thorsell, T Ekblad, T Karlberg… - Journal of medicinal …, 2017 - ACS Publications
Selective inhibitors could help unveil the mechanisms by which inhibition of poly(ADP-ribose)
polymerases (PARPs) elicits clinical benefits in cancer therapy. We profiled 10 clinical …
polymerases (PARPs) elicits clinical benefits in cancer therapy. We profiled 10 clinical …
[HTML][HTML] Comparative structural analysis of lipid binding START domains
AG Thorsell, WH Lee, C Persson, MI Siponen… - Plos one, 2011 - journals.plos.org
Background Steroidogenic acute regulatory (StAR) protein related lipid transfer (START)
domains are small globular modules that form a cavity where lipids and lipid hormones bind. …
domains are small globular modules that form a cavity where lipids and lipid hormones bind. …
[PDF][PDF] Recognition of mono-ADP-ribosylated ARTD10 substrates by ARTD8 macrodomains
AH Forst, T Karlberg, N Herzog, AG Thorsell, A Gross… - Structure, 2013 - cell.com
ADP-ribosyltransferases (ARTs) catalyze the transfer of ADP-ribose from NAD + onto
substrates. Some ARTs generate in an iterative process ADP-ribose polymers that serve as …
substrates. Some ARTs generate in an iterative process ADP-ribose polymers that serve as …
[HTML][HTML] Comparative structural analysis of human DEAD-box RNA helicases
…, HW Park, M Hammarström, M Moche, AG Thorsell… - PloS one, 2010 - journals.plos.org
DEAD-box RNA helicases play various, often critical, roles in all processes where RNAs are
involved. Members of this family of proteins are linked to human disease, including cancer …
involved. Members of this family of proteins are linked to human disease, including cancer …
[HTML][HTML] Engineering Af1521 improves ADP-ribose binding and identification of ADP-ribosylated proteins
…, T Karlberg, M Bütepage, AG Thorsell… - Nature …, 2020 - nature.com
Protein ADP-ribosylation is a reversible post-translational modification that regulates important
cellular functions. The identification of modified proteins has proven challenging and has …
cellular functions. The identification of modified proteins has proven challenging and has …
A Focused DNA-Encoded Chemical Library for the Discovery of Inhibitors of NAD+-Dependent Enzymes
DNA-encoded chemical libraries are increasingly used in pharmaceutical research because
they enable the rapid discovery of synthetic protein ligands. Here we explored whether …
they enable the rapid discovery of synthetic protein ligands. Here we explored whether …
[HTML][HTML] System-wide identification and prioritization of enzyme substrates by thermal analysis
…, S Rodin, K Näreoja, AG Thorsell… - Nature …, 2021 - nature.com
Despite the immense importance of enzyme–substrate reactions, there is a lack of general
and unbiased tools for identifying and prioritizing substrate proteins that are modified by the …
and unbiased tools for identifying and prioritizing substrate proteins that are modified by the …