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Results: 153
Structure of Gremlin-1 and analysis of its interaction with BMP-2.
Gremlin X-ray crystallography Bone Morphogenetic Protein (BMP) differential screening-aberrative in neuroblastoma (DAN) extracellular antagonism structural biology transforming growth factor-β (TGF-β) Bone Morphogenetic Protein 2 Carrier Proteins Crystallography X-Ray Glycoproteins Humans Intercellular Signaling Peptides and Proteins Mutation Protein Binding Protein Conformation Protein Multimerization Signal Transduction
Crystal structure of the Rho-associated coiled-coil kinase 2 inhibitor belumosudil bound to CK2α.
The small molecule belumosudil was initially identified as a selective inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2) and has recently been approved for the treatment of graft-versus-host disease. However, recent...
Structure and activation of pro-activin A.
Activins are growth factors with multiple roles in the development and homeostasis. Like all TGF-β family of growth factors, activins are synthesized as large precursors from which mature dimeric growth factors are released...
Proposed Allosteric Inhibitors Bind to the ATP Site of CK2α.
CK2α is a ubiquitous, well-studied kinase that is a target for small-molecule inhibition, for treatment of cancers. While many different classes of adenosine 5'-triphosphate (ATP)-competitive inhibitors have been described for...
Adenosine Triphosphate Allosteric Regulation Allosteric Site Binding Competitive Casein Kinase II Crystallography X-Ray Deuterium Exchange Measurement Humans Ligands Molecular Dynamics Simulation Naphthyridines Nuclear Magnetic Resonance Biomolecular Phenazines Protein Binding Protein Kinase Inhibitors Recombinant Proteins
Genomic structure and transcript analysis of the Rapid Alkalinization Factor (RALF) gene family during host-pathogen crosstalk in Fragaria vesca and Fragaria x ananassa strawberry
Rapid Alkalinization Factors (RALFs) are cysteine-rich peptides ubiquitous within plant kingdom. They play multiple roles as hormonal signals in diverse processes, including root elongation, cell growth, pollen tube development...
Supporting data on combined transcriptomic and phosphoproteomic analysis of BMP4 signaling in human embryonic stem cells.
Angelos Papadopoulos, Varvara Chalmantzi, Marko Hyvönen, Dimitris Stellas, Marika Syrrou, Theodore Fotsis, Carol Murphy
Apr 23, 2021
Human embryonic stem cells exhibit great potential as a therapeutic tool in regenerative medicine due to their self-renewal and trilineage differentiation capacity. Maintaining this unique cellular state has been shown to rely...
Genomic structure and transcript analysis of the Rapid Alkalinization Factor (RALF) gene family during host-pathogen crosstalk in Fragaria vesca and Fragaria x ananassa strawberry.
Rapid Alkalinization Factors (RALFs) are cysteine-rich peptides ubiquitous within plant kingdom. They play multiple roles as hormonal signals in diverse processes, including root elongation, cell growth, pollen tube development...
Organoid culture media formulated with growth factors of defined cellular activity.
Manuela Urbischek, Helena Rannikmae, Thomas Foets, Katharina Ravn, Marko Hyvönen, Marc de la Roche
Apr 15, 2019
The media formulations necessary for deriving and sustaining organoids from epithelial tissues such as prostate, colon, gastric, liver, pancreas, and others have been established. Critical components of organoid media are a set...
Downfalls of Chemical Probes Acting at the Kinase ATP-Site
Eleanor L. Atkinson, Jessica Iegre, Paul D. Brear, Elizabeth A. Zhabina, Marko Hyvönen, David R. Spring
Apr 01, 2021
Protein kinases are a large class of enzymes with numerous biological roles and many have been implicated in a vast array of diseases, including cancer and the novel coronavirus infection COVID-19. Thus, the development of...
Organoid culture media formulated with growth factors of defined cellular activity
Manuela Urbischek, Helena Rannikmae, Thomas Foets, Katharina Ravn, Marko Hyvönen, Marc de la Roche
Jul 09, 2020
Abstract: The media formulations necessary for deriving and sustaining organoids from epithelial tissues such as prostate, colon, gastric, liver, pancreas, and others have been established. Critical components of organoid media...
Structure of the human myostatin precursor and determinants of growth factor latency.
Thomas R Cotton, Gerhard Fischer, Xuelu Wang, Jason C McCoy, Magdalena Czepnik, Thomas B Thompson, Marko Hyvönen
Feb 26, 2018
Myostatin, a key regulator of muscle mass in vertebrates, is biosynthesised as a latent precursor in muscle and is activated by sequential proteolysis of the pro-domain. To investigate the molecular mechanism by which...
Evolution of protease activation and specificity via alpha-2-macroglobulin-mediated covalent capture
Abstract Tailoring of the activity and specificity of proteases is critical for their utility across industrial, medical and research purposes. However, engineering or evolving protease catalysts...
Philipp Knyphausen, Mariana Rangel Pereira, Paul Brear, Marko Hyvönen, Lutz Jermutus, Florian Hollfelder
Feb 11, 2023
A versatile Halo- and SNAP-tagged BMP/TGFβ receptor library for quantification of cell surface ligand binding
Jerome Jatzlau, Wiktor Burdzinski, Michael Trumpp, Leon Obendorf, Kilian Roßmann, Katharina Ravn, Marko Hyvönen, Francesca Bottanelli, Johannes Broichhagen, Petra Knaus
Jan 25, 2023
Published by: Nature Publishing Group UK
Small-molecule inhibitors that target protein-protein interactions in the RAD51 family of recombinases.
Duncan E Scott, Anthony G Coyne, Ashok Venkitaraman, Tom L Blundell, Chris Abell, Marko Hyvönen
Dec 16, 2014
BRCA2 RAD51 biophysics homologous recombination INHIBITORS protein-protein interactions Amino Acid Motifs BRCA2 Protein Binding Sites Drug Design Humans Molecular Dynamics Simulation Protein Binding Protein Structure Tertiary Pyrococcus furiosus Rad51 Recombinase Small Molecule Libraries Structure-Activity Relationship Thermodynamics
A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action.
Paul Brear, Claudia De Fusco, Eleanor L Atkinson, Jessica Iegre, Nicola J Francis-Newton, Ashok R Venkitaraman, Marko Hyvönen, David R Spring
Dec 25, 2022
CK2 is a ubiquitous protein kinase with an anti-apoptotic role and is found to be overexpressed in multiple cancer types. To this end, the inhibition of CK2 is of great interest with regard to the development of novel...
Second-generation CK2α inhibitors targeting the αD pocket.
Jessica Iegre, Paul Brear, Claudia De Fusco, Masao Yoshida, Sophie L Mitchell, Maxim Rossmann, Laura Carro, Hannah F Sore, Marko Hyvönen, David R Spring
Jun 18, 2018
CK2 is a critical cell cycle regulator that also promotes various anti-apoptotic mechanisms. Development of ATP-non-competitive inhibitors of CK2 is a very attractive strategy considering that the ATP binding site is highly...
Downfalls of Chemical Probes Acting at the Kinase ATP-Site
Eleanor L Atkinson, Jessica Iegre, Paul D Brear, Elizabeth A Zhabina, Marko Hyvönen, David R Spring
Jun 17, 2021
Protein kinases are a large class of enzymes with numerous biological roles and many have been implicated in a vast array of diseases, including cancer and the novel coronavirus infection COVID-19. Thus, the development of...
Structural and Mechanistic Analysis of the Choline Sulfatase from Sinorhizobium melliloti
Bert van Loo, Markus Schober, Eugene Valkov, Magdalena Heberlein, Erich Bornberg-Bauer, Kurt Faber, Marko Hyvönen, Florian Hollfelder
May 02, 2018
Hydrolysis of organic sulfate esters proceeds by two distinct mechanisms, water attacking at either sulfur (S-O bond cleavage) or carbon (C-O bond cleavage). In primary and secondary alkyl sulfates, attack at carbon is favored...
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