Advanced search    

Search: authors:"Apirat Chaikuad"

6 papers found.
Use AND, OR, NOT, +word, -word, "long phrase", (parentheses) to fine-tune your search.

Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype

) Acknowledgments The technical assistance by Petra Lippmann is acknowledged. Conceptualization: Anne Walter, Stefan Knapp, Laurent Meijer, Conrad Kunick. Data curation: Anne Walter, Apirat Chaikuad, Renate Helmer ... , Nadège LoaeÈc, Ingo Ott, Stefan Knapp, Laurent Meijer, Conrad Kunick. Formal analysis: Anne Walter, Apirat Chaikuad, Nadège LoaeÈc, Lutz Preu, Ingo Ott, Laurent Meijer, Conrad Kunick. Funding

A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis

Activin receptor-like kinase 1 (ALK1, encoded by the gene ACVRL1) is a type I BMP/TGF-β receptor that mediates signalling in endothelial cells via phosphorylation of SMAD1/5/8. During angiogenesis, sprouting endothelial cells specialise into tip cells and stalk cells. ALK1 synergises with Notch in stalk cells to induce expression of the Notch targets HEY1 and HEY2 and thereby...

Conservation of structure and activity in Plasmodium purine nucleoside phosphorylases

Background Purine nucleoside phosphorylase (PNP) is central to purine salvage mechanisms in Plasmodium parasites, the causative agents of malaria. Most human malaria results from infection either by Plasmodium falciparum (Pf), the deadliest form of the parasite, or by the widespread Plasmodium vivax (Pv). Whereas the PNP enzyme from Pf has previously been studied in detail...

Structure of human aspartyl aminopeptidase complexed with substrate analogue: insight into catalytic mechanism, substrate specificity and M18 peptidase family

BackroundAspartyl aminopeptidase (DNPEP), with specificity towards an acidic amino acid at the N-terminus, is the only mammalian member among the poorly understood M18 peptidases. DNPEP has implicated roles in protein and peptide metabolism, as well as the renin-angiotensin system in blood pressure regulation. Despite previous enzyme and substrate characterization, structural...

A New Class of Small Molecule Inhibitor of BMP Signaling

Growth factor signaling pathways are tightly regulated by phosphorylation and include many important kinase targets of interest for drug discovery. Small molecule inhibitors of the bone morphogenetic protein (BMP) receptor kinase ALK2 (ACVR1) are needed urgently to treat the progressively debilitating musculoskeletal disease fibrodysplasia ossificans progressiva (FOP...

Structural Comparison of Human Mammalian Ste20-Like Kinases

Background The serine/threonine mammalian Ste-20 like kinases (MSTs) are key regulators of apoptosis, cellular proliferation as well as polarization. Deregulation of MSTs has been associated with disease progression in prostate and colorectal cancer. The four human MSTs are regulated differently by C-terminal regions flanking the catalytic domains. Principal Findings We have...