Journal: FEBS Open Bio

Article Title: Identification of small‐molecule elastase inhibitors as antagonists of IL‐36 cytokine activation

doi: 10.1002/2211-5463.12406

Figure Lengend Snippet: Structure‐based in silico screening strategy to identify candidate elastase inhibitors. (A, B) In silico docking of the elastase crystal structure with the elastase inhibitor DHPI. (C, D) In silico docking of the elastase crystal structure with the elastase inhibitor Alvelestat/AZD9668. (E, F) Representation of the binding pose of newly identified LCB016 inhibitor and interaction interface of LCB016 in the active site of NE. Magenta arrow represents H‐bond, and green represents π–π contacts.

Article Snippet: Suc(OMe)‐AAPV‐AMC was purchased from PeptaNova (Sandhausen, Germany); elastase inhibitor Alvelestat/AZD9668 was purchased from MedChem Express (Solentuna, Sweden).

Techniques: In Silico, Binding Assay

Journal: FEBS Open Bio

Article Title: Identification of small‐molecule elastase inhibitors as antagonists of IL‐36 cytokine activation

doi: 10.1002/2211-5463.12406

Figure Lengend Snippet: Several candidates identified by in silico screening exhibit inhibitory activity towards purified elastase. (A) General structural formula of LCB016 NE azolactone inhibitor. A series of azolactone analogues were synthesized with substitutions at position R 1 , R 2 or R 3 . (B) LCB016 and its derivatives (10 μ m ) were incubated with NE for 2 h at 37 °C. Elastase enzymatic activity was measured by hydrolysis of the elastase substrate peptide Suc‐AAPV‐AMC (50 μ m ). AZD9668 (1 μ m ) was used as a positive control for elastase inhibition.

Article Snippet: Suc(OMe)‐AAPV‐AMC was purchased from PeptaNova (Sandhausen, Germany); elastase inhibitor Alvelestat/AZD9668 was purchased from MedChem Express (Solentuna, Sweden).

Techniques: In Silico, Activity Assay, Purification, Synthesized, Incubation, Positive Control, Inhibition

Journal: FEBS Open Bio

Article Title: Identification of small‐molecule elastase inhibitors as antagonists of IL‐36 cytokine activation

doi: 10.1002/2211-5463.12406

Figure Lengend Snippet: Azolactone derivatives inhibit elastase activity. LCB016 and its derivatives were titrated against purified NE. Azolactone derivatives were incubated with elastase for 2 h at 37 °C, as indicated. AZD9668 (1 μ m ) was used as a positive control for elastase inhibition. Elastase enzymatic activity was measured by hydrolysis of the elastase substrate peptide Suc‐AAPV‐AMC (50 μ m ).

Article Snippet: Suc(OMe)‐AAPV‐AMC was purchased from PeptaNova (Sandhausen, Germany); elastase inhibitor Alvelestat/AZD9668 was purchased from MedChem Express (Solentuna, Sweden).

Techniques: Activity Assay, Purification, Incubation, Positive Control, Inhibition

Journal: Molecular Cell

Article Title: Polε Instability Drives Replication Stress, Abnormal Development, and Tumorigenesis

doi: 10.1016/j.molcel.2018.04.008

Figure Lengend Snippet:

Article Snippet: Rabbit polyclonal anti-GINS3 , ProteinTech , Cat#15651-1-AP; RRID: AB_2247477.

Techniques: Plasmid Preparation, Recombinant, Protease Inhibitor, Giemsa Stain, DNA Extraction, Cell Isolation, Flow Cytometry, Mutagenesis, Software