a calpain inhibitor iv  (Gilead Sciences)

Journal: Heliyon

Article Title: Discovery of Clioquinol and analogues as novel inhibitors of Severe Acute Respiratory Syndrome Coronavirus 2 infection, ACE2 and ACE2 - Spike protein interaction in vitro

doi: 10.1016/j.heliyon.2021.e06426

Figure Lengend Snippet: Efficacy of Reference Inhibitors against SARS-CoV-2 induced Cytopathic Effect (CPE) in Vero E6 cells: A. Calpain Inhibitor IV, B. Chloroquine, C Remdesivir, D. Hydroxychloroquine, and E. E64d (Aloxistatin).

Article Snippet: Efficacy of Reference Inhibitors against SARS-CoV-2 induced Cytopathic Effect (CPE) in Vero E6 cells: A. Calpain Inhibitor IV, B. Chloroquine, C Remdesivir, D. Hydroxychloroquine, and E. E64d (Aloxistatin).

Techniques:

Journal: Heliyon

Article Title: Discovery of Clioquinol and analogues as novel inhibitors of Severe Acute Respiratory Syndrome Coronavirus 2 infection, ACE2 and ACE2 - Spike protein interaction in vitro

doi: 10.1016/j.heliyon.2021.e06426

Figure Lengend Snippet: Chemical Structure and Activity of Reference Inhibitors against SARS-CoV-2 induced Cytopathic Effect (CPE) in Vero E6 Cells.

Article Snippet: Efficacy of Reference Inhibitors against SARS-CoV-2 induced Cytopathic Effect (CPE) in Vero E6 cells: A. Calpain Inhibitor IV, B. Chloroquine, C Remdesivir, D. Hydroxychloroquine, and E. E64d (Aloxistatin).

Techniques: Activity Assay, Inhibition, Concentration Assay

Journal: Heliyon

Article Title: Discovery of Clioquinol and analogues as novel inhibitors of Severe Acute Respiratory Syndrome Coronavirus 2 infection, ACE2 and ACE2 - Spike protein interaction in vitro

doi: 10.1016/j.heliyon.2021.e06426

Figure Lengend Snippet: Cytotoxicity of Clioquinol (CLQ) and analogues in Vero E6 cells, in comparison to reference inhibitors of SARS-CoV-2.

Article Snippet: Efficacy of Reference Inhibitors against SARS-CoV-2 induced Cytopathic Effect (CPE) in Vero E6 cells: A. Calpain Inhibitor IV, B. Chloroquine, C Remdesivir, D. Hydroxychloroquine, and E. E64d (Aloxistatin).

Techniques: Concentration Assay

Journal: Biomaterials

Article Title: Integrin α 6 and EGFR Signaling Converge at Mechanosensitive Calpain 2

doi: 10.1016/j.biomaterials.2018.05.056

Figure Lengend Snippet: (a) Clustering of PCR data on genes expressed after 24 hours of culture on gels functionalized with 10μg/cm2 collagen 1 (data in Fig. 1a). (b) Calpain 2 activity during adhesion was measured by evaluating the ratio of autolyzed/full length calpain 2 via western blot in both the adhered and suspended cell fractions during the first 60 minutes, or just the adhered fraction after 24 hours. N=2. (c-d) Cell area was quantified during adhesion in the presence of an ERK1/2 inhibitor or calpain 2 inhibitor on 1 kPa (c) and 41 kPa (d) gels. N=2, n=50. (e) Cell migration speeds quantified the presence of an ERK1/2 or calpain 2 inhibitor. N=2, n=48. (f) Representative western blot for full length and autolyzed calpain 2, with loading control GAPDH. In order of lanes from left to right: 1 kPa with collagen 1, 41 kPa with collagen 1, TCPS, 1 kPa with collagen 1 + 100ng/mL soluble EGF for 10 minutes, 41 kPa with collagen 1 + 100ng/mL soluble EGF for 10 minutes, TCPS + 100ng/mL soluble EGF for 10 minutes, 1 kPa with collagen and laminin, 41 kPa with collagen and laminin.

Article Snippet: For inhibitor conditions, cells were treated 2 hours prior to the start of imaging with 10 μg/mL calpain inhibitor IV, 20 μM ERK inhibitor {"type":"entrez-nucleotide","attrs":{"text":"FR180204","term_id":"258307209"}} FR180204 , 20 μM lapatinib, or 10 ng/mL EGF (R&D Systems).

Techniques: Activity Assay, Western Blot, Migration

Journal: Biomaterials

Article Title: Integrin α 6 and EGFR Signaling Converge at Mechanosensitive Calpain 2

doi: 10.1016/j.biomaterials.2018.05.056

Figure Lengend Snippet: (a) Breast cancer cells on soft gels, or any stiffness gel supplemented with EGF, were small and motile. Cells on soft gels produced their own laminin to engage α6, or we added it exogenously. Our data suggests this increases activation of ERK and Calpain 2, which feeds back to increase turnover of focal adhesions. (b) During adhesion to substrates, cells were more responsive to laminin on soft substrates but did not adhere as well on stiff substrates with a calpain 2 inhibitor. Cell adhesion was facilitated in the presence of EGF on both soft and stiff gels. After 24 hours on gels, calpain 2 activity decreased with increasing stiffness, while EGFR phosphorylation increased with stiffness without added EGF. Cell motility had a biphasic dependence on substrate stiffness.

Article Snippet: For inhibitor conditions, cells were treated 2 hours prior to the start of imaging with 10 μg/mL calpain inhibitor IV, 20 μM ERK inhibitor {"type":"entrez-nucleotide","attrs":{"text":"FR180204","term_id":"258307209"}} FR180204 , 20 μM lapatinib, or 10 ng/mL EGF (R&D Systems).

Techniques: Produced, Activation Assay, Activity Assay