Journal: EMBO Molecular Medicine

Article Title: LILRB1-HLA-G axis defines a checkpoint driving natural killer cell exhaustion in tuberculosis

doi: 10.1038/s44321-024-00106-1

Figure Lengend Snippet: ( A , B ) Immunoblotting ( A ) and quantitation ( B ) for expression of indicated proteins in HC-donor-derived NK cells with overexpression of MSCV or MSCV-LILRB1. Cells were co-cultured with Mtb-infected MDMs for 24 h in the presence of anti-HLA-G (87G) antibody or IgG control. ( C , D ) Immunoblotting ( C ) and quantitation ( D ) for expression of indicated proteins in HC-donor-derived NK cells co-cultured with or without Mtb-infected MDMs (Mtb-Mφ) and treated with or without dabrafenib mesylate (DM) or SCH772984 for 24 h. ( E , F ) Percentages of CD107a + ( E ) and apoptotic ( F ) cells within total NK cells from ATB patients. NK cells were co-cultured with Mtb-infected MDMs and treated with the indicated inhibitors in the presence of anti-LILRB1 (GHI/75) mAb or IgG control for 24 h. ( G ) Phosphatase activity of SHP1 and SHP2 in NK cells derived from ATB patients. Cells were treated with or without 0.5 μM TPI-1, SHP099, or NSC87877 for 24 h. ( H , I ) Immunoblotting ( H ) and quantitation ( I ) for expression of indicated proteins in ATB patient-derived NK cells. Cells were co-cultured with or without Mtb-Mφ in the presence or absence of indicated inhibitors (0.5 μM each) for 24 h. ( J , K ) Percentages of CD107a + ( J ) and apoptotic ( K ) cells within total NK cells from ATB patients. NK cells were co-cultured with Mtb-infected MDMs and treated with the indicated inhibitors in the presence of anti-LILRB1 (GHI/75) mAb or IgG control for 24 h. Data are mean ± SEM [ n = 3 donors per group in ( B , D , G , I ) and n = 5 donors per group in ( E , F , J , K )]. Statistical significance was determined using two-way ANOVA ( B , D , G , I ) and one-way ANOVA ( E , F , J , K ) with Tukey’s post-hoc test. Results are representative of three independent experiments. .

Article Snippet: For inhibition of B-raf and ERK1/2, cells were treated with 5 μM dabrafenib mesylate (Selleck, Cat# S5069) and 5 μM SCH772984 (Selleck, Cat# S7101), respectively.

Techniques: Western Blot, Quantitation Assay, Expressing, Derivative Assay, Over Expression, Cell Culture, Infection, Control, Activity Assay

Journal: EMBO Molecular Medicine

Article Title: LILRB1-HLA-G axis defines a checkpoint driving natural killer cell exhaustion in tuberculosis

doi: 10.1038/s44321-024-00106-1

Figure Lengend Snippet: Reagents and tools table

Article Snippet: For inhibition of B-raf and ERK1/2, cells were treated with 5 μM dabrafenib mesylate (Selleck, Cat# S5069) and 5 μM SCH772984 (Selleck, Cat# S7101), respectively.

Techniques: Recombinant, Western Blot, Sequencing, Modification, Cell Isolation, Enzyme-linked Immunosorbent Assay, Isolation, Antibody Labeling, Transfection, Lysis, Protease Inhibitor, Blocking Assay, Software, Flow Cytometry, Cytometry

Journal: Cellular Oncology (Dordrecht)

Article Title: Drug combination screening as a translational approach toward an improved drug therapy for chordoma

doi: 10.1007/s13402-021-00632-x

Figure Lengend Snippet: Anticancer drugs ( n = 8) exerting a shift in potency in at least one test concentration (minimum plus 20%) upon combination with an EGFR i . ALK: anaplastic lymphoma kinase. MET: MET proto-oncogene, c-MET. ROS1: ROS proto-oncogene 1. HDAC: histone deacetylase. BRAF: B-Raf proto-oncogene. Bcl-2: B cell lymphoma 2. SRC: SRC proto-oncogene. ABL: ABL proto-oncogene 1

Article Snippet: Dabrafenib mesylate , (Mutated) BRAF kinases , TAFINLAR, GlaxoSmithKline, London, UK.

Techniques: Concentration Assay, Histone Deacetylase Assay

Journal: Cellular Oncology (Dordrecht)

Article Title: Drug combination screening as a translational approach toward an improved drug therapy for chordoma

doi: 10.1007/s13402-021-00632-x

Figure Lengend Snippet: Statistical analysis of matrix screening results of n = 6 anticancer drugs (panobinostat, doxorubicin, dabrafenib, crizotinib, regorafenib and venetoclax) in combination with the EGFR i afatinib. P values ≤ 0.05 are considered significant (* p = 0.01 to 0.05; ** p = 0.001 to 0.01; *** p = 0.0001 to 0.001; **** p < 0.0001; ns: p ≥ 0.05; non-significant). Bar graphs illustrate percentages of inhibition (defined as reduction in cell viability) obtained with the anticancer drugs panobinostat (0.0064 μM; a ), doxorubicin (0.032 μM; b ), dabrafenib (0.800 μM; c ) and crizotinib (4 μM; d ), and the EGFR i afatinib (0.0064 μM), alone and in combination. Venetoclax ( e ) and regorafenib ( f ) do not induce significantly increased cell killing at comparable concentrations (anticancer drug ≤ 4 μM; afatinib ≤ 1 μM)

Article Snippet: Dabrafenib mesylate , (Mutated) BRAF kinases , TAFINLAR, GlaxoSmithKline, London, UK.

Techniques: Inhibition

Journal: Current Drug Delivery

Article Title: Drugs in the GIST Field (Therapeutic Targets and Clinical Trial Staging)

doi: 10.2174/1567201820666221122120657

Figure Lengend Snippet: Targets of drugs in active phase II clinical trials.

Article Snippet: Dabrafenib (Tafinlar, dabrafenib mesylate, 2118436, DRB-436, GSK-2118436) is a TKI targeting B-Raf [ , ] and is produced by Novartis (Table ).

Techniques:

Journal: Clinical Pharmacology and Therapeutics

Article Title: Evaluating the Role of Solubility in Oral Absorption of Poorly Water‐Soluble Drugs Using Physiologically‐Based Pharmacokinetic Modeling

doi: 10.1002/cpt.1672

Figure Lengend Snippet: Summary of biopharmaceutical properties and metabolizing CYP enzymes

Article Snippet: Dabrafenib mesylate and vemurafenib were purchased from Chem Shuttle (Hayward, CA), lapatinib ditosylate monohydrate and pazopanib hydrochloride (HCl) from Ark Pharm (Arlington Heights and Libertyville), erlotinib HCl from Activate Scientific (Prien‐Chiemsee, Germany), imatinib mesylate from abcr GmbH (Karlsruhe, Germany), and trametinib *DMSO solvate from Asta Tech (Bristol, PA).

Techniques: Solubility

Journal: Clinical Pharmacology and Therapeutics

Article Title: Evaluating the Role of Solubility in Oral Absorption of Poorly Water‐Soluble Drugs Using Physiologically‐Based Pharmacokinetic Modeling

doi: 10.1002/cpt.1672

Figure Lengend Snippet: Observed vs. predicted pharmacokinetic parameters at doses used in their clinical food effect studies and simulation using hypothetical BCS class I‐like solubility

Article Snippet: Dabrafenib mesylate and vemurafenib were purchased from Chem Shuttle (Hayward, CA), lapatinib ditosylate monohydrate and pazopanib hydrochloride (HCl) from Ark Pharm (Arlington Heights and Libertyville), erlotinib HCl from Activate Scientific (Prien‐Chiemsee, Germany), imatinib mesylate from abcr GmbH (Karlsruhe, Germany), and trametinib *DMSO solvate from Asta Tech (Bristol, PA).

Techniques: Solubility, Permeability

Journal: Clinical Pharmacology and Therapeutics

Article Title: Evaluating the Role of Solubility in Oral Absorption of Poorly Water‐Soluble Drugs Using Physiologically‐Based Pharmacokinetic Modeling

doi: 10.1002/cpt.1672

Figure Lengend Snippet: Evaluation of dose‐exposure proportionality for model compounds from the FDA's Clinical Pharmacology and Biopharmaceutics Reviews and food effect

Article Snippet: Dabrafenib mesylate and vemurafenib were purchased from Chem Shuttle (Hayward, CA), lapatinib ditosylate monohydrate and pazopanib hydrochloride (HCl) from Ark Pharm (Arlington Heights and Libertyville), erlotinib HCl from Activate Scientific (Prien‐Chiemsee, Germany), imatinib mesylate from abcr GmbH (Karlsruhe, Germany), and trametinib *DMSO solvate from Asta Tech (Bristol, PA).

Techniques:

Journal: Clinical Pharmacology and Therapeutics

Article Title: Evaluating the Role of Solubility in Oral Absorption of Poorly Water‐Soluble Drugs Using Physiologically‐Based Pharmacokinetic Modeling

doi: 10.1002/cpt.1672

Figure Lengend Snippet: Heatmap summarizing the properties in the BCS and DCS frameworks along with properties/methods used in this analysis for the identification of solubility‐limited exposure

Article Snippet: Dabrafenib mesylate and vemurafenib were purchased from Chem Shuttle (Hayward, CA), lapatinib ditosylate monohydrate and pazopanib hydrochloride (HCl) from Ark Pharm (Arlington Heights and Libertyville), erlotinib HCl from Activate Scientific (Prien‐Chiemsee, Germany), imatinib mesylate from abcr GmbH (Karlsruhe, Germany), and trametinib *DMSO solvate from Asta Tech (Bristol, PA).

Techniques: Solubility, Permeability