Nathaniel L. Elsen

Structure-Based Drug Design of Quinoline CYP8B1 Inhibitors for the Potential Treatment of Metabolic Disease

Amy Bittner McCracken, Derun Li, John P. Caldwell, Claire Lankin et autres

Abstract CYP8B1 has been identified as a potential target for the treatment of metabolic diseases, such as nonalcoholic fatty liver disease (NAFLD) and type 2 diabetes (T2D). CYP8B1 enzyme inhibitor 1 was discovered from a high-throughput screen of our compound collection; however, …

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Table S1 from Microsatellite Instable Cancer Cells Acquire On-target Resistance Mutations to WRN Helicase Inhibitors

Faith C. Fowler, Jessica Gajda, Amirhossein Mafi, Aileen Kelly et autres

Summary of cellular and biochemical IC50 values for each WRN mutation and inhibitor.

Data from Microsatellite Instable Cancer Cells Acquire On-target Resistance Mutations to WRN Helicase Inhibitors

Faith C. Fowler, Jessica Gajda, Amirhossein Mafi, Aileen Kelly et autres

Abstract The Werner syndrome helicase (WRN) is a promising target for cancers with microsatellite instability (MSI), leading to the initiation of at least five phase I clinical trials. Acquired resistance is a substantial obstacle to obtaining lasting benefits from targeted therapies in …

Figure S5 from Microsatellite Instable Cancer Cells Acquire On-target Resistance Mutations to WRN Helicase Inhibitors

Faith C. Fowler, Jessica Gajda, Amirhossein Mafi, Aileen Kelly et autres

DNA unwinding activity of WRN mutant proteins

Table S2 from Microsatellite Instable Cancer Cells Acquire On-target Resistance Mutations to WRN Helicase Inhibitors

Faith C. Fowler, Jessica Gajda, Amirhossein Mafi, Aileen Kelly et autres

Summary of SPR data.

Figure S2 from Microsatellite Instable Cancer Cells Acquire On-target Resistance Mutations to WRN Helicase Inhibitors

Faith C. Fowler, Jessica Gajda, Amirhossein Mafi, Aileen Kelly et autres

Related to figure 2. (A) SPR sensorgrams of WRN WT and G729D treated with AC1 and AC2 (B) SPR sensorgram of WRN WT and D526_P530del treated with AC1 (C) Top: IGV browser window of whole exome sequencing variant calling file for AC1-resistant …

Figure S4 from Microsatellite Instable Cancer Cells Acquire On-target Resistance Mutations to WRN Helicase Inhibitors

Faith C. Fowler, Jessica Gajda, Amirhossein Mafi, Aileen Kelly et autres

Related to figure 4. (A) SPR sensorgram of WRN WT and F730L treated with AC1 (B) As in (A) with AC2 (C) As in (A) with C727R (D) SPR sensorgram of WRN WT and L528S treated with HRO761 (E) SPR sensorgram of …

Figure S1 from Microsatellite Instable Cancer Cells Acquire On-target Resistance Mutations to WRN Helicase Inhibitors

Faith C. Fowler, Jessica Gajda, Amirhossein Mafi, Aileen Kelly et autres

Related to figure 1. (A) SPR sensorgrams of WT WRN treated with AC1 and AC2. (B) DNA unwinding activity of wildtype WRN in the presence of AC1 and AC2. (C) Molecular docking of AC1 bound to the WRN helicase region (D) Viability …

Figure S3 from Microsatellite Instable Cancer Cells Acquire On-target Resistance Mutations to WRN Helicase Inhibitors

Faith C. Fowler, Jessica Gajda, Amirhossein Mafi, Aileen Kelly et autres

Related to figure 3. (A) Mean tumor volume measurements (± SEM) in a HRO71-resistant SW48 xenograft model treated with vehicle or 120 mg/kg HRO761 (n = 10 mice per treatment group). (B) Mean body weight of mice corresponding to figure 3A (C) …

Supplementary Figure 2 from Inhibition of MALT1 and BCL2 Induces Synergistic Antitumor Activity in Models of B-Cell Lymphoma

Joshua P. Plotnik, Adam E. Richardson, Haopeng Yang, Estela Rojas et autres

Whole proteomic analysis of ABBV-MALT1 in OCI-LY3

Supplementary File 1 from Inhibition of MALT1 and BCL2 Induces Synergistic Antitumor Activity in Models of B-Cell Lymphoma

Joshua P. Plotnik, Adam E. Richardson, Haopeng Yang, Estela Rojas et autres

Excel Workbook ABBV-MALT1 Pharmacology

Supplementary Figure 4 from Inhibition of MALT1 and BCL2 Induces Synergistic Antitumor Activity in Models of B-Cell Lymphoma

Joshua P. Plotnik, Adam E. Richardson, Haopeng Yang, Estela Rojas et autres

Efficacy of ABBV-MALT1 across non-GCB PDX models