Krzysztof Matyszewski

Structure-Guided Discovery of OAT-4828 as Potent, Selective, and Orally Bioavailable USP7 Inhibitor with In Vivo Antileukemic Activity

Jacek Chrzanowski, Julita Nowicka, Robert Koralewski, Łukasz Joachimiak et autres

Ubiquitin-specific protease 7 (USP7) is a deubiquitinating enzyme implicated in cancer development via stabilization of oncogenic proteins and immunosuppressive factors. We used a structure-based approach to design selective USP7 inhibitors to exploit this therapeutic target. Starting from allosteric USP7 ligand scaffolds, we …

pl (code pays fourni par la source)

Supplementary Figure 21 from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

Allometric scaling of human volume of distribution (V-SAfu)

Supplementary Tables 1-11 from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

In vitro activity; data collection of hARG1 – OATD-02 complex crystal; PK data; HED and MRSD calculations; projected human exposure to OATD-02

Supplementary Figure 1 from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

The immunosuppressive character of ARG1 and ARG2 in the tumor microenvironment (TME)

Supplementary Figure 15 from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

Crystal structure of OATD-02 bound to hARG1

Supplementary Figure 17 from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

Analysis of B16F10 tumor growth in mice treated with OATD-02 in all individuals subjected to the study.

Supplementary Figure 16 from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

PK and PD effects after intravenous administration of OATD-02 and CB-1158 in Sprague-Dawley rats

Supplementary Materials and Methods from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

Supplementary Materials and Methods not included in the main manuscript

Supplementary Figure 23 from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

Simulated human plasma concentration time profiles of OATD-02

Supplementary Figure 19 from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

Allometric scaling of human plasma clearance (CL-ROE)

Supplementary Figure 18 from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

Individual body weight changes in animals treated with OATD-02

Supplementary Figure 20 from Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy

Bartlomiej Borek, Julita Nowicka, Anna Gzik, Marek Dzięgielewski et autres

Allometric scaling of human plasma clearance (CL-NAS)