Scientific Publications and Presentations
Resources
Ribon Scientific Publications and Presentations
Niepel et al. The PARP14 inhibitor RBN-3143 suppresses skin inflammation in preclinical models. ISID 2023 Meeting. Presentation
Yap et al. First-in-Class First-in-Human Phase 1 Trial and Translational Study of the Mono (ADP-Ribose) Polymerase-7 (PARP7) Inhibitor RBN-2397 in Patients With Selected Advanced Solid Tumors. AACR Annual Meeting 2023. Presentation
Kaiko et al. Potentiation of Type I Interferon Signaling Leads to In Vivo Efficacy Achieved with Combination of Chemotherapy and the PARP7 Inhibitor RBN-2397. AACR Annual Meeting 2023. Presentation
Wong et al. PARP14 inhibition restores PD-1 immune checkpoint inhibitor response following IFNγ-driven adaptive resistance. AACR Annual Meeting 2023. Presentation
Ahumada et al. Clinical significance of PARP7 (TIPARP) gene copy number alterations in human non-small cell lung cancer and head & neck carcinomas. AACR Annual Meeting 2023. Presentation
Yap et al. First-in-Class First-in-Human Phase 1 Trial of RBN-2397 in Patients with Advanced Solid Tumors Validates PARP7 as a Novel Anticancer Therapeutic Target. ESMO Targeted Anticancer Therapies Conference 2023. Presentation
Niepel et al. The PARP14 Inhibitor RBN-3143 Suppresses Lung Inflammation in Preclinical Models. ERS International Congress 2022. Presentation
Eddie et al. Selective Pharmaceutical Inhibition of PARP14 Mitigates Allergen-Induced IgE and Mucus Overproduction in a Mouse Model of Pulmonary Allergic Response. ImmunoHorizons (2022), https://www.immunohorizons.
Kuplast-Barr K, Johnson M et al. RBN-2397, a novel, potent, and selective PARP7 inhibitor, induces tumor-intrinsic type I interferon responses and adaptive immunity in patient tumors. AACR 2022 Annual Meeting. Presentation
Molina J, Gozgit J et al. PARP7 inhibitor RBN-2397 increases tumoral IFN signaling leading to various tumor cell intrinsic effects and tumor regressions in mouse models. AACR 2022 Annual Meeting. Presentation
Gozgit et al., PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer Cell (2021), https://doi.org/10.1016/j.
Gozgit J, Vasbinder MM, Abo R et al. RBN-2397: A potent and selective small molecule inhibitor of PARP7 that induces tumor-derived antitumor immunity dependent on CD8 T cells. April 2021 AACR 2021 Virtual Annual Meeting. Presentation | Video
Wong J, Kuplast-Barr K, Abo R et al. Elevated PARP7 expression in select cancers identifies a target population for RBN-2397 therapy. April 2021 AACR 2021 Virtual Annual Meeting. Poster | Audio
Gui B, Abo R, Flynn P et al. Investigating the mechanism of PARP7 inhibition in Type I interferon signaling by arrayed CRISPR screening. April 2021 AACR 2021 Virtual Annual Meeting. Poster | Audio
Wigle T, Ren Y, Molina J et al. Targeted degradation of PARP14 using a heterobifunctional small molecule. April 2021 AACR 2021 Virtual Annual Meeting. Poster | Audio
Shambarkhar PB, Blackwell DJ, Vasbinder MM et al. Small molecule inhibitor of CD38 modulates its intra- and extracellular functions leading to antitumor activity. April 2021 AACR 2021 Virtual Annual Meeting. Poster | Audio
Falchook GS, Patel MR, Yap TA et al. A first-in-human phase 1 study of a novel PARP7 inhibitor RBN-2397 in patients with advanced solid tumors. 2021 ASCO Annual Meeting. Poster
Wigle T, Ren Y, Molina JR et al. Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule. ChemBioChem (2021). https://doi.org/10.1002/cbic.
Schenkel et al., A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants. Cell Chemical Biology (2021), https://doi.org/10.1016/j.chembiol.2021.02.010.
Wigle TJ. A Bespoke Screening Platform to Study Mono(ADP-ribosylation). Jan 2021 PARP & DDR Inhibitors Digital Summit 2021. Presentation | Video
Wigle TJ, Blackwell DJ, Schenkel LB, Ren Y, Church DW, Desai, HJ, Swinger KK, Santospago AG, Majer CR, Lu AZ, Niepel M, Perl NR, Vasbinder MM, Keilhack H, Kuntz KW. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement. Cell Chemical Biology (2020); 27:877-887. doi: 10.1016/j.chembiol.2020.06.009.
Gozgit, JM. PARP7 negatively regulates the Type I interferon response in cancer cells and its inhibition leads to tumor regression. June 2020 American Association of Cancer Research (AACR) Virtual Annual Meeting II. Presentation | Video
Wigle TJ, Blackwell DJ, Schenkel LB, Swinger KK, Vasbinder MM, Ren Y, Church WD, Majer CR, Desai HJ, Perl NR, Santospago AG, Lu AZ, Niepel M, Keilhack H, Kuntz KW. A bespoke screening platform to study mono(ADP-ribosylation). 2020 American Association of Cancer Research (AACR) Virtual Annual Meeting II. Poster | Audio
Abo RP, Niepel M, Keilhack, H. A multi-omic characterization of PARP enzymes in cancer to identify novel monoPARP drug targets. June 2020 American Association of Cancer Research (AACR) Virtual Annual Meeting II. Poster | Audio
Vasbinder MM, Gozgit JM, Abo RP, Kunii K, Kuplast-Barr KG, Gui B, Lu AZ, Swinger KK, Wigle TJ, Blackwell DJ, Majer CR, Ren Y, Niepel M, Varsamis ZA, Nayak SP, Bamberg E, Mo JR, Church WD, Song J, Utley L, Rao PE, Mitchison TJ, Kuntz KW, Richon VM, Keilhack H. RBN-2397 – A First-in-Class PARP7 Inhibitor Targeting a Newly Discovered Cancer Vulnerability in Stress-Signaling Pathways. April 2020 American Association of Cancer Research (AACR) Virtual Annual Meeting I. Presentation | Video
Schenkel L, Molina J, Swinger KK, Abo RP, Blackwell DJ, Cheung A, Church WD, Kuplast-Barr KG, Lu AZ, Minissale E, Niepel M, Vasbinder MM, Wigle TJ, Richon VM, Keilhack H, Kuntz KW. RBN012759 – A Potent and Selective PARP14 Inhibitor Decreases Pro-tumor Macrophage Function and Elicits Inflammatory Responses in Tumor Explants. April 2020 American Association of Cancer Research (AACR) Virtual Annual Meeting I. Presentation | Video
Wigle TJ, Church WD, Majer CR, Swinger KK, Aybar D, Schenkel LB, Vasbinder MM, Brendes A, Beck C, Prahm M, Wegener D, Chang P, Kuntz KW. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes. SLAS Discovery (2019); doi: 10.1177/2472555219883623.
Church WD, Majer CR, Swinger KK, Aybar D, Santospago AG, Perl NR, Schenkel LB, Vasbinder MM, Kuntz KW, Wigle TJ. Development of Novel Biochemical Assays for the Screening of MonoPARP Enzymes. Society for Laboratory Automation and Screening (SLAS) January 2020 International Conference and Exhibition.
Lu AZ, Abo R, Ren Y, Gui B, Mo J, Blackwell D, Wigle TJ, Keilhack H, Niepel M. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation. Biochem Phamacol (2019); 167:97-106. doi: 10.1016/j.bcp.2019.05.007.
Lu AZ, Najjar R, Niepel M, Stokes M. Novel antibody reagents for the characterization of protein ADP-ribosylation. April 2018 Cold Springs Harbor Laboratory Meeting on the PARP Family and ADP-Ribosylation.
Swinger K, Wigle TJ, Wei P, Zhang S, Tong S, Chang P, Kuntz KW. Co-crystal structure of PARP16 bound to its physiological cofactor NAD+. April 2018 Cold Springs Harbor Laboratory Meeting on the PARP Family and ADP-Ribosylation.
Selected Scientific References
Cellular Stress and Disease
Luo J, Solimini NL, Elledge SJ. Principles of cancer therapy: oncogene and non-oncogene addiction. Cell. (2009); 136(5): 823-37. doi: 10.1016/j.cell.2009.02.024.
Paludan SR, Reinert, Ls, Hornung V. DNA-stimulated cell death: implications for host defence, inflammatory diseases and cancer. Nat Rev Immunol. (2019); 19(3): 141-153. doi: 10.1038/s41577-018-0117-0.
Costa-Mattioli M, Walter P. The integrated stress response: From mechanism to disease. Science (2020); 368 (6489): eaat5314. doi: 10.1126/science.aat5314
PARP Family
Luscher B, et al. ADP-ribosyltransferases, an update on function and nomenclature. FEBS. (2021). https://doi.org/10.1111/FEBS.
Bock FJ, Chang P. New Directions in PARP Biology. FEBS J. (2016); doi: 10.1111/febs.13737.
Kim D-S, Challa S, Jones A, Kraus WL. PARPs and ADP-ribosylation in RNA biology: from RNA expression and processing to protein translation and proteostasis. Genes Dev. (2020 Mar); doi: 10.1101/gad.334433.119.
Vyas S, Matic I, Uchima L, Rood J, Zaha R, Hay RT, Ahel I, Chang P. Family-wide analysis of poly(ADP-ribose) polymerase activity. Nat Commun. (2014); 5:4426. doi: 10.1038/ncomms5426.
Vyas S, Chang P. New PARP targets for cancer therapy. Nat Rev Cancer (2014); 14:502-9. doi: 10.1038/nrc3748.
Cohen MS, Chang P. Insights into the biogenesis, function, and regulation of ADP-ribosylation. Nat Chem Biol. (2018); doi: 10.1038/nchembio.2568.