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PG545 sensitizes ovarian cancer cells to PARP inhibitors through modulation of RAD51-DEK interaction.
Ray U, Thirusangu P, Jin L, Xiao Y, Pathoulas CL, Staub J, Erskine CL, Dredge K, Hammond E, Block MS, Kaufmann SH, Bakkum-Gamez JN, Shridhar V. Ray U, et al. Oncogene. 2023 Sep;42(37):2725-2736. doi: 10.1038/s41388-023-02785-5. Epub 2023 Aug 7. Oncogene. 2023. PMID: 37550562 Free PMC article.
PG545 (Pixatimod) is a highly sulfated small molecule known for its ability to inhibit heparanase and disrupt signaling mediated by heparan-binding-growth factors (HB-GF). ...
PG545 (Pixatimod) is a highly sulfated small molecule known for its ability to inhibit heparanase and disrupt signaling mediated by h …
PI-88 and Related Heparan Sulfate Mimetics.
Chhabra M, Ferro V. Chhabra M, et al. Adv Exp Med Biol. 2020;1221:473-491. doi: 10.1007/978-3-030-34521-1_19. Adv Exp Med Biol. 2020. PMID: 32274723 Review.
In addition, we discuss the PI-88-inspired development of related HS mimetic heparanase inhibitors with improved properties, ultimately leading to the discovery of PG545 (pixatimod) which is currently in clinical trials....
In addition, we discuss the PI-88-inspired development of related HS mimetic heparanase inhibitors with improved properties, ultimately lead …
Heparanase Inhibition by Pixatimod (PG545): Basic Aspects and Future Perspectives.
Hammond E, Dredge K. Hammond E, et al. Adv Exp Med Biol. 2020;1221:539-565. doi: 10.1007/978-3-030-34521-1_22. Adv Exp Med Biol. 2020. PMID: 32274726 Review.
Pixatimod is an inhibitor of heparanase, a protein which promotes cancer via its regulation of the extracellular environment by enzymatic cleavage of heparan sulfate (HS) and non-enzymatic signaling. ...Clinical testing has shown pixatimod to be well tolerated as a …
Pixatimod is an inhibitor of heparanase, a protein which promotes cancer via its regulation of the extracellular environment by enzym …
Immunomodulatory Activities of the Heparan Sulfate Mimetic PG545.
Bendersky V, Yang Y, Brennan TV. Bendersky V, et al. Adv Exp Med Biol. 2020;1221:461-470. doi: 10.1007/978-3-030-34521-1_18. Adv Exp Med Biol. 2020. PMID: 32274722 Review.
For this reason, heparanase is an attractive target for the development of novel anti-cancer therapies. Pixatimod (PG545), a heparanase inhibitor, has shown promising results in the treatment of multiple tumor types. ...
For this reason, heparanase is an attractive target for the development of novel anti-cancer therapies. Pixatimod (PG545), a heparana …
Phase Ib open-label, multicenter study of pixatimod, an activator of TLR9, in combination with nivolumab in subjects with microsatellite-stable metastatic colorectal cancer, metastatic pancreatic ductal adenocarcinoma and other solid tumors.
Lemech C, Dredge K, Bampton D, Hammond E, Clouston A, Waterhouse NJ, Stanley AC, Leveque-El Mouttie L, Chojnowski GM, Haydon A, Pavlakis N, Burge M, Brown MP, Goldstein D. Lemech C, et al. J Immunother Cancer. 2023 Jan;11(1):e006136. doi: 10.1136/jitc-2022-006136. J Immunother Cancer. 2023. PMID: 36634920 Free PMC article. Clinical Trial.
BACKGROUND: Pixatimod is a unique activator of the Toll-like Receptor 9 pathway. This phase I trial evaluated safety, efficacy and pharmacodynamics of pixatimod and PD-1 inhibitor nivolumab in immunologically cold cancers. ...
BACKGROUND: Pixatimod is a unique activator of the Toll-like Receptor 9 pathway. This phase I trial evaluated safety, efficacy and ph …
Heparanase as a potential player in SARS-CoV-2 infection and induced coagulopathy.
Kinaneh S, Khamaysi I, Karram T, Hamoud S. Kinaneh S, et al. Biosci Rep. 2021 Jul 30;41(7):BSR20210290. doi: 10.1042/BSR20210290. Biosci Rep. 2021. PMID: 34132790 Free PMC article. Review.
Herein we discuss the molecular involvement of HSPGs and heparanase in SARS-CoV-2 infection, namely cell entry and release, and the accompanied coagulopathy complications, which assumedly could be blocked by heparanase inhibitors such as Heparin and Pixatimod....
Herein we discuss the molecular involvement of HSPGs and heparanase in SARS-CoV-2 infection, namely cell entry and release, and the accompan …
Development of Improved Synthetic Routes to Pixatimod (PG545), a Sulfated Oligosaccharide-Steroid Conjugate.
Chhabra M, Wimmer N, He QQ, Ferro V. Chhabra M, et al. Bioconjug Chem. 2021 Nov 17;32(11):2420-2431. doi: 10.1021/acs.bioconjchem.1c00453. Epub 2021 Oct 15. Bioconjug Chem. 2021. PMID: 34652896
The heparan sulfate (HS) mimetic pixatimod (PG545) is a highly potent inhibitor of angiogenesis, tumor growth, and metastasis currently in clinical trials for cancer. ...
The heparan sulfate (HS) mimetic pixatimod (PG545) is a highly potent inhibitor of angiogenesis, tumor growth, and metastasis current …
Synthetic Heparan Sulfate Mimetic Pixatimod (PG545) Potently Inhibits SARS-CoV-2 by Disrupting the Spike-ACE2 Interaction.
Guimond SE, Mycroft-West CJ, Gandhi NS, Tree JA, Le TT, Spalluto CM, Humbert MV, Buttigieg KR, Coombes N, Elmore MJ, Wand M, Nyström K, Said J, Setoh YX, Amarilla AA, Modhiran N, Sng JDJ, Chhabra M, Young PR, Rawle DJ, Lima MA, Yates EA, Karlsson R, Miller RL, Chen YH, Bagdonaite I, Yang Z, Stewart J, Nguyen D, Laidlaw S, Hammond E, Dredge K, Wilkinson TMA, Watterson D, Khromykh AA, Suhrbier A, Carroll MW, Trybala E, Bergström T, Ferro V, Skidmore MA, Turnbull JE. Guimond SE, et al. ACS Cent Sci. 2022 May 25;8(5):527-545. doi: 10.1021/acscentsci.1c01293. Epub 2022 Mar 29. ACS Cent Sci. 2022. PMID: 35647275 Free PMC article.
Pixatimod also retained broad potency against variants of concern (VOC) including B.1.1.7 (Alpha), B.1.351 (Beta), B.1.617.2 (Delta), and B.1.1.529 (Omicron). Furthermore, in a K18-hACE2 mouse model, pixatimod significantly reduced SARS-CoV-2 viral titers in the upp …
Pixatimod also retained broad potency against variants of concern (VOC) including B.1.1.7 (Alpha), B.1.351 (Beta), B.1.617.2 (Delta), …
Immunomodulatory activities of pixatimod: emerging nonclinical and clinical data, and its potential utility in combination with PD-1 inhibitors.
Hammond E, Haynes NM, Cullinane C, Brennan TV, Bampton D, Handley P, Karoli T, Lanksheer F, Lin L, Yang Y, Dredge K. Hammond E, et al. J Immunother Cancer. 2018 Jun 14;6(1):54. doi: 10.1186/s40425-018-0363-5. J Immunother Cancer. 2018. PMID: 29898788 Free PMC article.
Pixatimod recently completed a Phase Ia monotherapy trial in advanced cancer patients. ...CONCLUSIONS: Pixatimod modulates innate immune cells but also enhances T cell infiltration in combination with anti-PD-1 therapy. ...
Pixatimod recently completed a Phase Ia monotherapy trial in advanced cancer patients. ...CONCLUSIONS: Pixatimod modulates inn …
Structural Insights into Pixatimod (PG545) Inhibition of Heparanase, a Key Enzyme in Cancer and Viral Infections.
Chhabra M, Wilson JC, Wu L, Davies GJ, Gandhi NS, Ferro V. Chhabra M, et al. Chemistry. 2022 Feb 19;28(11):e202104222. doi: 10.1002/chem.202104222. Epub 2022 Jan 31. Chemistry. 2022. PMID: 34981584 Free PMC article.
Pixatimod (PG545), a heparan sulfate (HS) mimetic and anticancer agent currently in clinical trials, is a potent inhibitor of heparanase. ...
Pixatimod (PG545), a heparan sulfate (HS) mimetic and anticancer agent currently in clinical trials, is a potent inhibitor of heparan …
12 results