- |||||||||| RGRN-305 / Regranion, MC2 Therap
Effects of heat shock protein 90 inhibition with RGRN-305/MC2-32 on skin biomarkers in patients with hidradenitis suppurativa (Poster Area) - Aug 5, 2024 - Abstract #EADV2024EADV_1639;
P1b
HSP90 inhibition with oral RGRN-305/MC2-32 was associated with the downregulation of multiple key inflammatory genes and reduced infiltration of immune cells in the skin of hidradenitis suppurativa patients. These findings support that HSP90 inhibition exerts a broad immunomodulation of multiple inflammatory pathways, supporting its potential as a therapeutic strategy for hidradenitis suppurativa.
- |||||||||| Dovonex (calcipotriol) / LEO Pharma, Novartis, RGRN-305 / Regranion, MC2 Therap
Journal: Heat shock protein 90 inhibition attenuates inflammation in models of atopic dermatitis: a novel mechanism of action. (Pubmed Central) - Jan 30, 2024
Lastly, we discovered using Western blot that RGRN-305 disrupted JAK-STAT signaling by suppressing the activity of STAT3 and STAT6 in primary human keratinocytes, which was consistent with enrichment analyses from the mouse model. HSP90 inhibition by RGRN-305 robustly suppressed inflammation in experimental models mimicking AD, proving that HSP90 inhibition may be a novel mechanism of action in treating AD.
- |||||||||| RGRN-305 / Regranion
Journal: Heat shock protein 90 inhibitor RGRN-305 potently attenuates skin inflammation. (Pubmed Central) - Feb 24, 2023
In summary, HSP90 inhibition robustly suppressed TPA-induced inflammation by targeting key proinflammatory cytokines and signaling pathways. Our findings suggest that HSP90 inhibition may be a novel mechanism of action for treating immune-mediated skin disease beyond psoriasis, and it may be a topical treatment option.
- |||||||||| CUDC-305 / Debiopharm, Curis, BeBetter Med, Regranion
Heat Shock Protein 90 Inhibitor Attenuates Inflammation Induced by 12-O-tetradecanoylphorbol-13-acetate in Primary Human Keratinocytes and Mice (Kiosk #2) - Aug 16, 2022 - Abstract #ESDR2022ESDR_744;
Also, the inhibitory effect of RGRN-305 was associated with reduced expression of proinflammatory cytokines (TNFα, IL-1β, IL-6, IL-17A) in the ear tissue. In summary, inhibition of HSP90 mediates a robust antiinflammatory effect, providing a potential therapeutic strategy for the management of autoimmune skin diseases.
- |||||||||| CUDC-305 / Debiopharm, Curis
[VIRTUAL] METPlatform identifies brain metastasis vulnerabilities and predicts patient response to therapy (Channel 2) - Aug 20, 2021 - Abstract #EANO2021EANO_95;
Our work validates METPlatform as a potent resource for metastasis research integrating drug-screening and unbiased omic approaches that is fully compatible with human samples and questions the rationale of excluding patients with brain metastasis from clinical trials. We envision that METPlatform will be established as a clinically relevant strategy to personalize the management of metastatic disease in the brain and elsewhere.
- |||||||||| CUDC-305 / Debiopharm, Curis
[VIRTUAL] METPlatform identifies brain metastasis vulnerabilities and predicts patient response to therapy () - May 30, 2021 - Abstract #EACR2021EACR_3290;
DEBIO-0932, a blood-brain barrier permeable HSP90 inhibitor, shows high potency against mouse and human brain metastases from different primary origin and oncogenomic profile at clinically relevant stages of the disease, including a novel model of local relapse after neurosurgery...Conclusion Our work validates METPlatform as a potent resource for metastasis research integrating drug-screening and unbiased omic approaches that is fully compatible with human samples and questions the rationale of excluding patients with brain metastasis from clinical trials. We envision that METPlatform will be established as a clinically relevant strategy to personalize the management of metastatic disease in the brain and elsewhere.
- |||||||||| CUDC-305 / Debiopharm, Curis
[VIRTUAL] METPlatform identifies brain metastasis vulnerabilities and predicts patient response to therapy () - May 30, 2021 - Abstract #EACR2021EACR_3289;
DEBIO-0932, a blood-brain barrier permeable HSP90 inhibitor, shows high potency against mouse and human brain metastases from different primary origin and oncogenomic profile at clinically relevant stages of the disease, including a novel model of local relapse after neurosurgery...Conclusion Our work validates METPlatform as a potent resource for metastasis research integrating drug-screening and unbiased omic approaches that is fully compatible with human samples and questions the rationale of excluding patients with brain metastasis from clinical trials. We envision that METPlatform will be established as a clinically relevant strategy to personalize the management of metastatic disease in the brain and elsewhere.
- |||||||||| CUDC-305 / Debiopharm, Curis
[VIRTUAL] METPlatform identifies brain metastasis vulnerabilities and predicts patient response to therapy () - May 30, 2021 - Abstract #EACR2021EACR_3288;
DEBIO-0932, a blood-brain barrier permeable HSP90 inhibitor, shows high potency against mouse and human brain metastases from different primary origin and oncogenomic profile at clinically relevant stages of the disease, including a novel model of local relapse after neurosurgery...Conclusion Our work validates METPlatform as a potent resource for metastasis research integrating drug-screening and unbiased omic approaches that is fully compatible with human samples and questions the rationale of excluding patients with brain metastasis from clinical trials. We envision that METPlatform will be established as a clinically relevant strategy to personalize the management of metastatic disease in the brain and elsewhere.
- |||||||||| CUDC-305 / Debiopharm, Curis
[VIRTUAL] METPlatform identifies brain metastasis vulnerabilities and predicts patient response to therapy () - May 30, 2021 - Abstract #EACR2021EACR_3287;
DEBIO-0932, a blood-brain barrier permeable HSP90 inhibitor, shows high potency against mouse and human brain metastases from different primary origin and oncogenomic profile at clinically relevant stages of the disease, including a novel model of local relapse after neurosurgery...Conclusion Our work validates METPlatform as a potent resource for metastasis research integrating drug-screening and unbiased omic approaches that is fully compatible with human samples and questions the rationale of excluding patients with brain metastasis from clinical trials. We envision that METPlatform will be established as a clinically relevant strategy to personalize the management of metastatic disease in the brain and elsewhere.
- |||||||||| Journal: Proteomic analysis of proteome and histone post-translational modifications in heat shock protein 90 inhibition-mediated bladder cancer therapeutics. (Pubmed Central) - Sep 7, 2018
Furthermore, quantitative proteome studies identified 14 types of PTMs with 93 marks on the core histones, including 34 novel histone marks of butyrylation, citrullination, 2-hydroxyisobutyrylation, methylation, O-GlcNAcylation, propionylation, and succinylation in AUY922- and ganetespib-treated 5637 cells. Together, this study outlines the association between proteomic changes and histone PTMs in response to HSP90 inhibitor treatment in bladder carcinoma cells, and thus intensifies the understanding of HSP90 inhibition-mediated bladder cancer therapeutics.
- |||||||||| RGRN-305 / Regranion, MC2 Therap
Trial termination, Trial primary completion date, Combination therapy, IO biomarker: A Clinical Study on the Safety and Efficacy of Debio 0932 in Combination With Standard of Care in Patients With Non-small Cell Lung Cancer [NSCLC] (clinicaltrials.gov) - Dec 10, 2014
P1, N=82, Terminated,
Together, this study outlines the association between proteomic changes and histone PTMs in response to HSP90 inhibitor treatment in bladder carcinoma cells, and thus intensifies the understanding of HSP90 inhibition-mediated bladder cancer therapeutics. Recruiting --> Terminated | Trial primary completion date: Apr 2015 --> Nov 2014
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