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- | amitriptyline / Generic mfg.
Journal: Antidepressants induce profibrotic responses via the lysophosphatidic acid receptor LPA. (Pubmed Central) - Nov 28, 2020
In both cell types amitriptyline, clomipramine and mianserin mimicked the ability of LPA to induce the phosphorylation/activation of extracellular signal -regulated kinases 1 and 2 (ERK1/2), which was blocked by the selective LPA receptor antagonist AM966 and the LPA antagonist Ki16425...Like LPA, antidepressants stimulated fibroblasts proliferation and this effect was blocked by either AM966 or the MEK1/2 inhibitor PD98059...Pharmacological blockade of TGF-β receptor type 1 prevented antidepressant- and LPA-induced α-SMA expression. These data indicate that in human dermal and lung fibroblasts different antidepressants can induce proliferative and differentiating responses by activating the LPA receptor coupled to ERK1/2 signalling and suggest that this property may contribute to the promotion of tissue fibrosis by these drugs.
- LPA pathway modulators (AM-966) / , AM 095 / BMS
[VIRTUAL] LPA1 signal transduction drives Schwann cell dedifferentiation in experimental autoimmune neuritis () - Nov 28, 2020 - Abstract #DGN2020DGN_322;
The myelin thickness was not affected by AM095 treatment. These results suggest that disruption of LPA1 signal transduction may represent a new therapeutic target for the treatment of inflammatory neuropathies that may modulate the regenerative responses in the peripheral nerve Schwann cell differentiation.
- | LPA pathway modulators (AM-966) / , AM 095 / BMS
Journal: Inhibition of LPA Signaling Impedes Conversion of Human Tenon's Fibroblasts into Myofibroblasts Via Suppressing TGF-β/Smad2/3 Signaling. (Pubmed Central) - Jun 19, 2020
By using an LPA-specific inhibitor, AM095, we confirmed that LPA signaling but not LPA or LPA is involved in TGF-β1 induced HTFs activation. Our results show that inhibition of LPA signaling presents potent antifibrotic effect in HTFs, which may serve as a promising intervention strategy for preventing subconjunctival fibrosis caused by glaucoma filtration surgery.
- | LPA pathway modulators (AM-966) / , AM 095 / BMS
Journal: Lysophosphatidic acid receptor 1 (LPA) plays critical roles in microglial activation and brain damage after transient focal cerebral ischemia. (Pubmed Central) - Feb 14, 2020
Our results show that inhibition of LPA signaling presents potent antifibrotic effect in HTFs, which may serve as a promising intervention strategy for preventing subconjunctival fibrosis caused by glaucoma filtration surgery. This study demonstrates that LPA is a new etiological factor for cerebral ischemia, strongly indicating that its modulation can be a potential strategy to reduce ischemic brain damage.
- | LPA pathway modulators (AM-966) / , AM 095 / BMS
Preclinical, Journal, IO Biomarker: Lysophosphatidic acid receptor 1 inhibitor, AM095, attenuates diabetic nephropathy in mice by downregulation of TLR4/NF-κB signaling and NADPH oxidase. (Pubmed Central) - Feb 7, 2020
Pharmacological or siRNA inhibition of TLR4 and NADPH oxidase mimicked the effects of AM095 in vitro. In conclusion, AM095 is effective in preventing the pathogenesis of DN by inhibiting TLR4/NF-κB and the NADPH oxidase system, consequently inhibiting the inflammatory signaling cascade in renal tissue of diabetic mice, suggesting that LPAR1 antagonism might provide a potential therapeutic target for DN.
- || LPA pathway modulators (AM-966) /
Wow! That worked out well. I am 966 followers away from 1k. Can I pass that by the time I see @VicOladipo return to @Pacers tonight? (Twitter) - Jan 29, 2020
- | ondansetron / Generic mfg., mirtazapine / Generic mfg.
Preclinical, Journal: Mirtazapine increases glial cell line-derived neurotrophic factor production through lysophosphatidic acid 1 receptor-mediated extracellular signal-regulated kinase signaling in astrocytes. (Pubmed Central) - Jan 10, 2020
The current findings demonstrate that the NaSSA mirtazapine, similar to other classes of antidepressants, increases GDNF expression through a Gi/o coupled LPA receptor-mediated ERK pathway. The current findings suggest a general mechanism underlying the psychotropic effect antidepressants.
- |||| LPA pathway modulators (AM-966) / , AM 095 / BMS
Checkpoint inhibition: Simultaneously, @NCItreatment also developed CITN12, as noted earlier, and AMC095. But we didn’t wait for those results to push for inclusion on our other immune checkpoint inhibitor trials. (Twitter) - Dec 1, 2019
- MK-2206 / Merck (MSD), LPA pathway modulators (AM-966) /
Radiation Inducing Pulmonary Cellular Senescence through the LPA-LPA1-Akt Pathway (Room W192) - Sep 24, 2019 - Abstract #ASTRO2019ASTRO_4623;
All above were ameliorated by AM966 or MK2206 pretreatment, while SC79 could counteract the effect of AM966.Conclusion LPA in high concentrations participates in the radiation-induced pulmonary cellular senescence through the LPA-LPA1-Akt signaling. Selectively blocking LPA1 by AM966 in the early stage could significantly ameliorate pulmonary cellular senescence and injuries.
- | LPA pathway modulators (AM-966) / , PF-8380 / Pfizer, AM 095 / BMS
Journal: Pharmacologic targeting of the ATX/LPA axis attenuates bleomycin-induced pulmonary fibrosis. (Pubmed Central) - Mar 29, 2019
In this report, we examined head-to-head the efficacy of a potent inhibitor of ATX (PF-8380), that has not been tested in pulmonary fibrosis models, and an antagonist of LPAR1 (AM095) in bleomycin (BLM)-induced pulmonary fibrosis. Both compounds abrogated the development of pulmonary fibrosis and prevented the distortion of lung architecture, exhibiting qualitative and quantitative differences in different manifestations of the modeled disease.