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About 52,080 results

Safety and efficacy of bexarotene in patients with relapsing-remitting multiple scleros...
https://doi.org/10.1016/S1474-4422(21)00179-4
The Lancet. Neurology; Brown JWL, Cunniffe NG et. al.

Aug 22nd, 2021 - Progressive disability in multiple sclerosis occurs because CNS axons degenerate as a late consequence of demyelination. In animals, retinoic acid receptor RXR-gamma agonists promote remyelination. We aimed to assess the safety and efficacy of a non-selective retinoid X receptor agonist in promoting remyelination in people with multiple sclerosis. This randomised, double-blind, placebo-controll...

The effect of Gö6976 on chronic myeloid leukemia in vitro and in vivo.
https://doi.org/10.1080/16078454.2021.1945235
Hematology (Amsterdam, Netherlands); Cao ZR, Chen XP et. al.

Aug 6th, 2021 - Objectives: Chronic myeloid leukemia (CML) is a malignant tumor of the blood system. Gö6976, as a type of indolocarbazole and shows strong antitumor effects, but there have been no reports on the effect of Gö6976 on CML. The objectives of this research were: (1) to explore the impact of Gö6976 on CML in vitro and in vivo; and (2) to explore the drug toxicity of Gö6976 to normal cells and animal...

miR‑351‑5p aggravates lipopolysaccharide‑induced acute lung injury via inhibiting AMPK.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8365417
Molecular Medicine Reports; Hu F, Dong X et. al.

Jul 31st, 2021 - Inflammation and oxidative stress have indispensable roles in the development of acute lung injury (ALI). MicroRNA (miRNA/miR)‑351‑5p was initially identified as a myogenesis‑associated miRNA; however, its role in lipopolysaccharide (LPS)‑induced ALI remains unclear. The aim of the present study was to investigate the role and potential mechanisms of miR‑351‑5p in ALI. ALI was induced through a...

STING suppresses bone cancer pain via immune and neuronal modulation.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8316360
Nature Communications; Wang K, Donnelly CR et. al.

Jul 29th, 2021 - Patients with advanced stage cancers frequently suffer from severe pain as a result of bone metastasis and bone destruction, for which there is no efficacious treatment. Here, using multiple mouse models of bone cancer, we report that agonists of the immune regulator STING (stimulator of interferon genes) confer remarkable protection against cancer pain, bone destruction, and local tumor burden...

Romiplostim in children with newly diagnosed or persistent primary immune thrombocytope...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8310729
Annals of Hematology; Grainger JD, Kühne T et. al.

Jul 27th, 2021 - Immune thrombocytopenia (ITP) is a disease of heterogenous origin characterized by low platelet counts and an increased bleeding tendency. Three disease phases have been described: newly diagnosed (≤ 3 months after diagnosis), persistent (> 3-12 months after diagnosis), and chronic (> 12 months after diagnosis). The majority of children with ITP have short-lived disease and will not need treatm...

Modulation of PPAR signaling disrupts pancreas development in the zebrafish, Danio rerio.
https://doi.org/10.1016/j.taap.2021.115653
Toxicology and Applied Pharmacology; Venezia O, Islam S et. al.

Jul 25th, 2021 - Peroxisome Proliferator Activated Receptors (PPARs) are transcription factors that regulate processes such as lipid and glucose metabolism. Synthetic PPAR ligands, designed as therapeutics for metabolic disease, provide a tool to assess the relationship between PPAR activity and pancreas development in vivo, an area that remains poorly characterized. Here, we aim to assess the effects of PPAR a...

A human CD137×PD-L1 bispecific antibody promotes anti-tumor immunity via context-depend...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8295259
Nature Communications; Geuijen C, Tacken P et. al.

Jul 23rd, 2021 - Immune checkpoint inhibitors demonstrate clinical activity in many tumor types, however, only a fraction of patients benefit. Combining CD137 agonists with these inhibitors increases anti-tumor activity preclinically, but attempts to translate these observations to the clinic have been hampered by systemic toxicity. Here we describe a human CD137xPD-L1 bispecific antibody, MCLA-145, identified ...

SAR1B senses leucine levels to regulate mTORC1 signalling.
https://doi.org/10.1038/s41586-021-03768-w 10.1038/ncb2763 10.1016/j.cell.2006.01.016 10.1038/nrm3522 10.1126/science.1232044 10.1016/j.cell.2016.02.035 10.1126/science.aab2674 10.1038/ncb2390 10.1126/science.1157535 10.1038/nature21423 10.1002/(SICI)1097-4644(20000501)77:2<234::AID-JCB7>3.0.CO;2-I 10.1093/jn/131.3.861S 10.1038/ncomms3267 10.7554/eLife.31268 10.1038/426620a 10.1038/nature08221 10.1016/j.ccr.2007.05.008 10.1080/15384101.2015.1084447 10.1172/JCI108201 10.1038/s41586-018-0128-9
Nature Chen J, Ou Y et. al.

Jul 23rd, 2021 - The mTOR complex 1 (mTORC1) controls cell growth in response to amino acid levels1. Here we report SAR1B as a leucine sensor that regulates mTORC1 signalling in response to intracellular levels of leucine. Under conditions of leucine deficiency, SAR1B inhibits mTORC1 by physically targeting its activator GATOR2. In conditions of leucine sufficiency, SAR1B binds to leucine, undergoes a conformat...

Refractoriness of STING therapy is relieved by AKT inhibitor through effective vascular...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8292391
Nature Communications; Jeong SH, Yang MJ et. al.

Jul 22nd, 2021 - Stimulator of interferon genes (STING) promotes anti-tumour immunity by linking innate and adaptive immunity, but it remains unclear how intratumoural treatment with STING agonists yields anti-tumour effects. Here we demonstrate that intratumoural injection of the STING agonist cGAMP induces strong, rapid, and selective apoptosis of tumour endothelial cells (ECs) in implanted LLC tumour, melano...

Tetrasubstituted imidazoles as incognito Toll-like receptor 8 a(nta)gonists.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8285539
Nature Communications; Yang Y, Csakai A et. al.

Jul 18th, 2021 - Small-molecule modulators of TLR8 have drawn much interests as it plays pivotal roles in the innate immune response to single-stranded RNAs (ssRNAs) derived from viruses. However, their clinical uses are limited because they can invoke an uncontrolled, global inflammatory response. The efforts described herein culminate in the fortuitous discovery of a tetrasubstituted imidazole CU-CPD107 which...

N-acylethanolamine regulation of TLR3-induced hyperthermia and neuroinflammatory gene e...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8243641
Journal of Neuroimmunology; Flannery LE, Kerr DM et. al.

Jul 16th, 2021 - Increasing evidence suggests that SARS-CoV-2, the virus responsible for the COVID-19 pandemic, is associated with increased risk of developing neurological or psychiatric conditions such as depression, anxiety or dementia. While the precise mechanism underlying this association is unknown, aberrant activation of toll-like receptor (TLR)3, a viral recognizing pattern recognition receptor, may pl...

Effectiveness and safety of romiplostim among patients with newly diagnosed, persistent...
https://doi.org/10.1080/16078454.2021.1948209
Hematology (Amsterdam, Netherlands); Skopec B, Sninska Z et. al.

Jul 10th, 2021 - The objective of this analysis was to assess the effectiveness and safety of romiplostim in the real-world by duration of primary immune thrombocytopenia (ITP): <3 ('newly diagnosed'), 3-12 ('persistent'), and >12 ('chronic') months. This was a post-hoc analysis of the PLATON single-arm, observational cohort study of adults from five Central and Eastern European countries receiving ≥1 romiplost...

Treating cognitive impairment in schizophrenia with GLP-1RAs: an overview of their ther...
https://doi.org/10.1080/13543784.2021.1951702
Expert Opinion on Investigational Drugs; Flintoff J, Kesby JP et. al.

Jul 3rd, 2021 - Schizophrenia is a neuropsychiatric disorder that affects approximately 1% of individuals worldwide. There are no available medications to treat cognitive impairment in this patient population currently. Preclinical evidence suggests that glucagon-like peptide-1 receptor agonists (GLP-1 RAs) improve cognitive function. There is a need to evaluate how GLP-1 RAs alter specific domains of cognitio...

Intensive Medical Management to Prevent Large and Small Artery Atherothrombotic Stroke:...
https://doi.org/10.1001/jama.2021.9917
JAMA Lee M, Ovbiagele B et. al.

Jul 2nd, 2021 - Intensive Medical Management to Prevent Large and Small Artery Atherothrombotic Stroke: Time to Expand the Horizon.|2021|Lee M,Ovbiagele B,Saver JL,|analogs & derivatives,blood,therapeutic use,therapeutic use,agonists,drug therapy,therapeutic use,therapeutic use,prevention & control,

GPR40 receptor agonist TAK-875 improves cognitive deficits and reduces β-amyloid produc...
https://doi.org/10.1007/s00213-021-05837-4 10.1002/jbt.22345 10.1074/jbc.M110.183608 10.1016/j.pharmthera.2013.12.009 10.1002/hipo.20732 10.1074/jbc.M211495200 10.1038/sj.bjp.0706770 10.1016/j.nbd.2018.07.002 10.1007/BF03402076 10.1007/s11745-000-0646-3 10.1016/j.plipres.2009.04.001 10.1038/s41598-020-68110-2 10.1073/pnas.0403921101 10.1016/j.neuropharm.2019.107899 10.1021/acs.jmedchem.6b00892 10.1046/j.1471-4159.2002.00905.x 10.1093/jn/135.3.549 10.1038/nature01478 10.1016/j.neuroscience.2014.01.003 10.1016/j.neurobiolaging.2015.05.010 10.1038/nature11283 10.1111/dom.12467 10.1093/toxsci/kfx058 10.1016/j.nlm.2016.03.006 10.3233/JAD-2011-111010 10.1124/dmd.115.064121 10.1016/j.neuroscience.2007.01.024 10.1016/j.neures.2007.05.001 10.1016/j.brainres.2010.03.002 10.1016/S0896-6273(02)00942-X 10.1111/bph.14054 10.1371/journal.pone.0081563 10.1021/ml1000855 10.1016/S0014-5793(00)02076-7 10.1093/toxsci/kfx040 10.1016/j.febslet.2014.05.017 10.1172/JCI78464 10.1056/NEJMra0909142 10.3389/fnagi.2019.00315 10.1038/s41573-020-0065-9 10.1038/375754a0 10.1159/000213716 10.1073/pnas.082107399 10.1186/s12974-018-1255-9 10.1523/JNEUROSCI.2211-04.2004 10.1016/B978-0-12-420170-5.00002-7 10.1186/s13041-019-0447-2 10.1111/bcpt.12581 10.1007/s00213-009-1526-3 10.1007/s00401-015-1387-2 10.1016/j.neuron.2004.09.010 10.1038/srep25912 10.1126/sciadv.aau2357 10.1002/hipo.22263 10.1016/j.pnpbp.2017.09.017 10.1002/ana.24361 10.1016/j.nbd.2010.10.001
Psychopharmacology Liu C, Cheng ZY et. al.

Jun 27th, 2021 - Alzheimer's disease (AD) is an age-related neurodegenerative disease characterized by progressive cognitive dysfunction and memory impairment. G protein-coupled receptor 40 (GPR40) is expressed in brain in addition to periphery and is associated with cognitive function such as space orientation, memory, and learning. However, the effects and mechanisms of GPR40 agonist in improving the AD progr...

Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes.
https://doi.org/10.1056/NEJMoa2107519
The New England Journal of Medicine; Frías JP, Davies MJ et. al.

Jun 26th, 2021 - Tirzepatide is a dual glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1 (GLP-1) receptor agonist that is under development for the treatment of type 2 diabetes. The efficacy and safety of once-weekly tirzepatide as compared with semaglutide, a selective GLP-1 receptor agonist, are unknown. In an open-label, 40-week, phase 3 trial, we randomly assigned 1879 patients, in a ...

Site selective C-H functionalization of Mitragyna alkaloids reveals a molecular switch ...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8219695
Nature Communications; Bhowmik S, Galeta J et. al.

Jun 24th, 2021 - Mitragynine (MG) is the most abundant alkaloid component of the psychoactive plant material "kratom", which according to numerous anecdotal reports shows efficacy in self-medication for pain syndromes, depression, anxiety, and substance use disorders. We have developed a synthetic method for selective functionalization of the unexplored C11 position of the MG scaffold (C6 position in indole num...

Progress in Pharmacotherapy for Obesity.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8277731
JAMA Yanovski SZ, Yanovski JA

Jun 24th, 2021 - Progress in Pharmacotherapy for Obesity.|2021|Yanovski SZ,Yanovski JA,|therapeutic use,therapeutic use,agonists,therapeutic use,drug therapy,

Semaglutide's Success Could Usher in a "New Dawn" for Obesity Treatment.
https://doi.org/10.1001/jama.2021.10307
JAMA Abbasi J

Jun 24th, 2021 - Semaglutide's Success Could Usher in a "New Dawn" for Obesity Treatment.|2021|Abbasi J,|therapeutic use,agonists,therapeutic use,drug therapy,

Pituitary apoplexy induced by gonadotropin-releasing hormone (GnRH) agonist administrat...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8236445
Journal of Cancer Research and Clinical Oncology; Raj R, Elshimy G et. al.

Jun 23rd, 2021 - We aimed to review of literature on the clinical presentation, management and outcomes of pituitary apoplexy following gonadotrophic release hormone (GnRH) agonist administration for the treatment of prostate cancer. We used PRISMA guidelines for our systematic review and included all English language original articles on pituitary apoplexy following GnRH agonist administration among prostate c...