- |||||||||| glibenclamide / Generic mfg.
Review, Journal: Targeting of neuroinflammation by glibenclamide in Covid-19: old weapon from arsenal. (Pubmed Central) - Mar 2, 2023 Glibenclamide reduces neuroinflammation and associated BBB injury by inhibiting the nod-like receptor pyrin 3 (NLRP3) inflammasome, oxidative stress, and microglial activation. Therefore, glibenclamide through inhibition of NLRP3 inflammasome, microglial activation, and oxidative stress may attenuate SARS-CoV-2-mediated neuroinflammation.
- |||||||||| Production of bioactive water-soluble indirubin derivative using novel plant P450 (Hall F-H (Indiana Convention Center)) - Feb 14, 2023 - Abstract #ACSSp2023ACS_SP_8840;
The compounds inhibit the growth of pathogenic strain Salmonella and cause cell cycle arrest of HeLa cells. In summary, we develop an efficient, sustainable, and green system for in vivo synthesis of pharmaceutically applicable indirubin derivatives.
- |||||||||| Sirturo (bedaquiline) / J&J, Pharmstandard
Synthesis of selective inhibitors of Pseudomonas aeruginosa ATP synthase (Room 109 (Indiana Convention Center)) - Feb 14, 2023 - Abstract #ACSSp2023ACS_SP_578; Since the development of the anti-tubercular drug Bedaquiline, ATP synthase has become a target of interest for antibiotic development...The strongest inhibitor showed an IC50 of 10 ?g/mL and decreased activity of PA ATP synthase to 24% relative to the control. Current work is focusing on improve whole cell antibiotic activity of these analogs by improving accumulation.
- |||||||||| chloroquine phosphate / Generic mfg.
Journal: Chloroquine-Based Mitochondrial ATP Inhibitors. (Pubmed Central) - Feb 12, 2023 The most potent mito. ATP inhibitor was found to be N-(4-((2,4-Dinitrophenyl)amino)pentyl)-N-ethylacetamide (17).
- |||||||||| Journal: A phytotherapic blend immunity-6™ inhibits myeloid leukemic cells 2 activation involving purinergic signaling. (Pubmed Central) - Jan 20, 2023
Beyond to inhibit the release of pro-inflammatory cytokines, both doses of Immunity-6™ induced the release of anti-inflammatory cytokine IL-10 (p < 0.001), while only the higher dose (10 ug/mL) of Immunity-6™ induced the release of anti-inflammatory IL-1ra (p < 0.05) and klotho (p < 0.001). Thus, Immunity-6™ may be a promising adjuvant in the treatment of leukemia and further clinical trials are guaranteed.
- |||||||||| paclitaxel / Generic mfg.
Journal: NIR Activated Multimodal Therapeutics Based on Metal-Phenolic Networks-Functionalized Nanoplatform for Combating against Multidrug Resistance and Metastasis. (Pubmed Central) - Jan 19, 2023 t-P@TFP NPs trigger the phase transition of perfluoropentane (PFP) to release tannic acid (TA)/ferric ion (Fe )-coated paclitaxel (PTX) and cause hyperthermia in the tumor region to efficiently kill cancer cells...Furthermore, hyperthermia-induced immunogenic cell death (ICD) transforms "cold" tumors into "hot" tumors with the assistance of PD-1/PD-L1 blockade to evoke antitumor immunogenicity. This work carefully reveals the mechanisms underlying the abilities of these multifunctional NPs, providing new insights into combating the proliferation and metastasis of multidrug-resistant tumors.
- |||||||||| Journal: Overcoming multidrug-resistant lung cancer by mitochondrial-associated ATP inhibition using nanodrugs. (Pubmed Central) - Jan 13, 2023
This study identified that H69AR lung cancer cells, an adriamycin (DOX) drug-resistant tumor cell line, did not activate drug resistance function on designed nano-anticancer drugs with a specific nano size. In summary, this study identified that the specific size of the nanodrug in combination with DOX overcame multidrug-resistant tumors by inducing selective accumulation in tumor cells and inhibiting ATP by mitochondrial damage.
- |||||||||| Nexletol (bempedoic acid) / Esperion Therap, Otsuka, Daiichi Sankyo
Preclinical, Journal: Bempedoic Acid Restores Liver HS Production in a Female Sprague-Dawley Rat Dietary Model of Non-Alcoholic Fatty Liver. (Pubmed Central) - Jan 9, 2023 Our data show that the HFHFr diet reduces the total and enzymatic production of liver HS, mainly by decreasing the expression of CBS and CSE. Furthermore, BemA treatment restored HS production, increasing the expression of CBS and CSE, providing evidence for the involvement of FXR transcriptional activity and the mTORC1 (mammalian target of rapamycin1)/S6K1 (ribosomal protein S6 kinase beta-1)/PGC1α (peroxisome proliferator receptor gamma coactivator1α) pathway.
- |||||||||| paclitaxel / Generic mfg.
Journal, PD(L)-1 Biomarker, IO biomarker: Nanoenabled Tumor Energy Metabolism Disorder via Sonodynamic Therapy for Multidrug Resistance Reversal and Metastasis Inhibition. (Pubmed Central) - Dec 29, 2022 A US-controlled "Nanoenabled Energy Metabolism Jammer" (TL@HPN) is designed using perfluoropentane (PFP) adsorbing oxygen in the core, and a targeting peptide (CGNKRTR) is attached to the liposome as the delivery carrier shell to incorporate hematoporphyrin monomethyl ether (HMME) and paclitaxel (PTX)...Persistently elevated oxidative stress levels inhibited ATP production and downregulated P-gp expression by disrupting the redox balance and electron transfer of the respiratory chain. We varied the effect of TL@HPN combined with PD-1/PD-L1 to activate autoimmunity and inhibit tumor metastasis, providing a practical strategy for expanding the use of SDT-mediated tumor energy metabolism.
- |||||||||| Journal: Is the vesicular nucleotide transporter a molecular target of eicosapentaenoic acid? (Pubmed Central) - Dec 27, 2022
These results indicate that EPA at sub-μM acts as a proton conductor and increases proton permeability across the membrane, regardless of the presence or absence of VNUT, thereby inhibiting non-specifically the vesicular storage of neurotransmitters. Thus, EPA may affect a broader range of chemical transmission than proposed.
- |||||||||| Journal: Substrate stiffness enhances human regulatory T cell induction and metabolism. (Pubmed Central) - Dec 2, 2022
Inhibition of ATP synthase significantly reduced the rate of Treg induction and abrogated the difference among gels while activation of AMPK (AMP-activated protein kinase) increased Treg induction on the softer sample but not on the harder sample. Treg induction is thus mechanosensitive and OXPHOS-dependent, providing new strategies for improving the production of these cells for cellular immunotherapy.
- |||||||||| Journal: TIMM44 is a potential therapeutic target of human glioma. (Pubmed Central) - Nov 29, 2022
Moreover, the intracranial growth of TIMM44 KO glioma cells in the mouse brain was largely inhibited. Together, overexpressed TIMM44 could be a novel and promising therapeutic target of human glioma.
- |||||||||| Review, Journal: Propofol-Related Infusion Syndrome: A Clinical Review. (Pubmed Central) - Nov 22, 2022
The other essentials of management of various manifestations of PRIS will be discussed in this article, along with a detailed explanation of the condition, its risk factors, diagnosis, pathophysiology, and presenting features. This article aims to make clinicians more aware of the occurrence of this syndrome so that better ways to manage and treat this condition can be formulated in the future.
- |||||||||| Biomarker, Journal: Peripheral blood mononuclear cell mitochondrial copy number and adenosine triphosphate inhibition test in NAFLD. (Pubmed Central) - Nov 16, 2022
The mtDNA copy number and mitochondrial ATP inhibition substrate test demonstrated negative correlations with the degree of hepatic steatosis, whereas the ATP concentration showed a positive correlation with the mtDNA copy number. The mitochondrial copy number of peripheral blood mononuclear cells and mitochondrial ATP inhibition substrate can be used as biomarkers for assessing the mitochondrial dysfunction in patients with NAFLD.
- |||||||||| doxorubicin hydrochloride / Generic mfg., epirubicin / Generic mfg.
Journal: 2,4-Dinitrophenol as an Uncoupler Augments the Anthracyclines Toxicity against Prostate Cancer Cells. (Pubmed Central) - Nov 16, 2022 The synergistic activity may consist of an inhibition of ATP synthesis and the simultaneous production of toxic amounts of ROS, destroying the mitochondria. Additionally, the sensitivity of the LNCaP cell line to the anthracyclines is relatively higher compared to the other two (PC-3, DU-145).
- |||||||||| Germanin (suramin) / Optimum Therap
Preclinical, Journal: Suramin prevents the development of diabetic kidney disease by inhibiting NLRP3 inflammasome activation in KK-Ay mice. (Pubmed Central) - Oct 30, 2022 Taken together, our results constitute a first step in paving the way for structure-based development of new allosteric drugs targeting FF-ATP synthase sites of exogenous inhibitors. These results suggest that the NLRP3 inflammasome is activated in a diabetic kidney and that inhibition of the NLRP3 inflammasome with suramin protects against the progression of early stage DKD.
- |||||||||| Review, Journal: Tyrosine Kinase Inhibitors for Pediatric Leukemia: History and Current Status. (Pubmed Central) - Oct 25, 2022
In conclusion, we focus on chronic myeloid leukemia and acute lymphoblastic leukemia as the examples of pediatric blood cancer that significantly benefit from TKIs-based target therapy. Further development of TKIs will allow us to better manage pediatric leukemia.
|