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- || hydroxocobalamin (vit B12) / Generic mfg.
Review, Journal: Vasoplegic Syndrome and Anaesthesia: A Narrative Review. (Pubmed Central) - Aug 17, 2023
Available treatments involve volume and inotropes administration, vasopressin, methylene blue, hydroxocobalamin, Ca++, vitamin C, and thiamine, and should also restore vascular tone and improve vasoplegia...It is challenging for an anaesthesiologist to consider this syndrome's diagnosis and manage its treatment. Our review aims to review the diagnosis, predisposing factors, pathophysiology, treatment, and anaesthesia approach of VS during anaesthesia and to suggest a treatment algorithm.
- | Preclinical, Journal: Tetracyclic 1,4-Naphthoquinone Thioglucoside Conjugate U-556 Blocks the Purinergic P2X7 Receptor in Macrophages and Exhibits Anti-Inflammatory Activity In Vivo. (Pubmed Central) - Aug 16, 2023
The study of biological activity in in vivo experiments shows that tetracylic conjugate significantly reduces inflammation provoked by carrageenan. The data obtained points out that the observed physiological effects of U-556 may be due to its ability to block the functioning of the P2X7R.
- | Miostat (carbachol) / Novartis
Journal: Sesquiterpene lactones improve secretory diarrhea symptoms by inhibiting intestinal Ca-activated Cl channel activities directly and indirectly. (Pubmed Central) - Aug 14, 2023
AL and iAL also inhibited the CaCC-mediated short-circuit currents induced by carbachol in the mouse colons...Preliminary mechanism studies showed that AL and iAL inhibited CaCCs at least partially by inhibiting Ca release and basolateral membrane K channels activity. These findings suggest a new pharmacological activity of sesquiterpene lactone compounds that might lead to the development of treatments for rotaviral secretory diarrhea.
- | Journal, IO biomarker: Plasma Membrane Channel TRPM4 Mediates Immunogenic Therapy-Induced Necrosis. (Pubmed Central) - Jul 31, 2023
Thus, TRPM4 plays a pivotal role in sustaining lethal a-UPR hyperactivation that mediates the anticancer activity of diverse necrosis-inducing therapies. A genome-wide CRISPR screen reveals a pivotal role for TRPM4 in cell death and immune activation following treatment with diverse necrosis-inducing anticancer therapies, which could facilitate development of necrosis-based cancer immunotherapies.
- | Journal: Oxidative stress and mitochondrial damage induced by a novel pesticide fluopimomide in Caenorhabditis elegans. (Pubmed Central) - Jul 22, 2023
ROS levels in the mev-1 and isp-1 mutants after fluopimomide treatments did not change significantly compared with the untreated mutants, suggesting that mev-1 and isp-1 may play critical roles in the toxicity induced by fluopimomide. Overall, the results demonstrate that oxidative stress and mitochondrial damage may be involved in toxicity of fluopimomide in C. elegans.
- | Journal: F-ATP synthase inhibitory factor 1 regulates metabolic reprogramming involving its interaction with c-Myc and PGC1?. (Pubmed Central) - Jul 20, 2023
This study suggested that the interactions of IF1 with transcription factors c-Myc and PGC1? might be involved in IF1-regulatory metabolic reprogramming and cell fate.
- | Vampex (carbenoxolone gel) / York Pharma
Preclinical, Journal: Ca Dynamics of Gap Junction Coupled and Uncoupled Deiters' Cells in the Organ of Corti in Hearing BALB/c Mice. (Pubmed Central) - Jul 18, 2023
We have compared the ATP-evoked Ca transients and the effect of two different gap junction (GJ) blockers (octanol and carbenoxolone, CBX) on the Ca transients in DCs located in the apical and middle turns of the hemicochlea preparation of BALB/c mice (P14-19)...The cochlear turn-dependent effect of CBX might be the result of the differing connexin isoform composition of GJs along the tonotopic axis. The contribution of IP-mediated Ca signalling inhibition by CBX cannot be excluded.
- | Preclinical, Journal: Involvement of P2Y, P2Y, A and A Receptors in the Purinergic Inhibition of NMDA-Evoked Noradrenaline Release in the Rat Brain Cortex. (Pubmed Central) - Jul 18, 2023
Characterization of the effects mediated by these compounds indicated the involvement of P2Y, P2Y, A and A receptors. It is concluded that, in the rat brain cortex, NMDA-evoked noradrenaline release is modulated by several purinergic receptors that may represent a relevant mechanism to regulate the permissive effect of noradrenaline on NMDA-induced neuroplasticity.
- | progesterone / Generic mfg.
Journal: ATP increases head volume in capacitated human sperm via a purinergic channel. (Pubmed Central) - Jul 18, 2023
We examined the involvement of purinergic receptors (PRs) P2X2R and P2X4R in ATPVI using their co-agonists progesterone and Ivermectin (Iver), and Cu, which co-activates P2X2Rs and inhibits P2X4Rs...ATP increased the concentration of intracellular Ca ([Ca]) in >45% of individual sperm, most of which underwent AR monitored using FM4-64. Our findings suggest that human sperm P2X4R activation by ATP increases [Ca] mainly due to Ca influx which leads to a sperm head volume increase, likely involving acrosomal swelling, and resulting in AR.
- | Preclinical, Journal: Sodium aescinate improve behavioral performance by inhibiting dorsal raphe nucleus NLRP3 inflammasome in Post-traumatic stress disorder Rat Model. (Pubmed Central) - Jul 18, 2023
In addition, NLRP3 inflammasome activation in DRN of PTSD rats impaired mitochondria function by inhibiting ATP synthesis and increasing ROS production, whereas SA can effectively reverse the pathological progression of mitochondria. We recommend SA as a new candidate for the pharmacological treatment of PTSD.
- | Journal: Exploitation of ATP-sensitive potassium ion (K) channels by HPV promotes cervical cancer cell proliferation by contributing to MAPK/AP-1 signalling. (Pubmed Central) - Jul 14, 2023
Mechanistically, we propose that the pro-proliferative effect of K channels is mediated via the activation of a MAPK/AP-1 signalling axis. A complete characterisation of the role of K channels in HPV-associated cancer is now warranted in order to determine whether the licensed and clinically available inhibitors of these channels could constitute a potential novel therapy in the treatment of HPV-driven cervical cancer.
- | Journal: RLI2 regulates Arabidopsis female gametophyte and embryo development by facilitating the assembly of the translational machinery. (Pubmed Central) - Jul 8, 2023
In particular, RLI2 knockdown mutant exhibits decreased expression of genes involved in auxin signaling and female gametophyte and embryo development. Therefore, our results reveal that RLI2 facilitates assembly of the translational machinery and indirectly modulates auxin signaling to regulate plant growth and development.
- Nexletol (bempedoic acid) / Esperion Therap, Otsuka, Daiichi Sankyo
Repurposing bempedoic acid as a therapeutic option in GSD type 1: from biochemical principles to first clinical data (Oren 3 (ICC),Oren 4 (ICC)) - Jul 6, 2023 - Abstract #SSIEM2023SSIEM_277;
In a pilot study, BA had a positive effect on metabolic control in patients with GSD1 without side effects. Therefore, repurposing of BA may be a novel treatment option in patients suffering from GSD1.
- | Preclinical, Journal, Metabolomic study: Study on the Intervention Mechanism of Cryptotanshinone on Human A2780 Ovarian Cancer Cell Line Using GC-MS-Based Cellular Metabolomics. (Pubmed Central) - Jun 28, 2023
Changes in the ATP and amino acid contents were verified with in vitro and in vivo experiments. Our results indicate that CT may exert an anti-ovarian cancer effect by inhibiting ATP production, promoting the protein catabolic process, and inhibiting protein synthesis, which may lead to cell cycle arrest and apoptosis.
- | Journal: Inhibiting ATP/P2X7R signaling protects intestinal barrier in DSS-induced colitis and Crohn's disease through inactivating NF-?B pathway in macrophages. (Pubmed Central) - Jun 20, 2023
Our results indicate that CT may exert an anti-ovarian cancer effect by inhibiting ATP production, promoting the protein catabolic process, and inhibiting protein synthesis, which may lead to cell cycle arrest and apoptosis. No abstract available
- | Journal: Atomic insights of an up and down conformation of the Acinetobacter baumannii F -ATPase subunit ? and deciphering the residues critical for ATP hydrolysis inhibition and ATP synthesis. (Pubmed Central) - Jun 19, 2023
does not bind MgATP, which is described to regulate the up and down movements in other bacterial counterparts. The data are compared to regulatory elements of F -ATPases in bacteria, chloroplasts, and mitochondria to prevent wasting of ATP.
- | Journal: Phosphate toxicity and SERCA2a dysfunction in sudden cardiac arrest. (Pubmed Central) - Jun 15, 2023
However, current technology lacks the ability to directly measure this pathophysiological mechanism in active myocardium, and further research is needed to confirm phosphate toxicity as a risk factor in individuals with sudden cardiac arrest. Moreover, phosphate toxicity may be reduced through modification of dietary phosphate intake, with potential for employing low-phosphate dietary interventions to reduce the risk of sudden cardiac arrest.
- | deoxyglucose / Generic mfg.
Journal: DNA Aptamer Beacon Probe (ABP) for Monitoring of Adenosine Triphosphate Level in SW480 Cancer Cells Treated with Glycolysis Inhibitor 2-Deoxyglucose. (Pubmed Central) - Jun 14, 2023
We have found that the inhibition of glycolysis in SW480 cancer cells by 2-deoxyglucose resulted in lowering of ATP production by 31.7%. Therefore, monitoring and modulation of ATP concentration may aid in future cancer treatment.
- | Journal: Citric Acid Confers Broad Antibiotic Tolerance through Alteration of Bacterial Metabolism and Oxidative Stress. (Pubmed Central) - May 31, 2023
Surprisingly, the addition of succinic acid and xanthine could reverse the antibiotic tolerance induced by citric acid in vitro and in animal infection models. In conclusion, these findings provide new insights into the potential risks of citric acid usage and the relationship between antibiotic tolerance and bacterial metabolism.
- | Journal: ATP Consumption Is Coupled with Endocytosis in Exudated Neutrophils. (Pubmed Central) - May 31, 2023
Furthermore, data from the NLR family pyrin domain containing three knockout mice suggest that inflammasome activation is not involved in neutrophil endocytosis or concomitant ATP consumption. To summarize, these molecular events occur via endocytosis, which is closely related to ATP-centered energy metabolism.
- | Journal: Forrestiacids E-K: Further [4 + 2]-Type Triterpene-Diterpene Hybrids as Potential ACL Inhibitors from the Vulnerable Conifer Pseudotsuga forrestii. (Pubmed Central) - May 29, 2023
Docking studies corroborated the findings by highlighting the interactions between the bioactive compounds and the ACL enzyme (binding affinities: -9.9 to -10.7 kcal/mol). The above findings reveal the important role of protecting plant species diversity in support of chemical diversity and potential sources of new therapeutics.
- | Journal: Molecular Docking and Molecular Dynamics Simulation of New Potential JAK3 Inhibitors. (Pubmed Central) - May 26, 2023
The above findings reveal the important role of protecting plant species diversity in support of chemical diversity and potential sources of new therapeutics. These findings reveal the mechanism of 1-phenylimidazolidine-2-one derivatives on JAK3 protein and provide a relatively solid theoretical basis for the development and structural optimization of JAK3 protein inhibitors.
- | Germanin (suramin) / Optimum Therap
Journal: Extracellular histone proteins activate P2XR7 channel current. (Pubmed Central) - May 22, 2023
As with ATP-evoked P2XR7 currents, histone-evoked currents were inhibited by non-selective P2XR7 antagonists (Suramin, PPADS, and TNP-ATP)...These data demonstrate that P2XR7 is necessary and sufficient for histone-evoked inward cation currents in a heterologous expression system. These results provide insight into a new allosteric mechanism of P2XR7 activation by histone proteins.
- | Journal: Mechanism of ADP-Inhibited ATP Hydrolysis in Single Proton-Pumping FF-ATP Synthase Trapped in Solution. (Pubmed Central) - May 17, 2023
By counting active versus inhibited enzymes, we revealed that ADP inhibition did not decrease the catalytic turnover of all FF-ATP synthases equally. Instead, increasing ADP in the ADP/ATP mixture reduced the number of remaining active enzymes that operated at similar catalytic rates for varying substrate/product ratios.
- | epicatechin (EB 002) / Epirium Bio
Journal: Inhibition of ATP synthase reverse activity restores energy homeostasis in mitochondrial pathologies. (Pubmed Central) - May 16, 2023
Inhibition of CV-ATP hydrolysis in a mouse model of Duchenne Muscular Dystrophy is sufficient to improve muscle force without any increase in mitochondrial content. We conclude that the impact of compromised mitochondrial respiration can be lessened using hydrolysis-selective inhibitors of CV.
- || Review, Journal: Role of the interaction between troponin T and AMP deaminase by zinc bridge in modulating muscle contraction and ammonia production. (Pubmed Central) - May 15, 2023
When a 95-residue N-terminal fragment is removed from AMPD by trypsin, simulating in vitro the calpain action, rabbit fast TnT or its phosphorylated 50-residue N-terminal peptide binds AMPD restoring the inhibition by ATP. Taking in consideration that the N-terminus of TnT expressed in human as well as rabbit white muscle contains a zinc-binding motif, we suggest that TnT might mimic the regulatory action of the inhibitory N-terminal domain of AMPD due to the presence of a zinc ion connecting the N-terminal and C-terminal regions of the enzyme, indicating that the two proteins might physiologically associate to modulate muscle contraction and ammonia production in fast-twitching muscle under strenuous conditions.
- Discovery and in vivo evaluation of novel inhibitors of the hydrolytic activity of mitochondrial F1Fo ATP synthase to alleviate myocardial ischemia reperfusion injury (Station 8) - May 13, 2023 - Abstract #ESC2023ESC_4354;
We discovered a novel pyrazolopyridine derivative that acts as an inhibitor of ATP hydrolysis and reduces myocardial IS in vivo. Its cardioprotective mechanism involves the activation of PKA signaling and alleviation of apoptosis.
- | Journal: Bacterial Persister Cells: Mechanisms of Formation, Control, and Eradication. (Pubmed Central) - May 12, 2023
However, eradicating persistent cells is challenging as the specific molecular mechanisms that initiate their formation remain fuzzy and unknown. Here we reviewed and summarized the current understanding of how bacterial persister cells are formed, controlled, and destroyed.
- | Journal: Resveratrol Attenuates the Mitochondrial RNA-Mediated Cellular Response to Immunogenic Stress. (Pubmed Central) - May 2, 2023
Notably, RES treatment fails to counter the effect of an endoplasmic reticulum stressor that does not affect the expression of mitochondrial RNAs. Overall, our study demonstrates the potential usage of RES to alleviate the mt-dsRNA-mediated immunogenic stress response.
- | Nexletol (bempedoic acid) / Esperion Therap, Otsuka, Daiichi Sankyo
Journal: The Disposition and Metabolism of Bempedoic Acid, A Potent Inhibitor of ATP Citrate Lyase, In Healthy Human Subjects. (Pubmed Central) - May 1, 2023
Significance Statement This study characterizes the disposition and metabolism of bempedoic acid, an inhibitor of ATP citrate lyase for hypercholesterolemia. This work provides further understanding of bempedoic acid clinical pharmacokinetics and clearance pathways in adult subjects.
- | Journal: Different cold tolerances among three strains of large yellow croaker: related to antioxidant defense and energy metabolism. (Pubmed Central) - Apr 28, 2023
Nrf2 and AMPK gene expressions were correlated with antioxidant and energy metabolism mRNA levels, respectively, suggesting Nrf2 and AMPK might participate in the modulation of target genes during the cold-stress adaptation. In conclusion, low temperature tolerance of fish depended on the antioxidant defense and energy metabolism efficiency, which contributes to understanding the underlying mechanisms of cold adaptation in large yellow croaker.
- || Sirturo (bedaquiline) / J&J, Pharmstandard, piceatannol / New York Medical College, Kyushu University
Review, Journal: Inhibitors of ATP Synthase as New Antibacterial Candidates. (Pubmed Central) - Apr 28, 2023
However, each of these inhibitors target ATP synthase differently, and their co-administration with antibiotics increases the susceptibility of pathogenic bacteria. After a brief description of the structure and function of ATP synthase, we aim in this review to highlight therapeutic applications of the major bacterial ATP synthase inhibitors, including animal's venoms, and to emphasize their importance in decreasing the activity of this enzyme and subsequently eradicating resistant bacteria as ATP synthase is their source of energy.
- | Journal: Membrane Potential-requiring Succinate Dehydrogenase Constitutes the Key to Propionate Oxidation and Is Unique to Syntrophic Propionate-oxidizing Bacteria. (Pubmed Central) - Apr 25, 2023
These chemicals inhibited hydrogen production, indicating that membrane-bound SDH requires a membrane potential for succinate oxidation, and this membrane potential is maintained by ATP synthase. In addition, the phylogenetic distribution of the flavin adenine dinucleotide-binding subunit and conserved amino acid sequences of the cytochrome b subunit of SDHs in propionate-oxidizing bacteria suggests that membrane-bound SDHs possess specific conserved amino acid residues that are strongly associated with efficient succinate oxidation in syntrophic propionate-oxidizing bacteria.
- | Journal: Platelet-inhibitory phenolic constituents from the fruits of Daemonorops draco. (Pubmed Central) - Apr 14, 2023
All the isolates were evaluated for their inhibitory activity against ATP release in thrombin-activated platelets. Compounds 2b, 3a, and 6 could significantly inhibit ATP release in thrombin-activated platelets.
- | MG132 / Jilin University, Dorothy M. Davis Heart and Lung Research Institute
Journal: BC-1215 inhibits ATP-induced IL-1? secretion via the FBXL2-mediated ubiquitination and degradation of not only NLRP3, but also pro-IL-1? in LPS-primed THP-1 (Pubmed Central) - Apr 12, 2023
secretion via the FBXL2-mediated ubiquitination and degradation of pro-IL-1? as well as NLRP3 in LPS-primed THP-1
- | Journal: Molecular mechanism on forcible ejection of ATPase inhibitory factor 1 from mitochondrial ATP synthase. (Pubmed Central) - Apr 5, 2023
Investigation of mutant IF with N-terminal truncations shows that the interaction with the ? subunit at the N-terminal regions is crucial for rotational-direction-dependent ejection, and the middle long helix is responsible for the inhibition of F.
- Miostat (carbachol) / Novartis
Long-term administration of a PDE-5 inhibitor prevents the development of bladder epithelial ATP increase and decreased detrusor contractility in type 2 diabetic rats (S401A) - Mar 30, 2023 - Abstract #AUA2023AUA_3044;
As a result, the bladder epithelial ATP release was enhanced, possibly via VNUT upregulation.A long-term administration of a PDE-5 inhibitor could prevent the development of storage and voiding dysfunction associated with T2DM. This study is the first to suggest that epithelium-derived ATP may be involved in urine storage dysfunction in T2DM and tadalafil inhibits ATP release and improves bladder contraction.
- | Journal: Assessing the Benefits and Costs of the Hydrogen Cyanide Antiherbivore Defense in Trifolium repens. (Pubmed Central) - Mar 30, 2023
Our study provides evidence that the benefits of HCN defense against herbivores are temperature dependent, and freezing may inhibit ATP production in cyanogenic plants, but the physiological performance of all plants recovered quickly following short-term freezing. These results contribute to understanding how varying environments alter the benefits and costs of defense in a model system for the study of plant chemical defenses against herbivores.
- | Nexletol (bempedoic acid) / Esperion Therap, Otsuka, Daiichi Sankyo
Journal: Effects of bempedoic acid on CRP, IL-6, fibrinogen and lipoprotein(a) in patients with residual inflammatory risk: A secondary analysis of the CLEAR harmony trial. (Pubmed Central) - Mar 28, 2023
P3
Thus, the pattern of lipid lowering and inflammation inhibition with BA is almost identical to what is observed with statin therapy suggesting that BA could be a useful treatment option to address both residual cholesterol risk and residual inflammatory risk. TRIAL REGISTRATION: ClinicalTrials.gov Identifier: NCT02666664; https://clinicaltrials.gov/ct2/show/NCT02666664.
- | Journal: Effects of PFOS, F53-B and F53-B on locomotor behaviour, the dopamine system and mitochondrial function in developing zebrafish (Danio rerio). (Pubmed Central) - Mar 25, 2023
Together, PFOS and emerging contaminants F53-B and OBS inhibit locomotion at similar concentrations, a finding correlated with decreased dopaminergic neuron numbers in the subpallium and decreased expression of pink1. These findings are relevant to wildlife and human health, as they suggest that PFOS as well as replacement compounds affect locomotion likely in part by negatively impacting the dopamine system.
- | Journal: Ainsliadimer A induces ROS-mediated apoptosis in colorectal cancer cells via directly targeting peroxiredoxin 1 and 2. (Pubmed Central) - Mar 24, 2023
Additionally, it inhibits tumor growth in mice and the growth of tumor organoid models. Therefore, AIN can be one of the natural compounds targeting PRDX1 and PRDX2 in the treatment of colorectal cancer.
- | Journal: Armeniaspirol analogues disrupt the electrical potential (??) of the proton motive force. (Pubmed Central) - Mar 20, 2023
Thus we propose that the armeniaspirols utilize a dual mechanism of action where they disrupt PMF and inhibit the ATP-dependent proteases ClpXP and ClpYQ. This type of dual mechanism has been observed in other natural product-based antibiotics, most notably chelocardin.
- | Journal: NRF-2? and mitophagy underlie enhanced mitochondrial functions and biogenesis induced by T-2 toxin in GH3 cells. (Pubmed Central) - Mar 14, 2023
Altogether, these results suggest that NRF-2? plays a critical role in promoting mitochondrial function and biogenesis through regulation of mitochondrial genes, and, interestingly, mitophagy caused by T-2 toxin positively affected mitochondrial function and protected cell survival against T-2 toxin.
- TOS-358 / Totus Medicines
TOS-358, a first-in-class covalent PI3K? inhibitor, demonstrates superior efficacy and does not induce significant hyperglycemia at efficacious doses in multiple animal models (Section 15; Poster Board #24) - Mar 14, 2023 - Abstract #AACR2023AACR_7347;
This data reveals that highly specific and potent covalent inhibition of PI3K? leads to dramatically superior efficacy and an improved safety profile.
- | Journal: The FF-ATP synthase ? subunit of Candida albicans induces inflammatory responses by controlling amino acid catabolism. (Pubmed Central) - Mar 14, 2023
subunit induces host inflammatory responses by controlling its own amino acid catabolism and it is significant to find drugs that inhibit FF-ATP synthase ? subunit activity to control the induction of host inflammatory responses.
- | Journal, Gram negative: Elucidating the Mechanism of Action of the Gram-Negative-Pathogen-Selective Cyclic Antimicrobial Lipopeptide Brevicidine. (Pubmed Central) - Mar 14, 2023
Finally, brevicidine showed a good therapeutic effect in a mouse peritonitis-sepsis model. Our findings pave the way for further research on the clinical applications of brevicidine to combat prevalent infections caused by AMR Gram-negative pathogens worldwide.
- | Journal: Effect of extreme pH conditions on methanogenesis: Methanogen metabolism and community structure. (Pubmed Central) - Mar 11, 2023
However, the EPS carbohydrate content at pH?4.0 and 10.0 both decreased. This study is expected to promote the understanding of the pH control-induced methanogenesis inhibition in the CEF system.
- || Nexletol (bempedoic acid) / Esperion Therap, Otsuka, Daiichi Sankyo
Review, Journal: Bempedoic acid in the management of lipid disorders and cardiovascular risk. 2023 position paper of the international lipid expert panel (ILEP). (Pubmed Central) - Mar 9, 2023
Practical evidence-based guidance is provided relating to the use of bempedoic acid in atherosclerotic CVD, familial hypercholesterolaemia, and statin intolerance. Although there are currently no data available for the role of bempedoic acid in the primary prevention of CVD, its favourable effects on plasma glucose and inflammatory markers makes this drug a rational choice in the patient-centred care of specific groups of primary prevention.
- || Preclinical, Review, Journal: Group II metabotropic glutamate receptor activation suppresses ATP currents in rat dorsal root ganglion neurons. (Pubmed Central) - Mar 2, 2023
mGluRs. These results indicated that peripheral group II mGluR activation inhibited the functional activity of P2X3 receptors via a G protein and cAMP/PKA signaling pathway in rat DRG neurons, which revealed a novel mechanism underlying analgesic effects of peripheral group II mGluRs.