ATP inhib 
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  • ||||||||||  tamoxifen / Generic mfg.
    Journal:  Have molecular hybrids delivered effective anti-cancer treatments and what should future drug discovery focus on? (Pubmed Central) -  Oct 16, 2021   
    The success of molecular hybridization in cancer chemotherapy is quite evident by the number of molecules entering into clinical trials and/or have entered the drug market over the past decade. Indeed, the recent advancements and co-ordinations in the interface between chemistry, biology and pharmacology will help further the advancement of hybrid chemotherapeutics in the future.
  • ||||||||||  Tabrecta (capmatinib) / Incyte, Novartis
    Journal:  HGF/MET in osteogenic differentiation of primary human palatal periosteum-derived mesenchymal stem cells. (Pubmed Central) -  Oct 7, 2021   
    We conclude that parasympathetic tone may reduce the arrhythmogenic substrate exerting a complex antiarrhythmic mechanism during hypoxic conditions. HGF/MET present in human PP and HGF is upregulated in vitro during osteogenesis; however the targeted pathways controlled by MET may not involve osteoblast maturation.
  • ||||||||||  Nexletol (bempedoic acid) / Esperion Therap, Otsuka
    Review, Journal:  Bempedoic Acid: A New Non-statin Drug for the Treatment of Dyslipidemia. (Pubmed Central) -  Oct 3, 2021   
    Decreased hemoglobin levels and rare tendon ruptures have also been observed. Due to its efficacy and good safety profile, bempedoic acid might serve as a potential therapeutic alternative for the management of dyslipidemia.
  • ||||||||||  Journal:  3-Bromopyruvate: A new strategy for inhibition of glycolytic enzymes in Leishmania amazonensis. (Pubmed Central) -  Oct 1, 2021   
    Furthermore, the ability to infect macrophages was reduced by approximately 50% when promastigotes were treated with 3-BrPA. Taken together, these studies corroborate with previous reports which suggest 3-BrPA as a potential drug against pathogenic microorganisms that are reliant on glucose catabolism for ATP supply.
  • ||||||||||  Nexletol (bempedoic acid) / Esperion Therap, Otsuka
    [VIRTUAL] Factors Associated with Enhanced Low-Density Lipoprotein Cholesterol Lowering with Bempedoic Acid Among Patients Enrolled in Phase 3 Studies (OnDemand) -  Sep 24, 2021 - Abstract #AHA2021AHA_6539;    
    Further, being female, a history of diabetes, baseline ezetimibe use, and a higher baseline hsCRP level were also associated with at least a 30% reduction in LDL-C levels (P < .01 for each). These findings suggest that 1) a significant proportion of patients initiating BA treatment may achieve LDL-C lowering comparable to moderate- or high-intensity statin therapy, especially among patients who cannot tolerate a statin, and 2) patients with hypercholesterolemia who are at higher risk for a cardiovascular event, including women and patients with a history of statin intolerance, diabetes, or higher baseline hsCRP levels, may also achieve enhanced LDL-C lowering with bempedoic acid.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg.
    Journal:  FOXO3a-dependent Parkin regulates the development of gastric cancer by targeting ATP-binding cassette transporter E1. (Pubmed Central) -  Sep 22, 2021   
    Additionally, doxorubicin (DOX) upregulated the expression of Parkin and promoted its anticancer effect...In addition, Parkin inhibited cell proliferation, migration, and promoted apoptosis by inhibiting ATP-binding box protein E1 (ABCE1) expression. In summary, our results demonstrated a new regulatory axis of FOXO3a-Parkin-ABCE1 that modulated GC cell proliferation, migration, and apoptosis, and it can serve as a potential therapeutic target in GC.
  • ||||||||||  Journal:  Role of Primary Afferents in Arthritis Induced Spinal Microglial Reactivity. (Pubmed Central) -  Sep 22, 2021   
    Our results demonstrate that early peripheral joint injury activates joint nociceptors, which triggers a central spinal microglial response. Elevation of ATP in the CSF, and spinal expression of VNUT suggest ATP signaling may modulate communication between sensory neurons and spinal microglia at 2 weeks of joint degeneration.
  • ||||||||||  Journal:  Structure of an AMPK complex in an inactive, ATP-bound state. (Pubmed Central) -  Sep 12, 2021   
    A 180° rotation and 100-angstrom displacement of the kinase domain fully exposes the AL. On the basis of the structure and supporting biophysical data, we propose a multistep mechanism explaining how adenine nucleotides and pharmacological agonists modulate AMPK activity by altering AL phosphorylation and accessibility.
  • ||||||||||  cisplatin / Generic mfg.
    Journal:  Blocking P2X7-Mediated Macrophage Polarization Overcomes Treatment Resistance in Lung Cancer. (Pubmed Central) -  Sep 10, 2021   
    Furthermore, resistance to immunotherapy (anti-PD-1 antibody) and chemotherapy (cisplatin) were both overcome by co-administration of the P2X7 inhibitors O-ATP, A-438079 hydrochloride and A-740003. Therefore, our data revealed a vital role of P2X7 in tumor formation through regulating TAM polarization, suggesting the therapeutic potential of P2X7 blockade in lung cancer patients.
  • ||||||||||  Journal:  Cells Lacking PA200 Adapt to Mitochondrial Dysfunction by Enhancing Glycolysis via Distinct Opa1 Processing. (Pubmed Central) -  Sep 4, 2021   
    The present study also demonstrates that the proteolytic cleavage of Opa1 is affected, and that the level of OMA1 is significantly reduced in shPA200 cells upon oligomycin-induced mitochondrial insult. Together, these findings suggest a role for PA200 in the regulation of metabolic changes in response to selective inhibition of ATP synthase in an in vitro cellular model.
  • ||||||||||  metformin / Generic mfg.
    Journal:  Metabolic Strategies for Inhibiting Cancer Development. (Pubmed Central) -  Aug 20, 2021   
    To create future personalized therapies for targeting each cancer tumor, novel techniques must be developed, such as new tracers for positron emission tomography/computed tomography scan and immunohistochemical markers to characterize the metabolic phenotype of cancer cells and their microenvironment. Pending personalized strategies that specifically target all metabolic components of cancer development in a patient, simple metabolic interventions could be tested in clinical trials in combination with standard cancer therapies, such as short cycles of fasting or the administration of sodium citrate or weakly toxic compounds (such as curcumin, metformin, lipoic acid) that target autophagy and biosynthetic or signaling pathways.
  • ||||||||||  remdesivir / Generic mfg.
    Journal:  Recent Advances towards Drug Design Targeting the Protease of 2019 novel coronavirus (2019-nCoV). (Pubmed Central) -  Aug 18, 2021   
    Pending personalized strategies that specifically target all metabolic components of cancer development in a patient, simple metabolic interventions could be tested in clinical trials in combination with standard cancer therapies, such as short cycles of fasting or the administration of sodium citrate or weakly toxic compounds (such as curcumin, metformin, lipoic acid) that target autophagy and biosynthetic or signaling pathways. In conclusion, this review summarizes recent progress in developing protease inhibitors for SARS-CoV-2.
  • ||||||||||  Journal:  Ethanol antagonizes P2X4 receptors in ventral tegmental area neurons. (Pubmed Central) -  Aug 15, 2021   
    These results support the idea that VTA neurons are inhibited by ATP, ethanol antagonizes this inhibition, and the ethanol-sensitive component of ATP inhibition is mediated by P2X4 receptors. This interaction of ethanol with P2X4 receptors may be an important regulator of the rewarding effects of ethanol, making P2X4 receptors an intriguing target for the development of agents to treat alcohol use disorders.
  • ||||||||||  Journal:  Analysis of the Structural Mechanism of ATP Inhibition at the AAA1 Subunit of Cytoplasmic Dynein-1 Using a Chemical "Toolkit". (Pubmed Central) -  Aug 13, 2021   
    Exploring ciliobrevin A geometrical configuration suggests the E isomer has a superior binding profile over the Z due to binding at the critical ATP motifs. Utilizing the refined structure of the motor domain obtained through protein conformational search in this study exhibits that Arg1852 of the yeast cytoplasmic dynein could involve in the "glutamate switch" mechanism in cytoplasmic dynein 1 in lieu of the conserved Asn in AAA+ protein family.
  • ||||||||||  Journal:  Cryo-EM structure of ABCG5/G8 in complex with modulating antibodies. (Pubmed Central) -  Aug 11, 2021   
    While mAb 11F4 increases the ATPase activity potentially by stabilization of the NBD dimer formation, mAb 2E10 inhibits ATP hydrolysis, likely by restricting the relative movement between the RecA and helical domain of ABCG8 NBD. Our study not only provides insights into the structural elements important for the transport cycle but also reveals novel epitopes for potential therapeutic interventions.
  • ||||||||||  deoxyglucose / Generic mfg.
    Journal:  The ATP synthase inhibition induces an AMPK-dependent glycolytic switch of mesenchymal stem cells that enhances their immunotherapeutic potential. (Pubmed Central) -  Aug 7, 2021   
    Human and murine-derived MSC were metabolically reprogramed using pro-inflammatory cytokines, an inhibitor of ATP synthase (oligomycin), or 2-deoxy-D-glucose (2DG)...Finally, we demonstrated that the MSC glycolytic switch effect partly depends on the activation of the AMPK signaling pathway. Altogether, our findings show that AMPK-dependent glycolytic reprogramming of MSC using an ATP synthase inhibitor contributes to their immunosuppressive and therapeutic functions, and suggest that pro-glycolytic drugs might be used to improve MSC-based therapy.
  • ||||||||||  Journal:  In S. cerevisiae hydroxycitric acid antagonizes chronological aging and apoptosis regardless of citrate lyase. (Pubmed Central) -  Aug 1, 2021   
    Genetic analyses on yeast CLS mutants indicated that part of the HCA effects can be sensed by Sch9 and Ras2, two conserved key regulators of nutritional and stress signal pathways of primary importance. Our data together with published biochemical analyses indicate that HCA may act with multiple mechanisms together with ACLY repression and allowed us to propose an integrated mechanistic model as a basis for future investigations.
  • ||||||||||  Review, Journal:  Therapeutic potential of biogenic titanium dioxide nanoparticles: a review on mechanistic approaches. (Pubmed Central) -  Jul 31, 2021   
    We have provided a detailed overview of some of these physiological mechanisms, including disruption of the electron transport chain, DNA fragmentation, mitochondrial damage, induction of apoptosis, disorganization of the plasma membrane, inhibition of ATP synthase activity, suspension of cellular signaling pathways and inhibition of enzymatic activity. The biogenic synthesis of customized titanium dioxide nanoparticles has future application potentials to do breakthroughs in the pharmaceutical sectors to advance precision medicine and to better explain the disease prognosis and treatment strategies.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg.
    Journal:  Synergistic Combination of Bioactive Hydroxyapatite Nanoparticles and the Chemotherapeutic Doxorubicin to Overcome Tumor Multidrug Resistance. (Pubmed Central) -  Jul 16, 2021   
    In addition to acting as the conventional nanocarriers to facilitate the cellular uptake and retention of DOX in MCF-7/ADR cells, more importantly, drug-free HAPNs themselves are able to prevent drug being pumped out of MDR cells through targeting mitochondria to induce mitochondrial damage and inhibit ATP production and to trigger sustained mitochondrial calcium overload and apoptosis in MDR cancer cells while not affecting normal cells. The results demonstrate that this simple but versatile bioactive nanoparticle provides a practical approach to effectively overcome MDR.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Journal:  Multicharge β-cyclodextrin supramolecular assembly for ATP capture and drug release. (Pubmed Central) -  Jul 14, 2021   
    A hyaluronidase-responsive polysaccharide supramolecular assembly was constructed from an amphiphilic β-cyclodextrin bearing seven hexylimidazolium units (AMCD), adamantyl-grafted hyaluronic acid, and chlorambucil, which showed specific cancer cell targeting and controlled drug release abilities. Interestingly, ternary supramolecular assembly can disassemble in the presence of hyaluronidase, and the released AMCD can assemble with ATP to form a stable 1 : 1 complex, which enhanced the efficacy of chlorambucil on cancer chemotherapy by inhibiting ATP hydrolysis.
  • ||||||||||  Journal:  IIIM-941, a Stilbene Derivative Inhibits NLRP3 Inflammasome Activation by Inducing Autophagy. (Pubmed Central) -  Jul 13, 2021   
    Finally, oral efficacy of IIIM-941 was also proved in MSU indued foot paw edema model of inflammation in mice at 10 and 20 mg/kg (b.w.). The compounds like IIIM-941 can be explored further for the development of therapies against diseases such as Alzheimer's disease and Parkinson's disease, where hampered autophagy and NLRP3 activation play a crucial role in the pathological development.
  • ||||||||||  Journal:  Molecular Docking studies reveals Rhein from rhubarb (Rheum rhabarbarum) as a putative inhibitor of ATP-binding Cassette Super Family G member 2. (Pubmed Central) -  Jun 30, 2021   
    The compounds like IIIM-941 can be explored further for the development of therapies against diseases such as Alzheimer's disease and Parkinson's disease, where hampered autophagy and NLRP3 activation play a crucial role in the pathological development. Our computer-based study systematically selected natural lead compounds, which could be effective in inhibiting ATP-binding cassette Super-family G member 2 and may help reverse the effect of multidrug resistance to increase the effectiveness of chemotherapy in cancer treatment.
  • ||||||||||  Journal:  Degradation of Intrinsically Disordered Proteins by the NADH 26S Proteasome. (Pubmed Central) -  Jun 30, 2021   
    These results indicate that in vitro, physiological concentrations of NADH can alter the processivity of ATP-dependent 26S PC substrates such as ODC and, more importantly, the NADH-stabilized 26S PCs promote the efficient degradation of many IDPs. Thus, ATP-independent, NADH-dependent 26S proteasome activity exemplifies a new principle of how mitochondria might directly regulate 26S proteasome substrate specificity.
  • ||||||||||  etoposide IV / Generic mfg.
    Journal:  Substituted 4,5'-Bithiazoles as Catalytic Inhibitors of Human DNA Topoisomerase IIα. (Pubmed Central) -  Jun 22, 2021   
    Selected compounds showed inhibition of human topo IIα comparable to that of the etoposide topo II drug, revealing a new class of inhibitors targeting this molecular motor...This confirms the mechanism of action of these compounds, which differs from topo II poisons also at the cellular level. Substituted 4,5'-bithiazoles appear to be a promising class for further development towards efficient and potentially safer cancer therapies exploiting the alternative topo II inhibition paradigm.
  • ||||||||||  Journal:  Nucleocapsid protein precursors NCp9 and NCp15 suppress ATP-mediated rescue of AZT-terminated primers by HIV-1 reverse transcriptase. (Pubmed Central) -  Jun 22, 2021   
    However, analysis of RNase H cleavage patterns revealed that in the presence of NCp9, RNA/DNA complexes containing duplexes of 12 base pairs had reduced stability in comparison with those obtained in the absence of NC, or with NCp7 or NCp15. These effects are expected to have a strong influence on the inhibitory action of NCp9 and NCp15, by affecting the efficiency of RNA-dependent DNA polymerization after unblocking DNA primers terminated with AZTMP and other nucleotide analogues.
  • ||||||||||  Nexletol (bempedoic acid) / Esperion Therap, Otsuka
    [VIRTUAL] Impact of ACLY on type 2 diabetes in UK Biobank: A Mendelian randomisation study () -  Jun 17, 2021 - Abstract #ESC2021ESC_354;    
    Bempedoic acid inhibits ATP citrate lyase (ACLY), a key enzyme in the cholesterol biosynthesis pathway, and has shown promising results in early-phase randomised controlled trials...Analyses exploring additional potential mediating factors, the relevance of inflammation, and the effects of ACLY on glycaemic control in individuals with diabetes are also reported. Conclusion This Mendelian randomisation study shows that genetic variants that mimic inhibition of ACLY and are associated with lower LDL-C levels lower the risks of developing T2DM as well as of CHD events.