Related ArticlesOSU-A9 induced-reactive oxygen species cause cytotoxicity in duodenal and gastric cancer cells by decreasing phosphorylated nuclear pyruvate kinase M2 protein levels. Biochem Pharmacol. 2020 Jan 16;:113811 Authors: Chiu CF, Weng JR, Lee SL, Wu CY, Chu PC, Shan YS, Yang HR, Bai LY Abstract Pyruvate kinase M2 (PKM2) is a key enzyme responsible for the final step of glycolysis. It is still unclear whether PKM2 is involved in reactive oxygen...
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Related ArticlesHGF induces protective effects in α-naphthylisothiocyanate-induced intrahepatic cholestasis by counteracting oxidative stress. Biochem Pharmacol. 2020 Jan 16;:113812 Authors: Salas-Silva S, Simoni-Nieves A, Razori MV, López-Ramirez J, Barrera-Chimal J, Lazzarini R, Bello O, Souza V, Miranda-Labra RU, Gutiérrez-Ruiz MC, Gomez-Quiroz LE, Roma MG, Bucio-Ortiz L Abstract Cholestasis is a clinical syndrome common to a large number of hepatopathies,...
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Related ArticlesThe effects of anthracycline drugs on the conformational distribution of mouse P-glycoprotein explains their transport rate differences. Biochem Pharmacol. 2020 Jan 16;:113813 Authors: Nguyen PH, Sigdel KP, Schaefer GAK, Mensah KG, King GM, Roberts AG Abstract P-glycoprotein (Pgp) is an ATP-dependent efflux transporter and plays a major role in anti-cancer drug resistance by pumping a chemically diverse range of cytotoxic drugs from cancerous...
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Related ArticlesPathway analysis of glutamate-mediated, calcium-related signaling in glioma progression. Biochem Pharmacol. 2020 Jan 16;:113814 Authors: Pei Z, Lee KC, Khan A, Erisnor G, Wang HY Abstract Brain tumors, particularly high-grade glioblastomas, are a crucial public health issue due to poor prognosis and an extremely low survival rate. The glioblastoma multiforme (GBM) grows rapidly within its unique microenvironment that is characterized...
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Related ArticlesStability and pharmacokinetics of separase inhibitor-sepin-1 in sprague-dawley rats. Biochem Pharmacol. 2020 Jan 10;:113808 Authors: Zhang N, Sarkar AK, Li F, Demerzhan SA, Gilbertson SR, Pati D Abstract Separase, a sister chromatid cohesion-resolving enzyme, is an oncogene and overexpressed in many human cancers. Sepin-1 (2,2-dimethyl-5-nitro-2H-benzimidazole-1,3-dioxide) is a potent Separase inhibitor that impedes cancer cell growth,...
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Related ArticlesHumanized mice as preclinical models for myeloid malignancies. Biochem Pharmacol. 2020 Jan 09;:113794 Authors: Gbyli R, Song Y, Halene S Abstract Humanized mice have proven to be invaluable for human hematological translational research since they offer essential tools to dissect disease biology and to bridge the gap between pre-clinical testing of novel therapeutics and their clinical applications. Many efforts have been placed to advance...
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Related ArticlesIs There Enough Evidence to Classify Cycloalkyl Amine Substituents as Structural Alerts? Biochem Pharmacol. 2020 Jan 09;:113796 Authors: Kalgutkar AS, Driscoll JP Abstract Basic amine substituents provide several pharmacokinetic benefits relative to acidic and neutral functional groups, and have been extensively utilized as substituents of choice in drug design. On occasions, basic amines have been associated with off-target pharmacology...
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Related ArticlesCurcumol enhances the sensitivity of doxorubicin in triple-negative breast cancer via regulating the miR-181b-2-3p-ABCC3 axis. Biochem Pharmacol. 2020 Jan 09;:113795 Authors: Zeng C, Fan D, Xu Y, Li X, Yuan J, Yang Q, Zhou X, Lu J, Zhang C, Han J, Gu J, Gao Y, Sun L, Wang S Abstract Chemoresistance is a major cause of recurrence and poor prognosis in triple-negative breast cancer (TNBC) patients. The essential oil of Rhizoma Curcumae...
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Related ArticlesThe kinase inhibitor BX795 suppresses the inflammatory response via multiple kinases. Biochem Pharmacol. 2020 Jan 09;:113797 Authors: Yu T, Wang Z, Jie W, Fu X, Li B, Xu H, Liu Y, Li M, Kim E, Yang Y, Youl Cho J Abstract BX795, a small molecule with an aminopyrimidine backbone, is a potent ATP-competitive inhibitor of phosphoinositide-dependent kinase 1 (PDK1) and TANK-binding kinase 1 (TBK1). BX795 has significant functions in various...
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Related ArticlesSmall molecule inhibitors and stimulators of inducible nitric oxide synthase in cancer cells from natural origin (phytochemicals, marine compounds, antibiotics). Biochem Pharmacol. 2020 Jan 08;:113792 Authors: Özenver N, Efferth T Abstract Nitric oxide synthases (NOS) are a family of isoforms, which generate nitric oxide (NO). NO is one of the smallest molecules in nature and acts mainly as a potent vasodilator. It participates in various...
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Related ArticlesHistorical origins of the discovery of mammalian nitric oxide (nitrogen monoxide) production/physiology/pathophysiology. Biochem Pharmacol. 2020 Jan 07;:113793 Authors: Lancaster JR Abstract The award of the 1998 Nobel Prize in Physiology or Medicine to Robert F. Furchgott, Louis J. Ignarro, and Ferid Murad "for their discoveries concerning nitric oxide as a signaling molecule in the cardiovascular system" highlighted the discovery of...
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A novel molecular mechanism involved in the crosstalks between homologous and PKC-mediated heterologous regulatory pathway of dopamine D2 receptor. Biochem Pharmacol. 2020 Jan 06;:113791 Authors: Zhang X, Min X, Zhu A, Kim KM Abstract Protein kinase C (PKC) is one of the major effectors involved in the heterologous regulatory pathways of G protein-coupled receptors (GPCRs). On the other hand, GRK2 and β-arrestins are the players of homologous regulatory...
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SOX9: The Master Regulator of Cell Fate in Breast Cancer. Biochem Pharmacol. 2020 Jan 03;:113789 Authors: Jana S, Krishna BM, Singhal J, Horne D, Awasthi S, Salgia R, Singhal SS Abstract SRY-related high-mobility group box 9 (SOX9) is an indispensable transcription factor that regulates multiple developmental pathways related to stemness, differentiation, and progenitor development. Previous studies have demonstrated that the SOX9 protein directs pathways...
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Potential of phytochemicals as immune-regulatory compounds in atopic diseases: a review. Biochem Pharmacol. 2020 Jan 03;:113790 Authors: Sharma S, Naura AS Abstract Atopic diseases (atopic dermatitis, asthma and allergic rhinitis) affects a huge number of people around the world and their incidence rate is on rise. Atopic dermatitis (AD) is more prevalent in paediatric population which sensitizes an individual to develop allergic rhinitis and asthma...
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Related ArticlesCharacterization of AN6001, a positive allosteric modulator of α6β2-containing nicotinic acetylcholine receptors. Biochem Pharmacol. 2019 Dec 27;:113788 Authors: van Hout M, Klein J, Ahring PK, Brown DT, Thaneshwaran S, Dos Santos AB, Jensen AA, Kohlmeier KA, Christophersen P, Dyhring T Abstract α6β2-containing nicotinic acetylcholine receptors (α6β2* nAChRs) are predominantly expressed in midbrain dopaminergic neurons, including substantia...
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Related ArticlesAndrographolide Promotes Pancreatic Duct Cells Differentiation into Insulin-Producing Cells by Targeting PDX-1. Biochem Pharmacol. 2019 Dec 27;:113785 Authors: Zhang S, Huang F, Tian W, Lai J, Qian L, Hong W, Chen H, Li LC Abstract Regeneration of β-cells by differentiation of pancreatic progenitor cells has the potential to fundamentally solve the problems of the loss of β-cell function and mass during disease progression in both type...
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Related ArticlesCharacterization of AN317, a novel selective agonist of α6β2-containing nicotinic acetylcholine receptors. Biochem Pharmacol. 2019 Dec 27;:113786 Authors: Sandager-Nielsen K, Ahring PK, Klein J, Hout MV, Thaneshwaran S, Santos ABD, Jacobsen TA, Amrutkar DV, Peters D, Jensen AA, Kohlmeier KA, Christophersen P, Dyhring T Abstract Neuronal nicotinic acetylcholine receptors (nAChRs) are crucial mediators of central presynaptic, postsynaptic,...
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Related ArticlesProfiling of anabolic androgenic steroids and selective androgen receptor modulators for interference with adrenal steroidogenesis. Biochem Pharmacol. 2019 Dec 26;:113781 Authors: Patt M, Beck KR, Di Marco T, Jäger MC, González-Ruiz Data Analysis V, Boccard Data Analysis J, Rudaz Data Analysis S, Hartmann RW, Salah M, van Koppen CJ, Grill M, Odermatt A Abstract Anabolic-androgenic steroids (AAS) are testosterone derivatives developed...
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Related ArticlesImmune-mediated anti-tumor effects of metformin; targeting metabolic reprogramming of T cells as a new possible mechanism for anti-cancer effects of metformin. Biochem Pharmacol. 2019 Dec 26;:113787 Authors: Bahrambeigi S, Shafiei-Irannejad V Abstract Immunotherapy-based cancer treatment has revolutionized the era of cancer patients recuperation and it has brought a strong hope to treatment of some types of cancers. Metformin, a widely...
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Related ArticlesAdenosinergic Signalling In Chondrogenesis And Cartilage Homeostasis: Friend Or Foe? Biochem Pharmacol. 2019 Dec 26;:113784 Authors: Pinto Cardoso R, Pereira Costa F, Pedro Faria J, Bandarrinha P, Bessa Andres C, Correia-de-Sa P, Bernardo Noronha Matos J Abstract Chondrocytes and their mesenchymal cell progenitors secrete a variety of bioactive molecules, including adenine nucleotides and nucleosides, but these molecules are not usually...
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Related ArticlesStructural basis of the potency and selectivity of Urotoxin, a potent Kv1 blocker from scorpion venom. Biochem Pharmacol. 2019 Dec 24;:113782 Authors: Luna-Ramirez K, Csoti A, McArthur JR, Chin YKY, Anangi R, Del Carmen Najera R, Possani LD, King GF, Panyi G, Yu H, Adams DJ, Finol-Urdaneta RK Abstract Urotoxin (α-KTx-6), a peptide from venom of the Australian scorpion Urodacus yaschenkoi, is the most potent inhibitor of Kv1.2 described...
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Related ArticlesInteraction of Oatp1b2 Expression and Nonalcoholic Steatohepatitis on Pravastatin Plasma Clearance. Biochem Pharmacol. 2019 Dec 24;:113780 Authors: Toth EL, Clarke JD, Csanaky IL, Cherrington NJ Abstract The downregulation of hepatic uptake transporters, including those of the OATP family, are a well known consequence of nonalcoholic steatohepatitis (NASH). Prior studies have shown that the combination of NASH and Oatp1b2 knockout synergistically...
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Related ArticlesStearoylethanolamide interferes with retrograde endocannabinoid signalling and supports the blood-brain barrier integrity under acute systemic inflammation. Biochem Pharmacol. 2019 Dec 24;:113783 Authors: Kasatkina LA, Heinemann A, Hudz YA, Thomas D, Sturm EM Abstract Neuroinflammation plays a prominent role in the onset of demyelinating diseases, major depressive disorder and delayed neurodegeneration. An open question remains whether...
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Related ArticlesPyroptotic and apoptotic cell death in iNOS and nNOS overexpressing K562 cells: a mechanistic insight. Biochem Pharmacol. 2019 Dec 24;:113779 Authors: Sadaf S, Awasthi D, Singh AK, Nagarkoti S, Kumar S, Barthwal MK, Dikshit M Abstract Previous studies from this lab and others have demonstrated that nitric oxide (NO) in a concentration dependent manner, modulated neutrophil and leukemic cell survival. Subsequent studies delineated importance...
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Related ArticlesMolecular therapy with derivatives of amino benzoic acid inhibits tumor growth and metastasis in murine models of bladder cancer through inhibition of TNFα/NFΚB and iNOS/NO pathways. Biochem Pharmacol. 2019 Dec 23;:113778 Authors: Girouard J, Belgorosky D, Hamelin-Morrissette J, Boulanger V, D'Orio E, Ramla D, Perron R, Charpentier L, Van Themsche C, Maria Eiján A, Bérubé G, Reyes-Moreno C Abstract Muscle-invasive bladder cancer (MIBC)...
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Related ArticlesAntiviral drug discovery against arthritogenic alphaviruses: tools and molecular targets. Biochem Pharmacol. 2019 Dec 21;:113777 Authors: Abdelnabi R, Jacobs S, Delang L, Neyts J Abstract Alphaviruses are (mainly) arthropod-borne viruses that belong to the family of the Togaviridae. Based on the disease they cause, alphaviruses are divided into an arthritogenic and an encephalitic group. Arthritogenic alphaviruses such as the chikungunya...
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Related ArticlesBerberine suppresses colon cancer cell proliferation by inhibiting the SCAP/SREBP-1 signaling pathway-mediated lipogenesis. Biochem Pharmacol. 2019 Dec 21;:113776 Authors: Yunxin L, Weiwei H, Yao L, Xirui X, Zheng Z, Chao L, Jianjun Z, Jun L, Xianjun F, Yubing Z Abstract Lipid metabolism is a significant section of energy homeostasis, and it affects the development of various cancers. Previous studies have revealed that berberine has...
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Related ArticlesInhibition of lipolysis: a novel explanation for the hypothermic actions of Acetaminophen in Non-Febrile Rodents. Biochem Pharmacol. 2019 Dec 20;:113774 Authors: Bashir S, Elegunde B, Morgan WA Abstract Acetaminophen is both widely used to treat children with fever and is also responsible for thousands being hospitalised annually. Historically the antipyretic actions of acetaminophen were attributed to the inhibition of cyclooxygenase...
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Related ArticlesHydrogen sulfide modulates epithelial-mesenchymal transition and angiogenesis in non-small cell lung cancer via HIF-1α activation. Biochem Pharmacol. 2019 Dec 20;:113775 Authors: Wang M, Yan J, Cao X, Hua P, Li Z Abstract Hydrogen sulfide (H2S) has been frequently implicated in tumor progression. However, the exact regulation mechanism of H2S in human non-small cell lung cancer (NSCLC) has not been fully elucidated. Here, analysis of...
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Related ArticlesCorrigendum to "A novel long non-coding RNA-ARA: Adriamycin resistance-associated" [Biochem. Pharmacol. 87 (2014) 254-283]. Biochem Pharmacol. 2019 Dec 20;172:113732 Authors: Jiang M, Huang O, Xie Z, Wu S, Zhang X, Shen A, Liu H, Chen X, Wu J, Lou Y, Mao Y, Sun K, Hu S, Geng M, Shen K PMID: 31869579 [PubMed - as supplied by publisher]
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Related ArticlesCircadian Pharmacological Effects of Berberine on Chronic Colitis in Mice: Role of the Clock Component Rev-erbα. Biochem Pharmacol. 2019 Dec 19;:113773 Authors: Zhou Z, Lin Y, Gao L, Yang Z, Wang S, Wu B Abstract Berberine, initially isolated from Rhizoma Coptidis (Huanglian in Chinese), is a drug used to treat gastrointestinal disorders such as colitis. Here we uncovered a time-varying berberine effect on chronic colitis in mice, and...
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Related ArticlesDACT2 modulated by TFAP2A-mediated allelic transcription promotes EGFR-TKIs efficiency in advanced lung adenocarcinoma. Biochem Pharmacol. 2019 Dec 19;:113772 Authors: Zhang N, Li Y, Xie M, Song Y, Liu J, Lei T, Shen Y, Yu J, Yang M Abstract Patients with epidermal growth factor receptor (EGFR)-mutant advanced non-small-cell lung cancer (NSCLC) benefits from EGFR-tyrosine kinase inhibitor (TKI) treatment. However, drug resistance to EGFR-TKIs...
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Related ArticlesAT-533, a novel Hsp90 inhibitor, inhibits breast cancer growth and HIF-1α/VEGF/VEGFR-2-mediated angiogenesis in vitro and in vivo. Biochem Pharmacol. 2019 Dec 18;:113771 Authors: Zhang PC, Liu X, Li MM, Ma YY, Sun HT, Tian XY, Wang Y, Liu M, Fu LS, Wang YF, Chen HY, Liu Z Abstract The inhibition of angiogenesis is suggested to be an attractive strategy for cancer therapeutics. Heat shock protein 90 (Hsp90) is closely related to tumorigenesis...
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Related ArticlesCCI52 sensitizes tumors to 6-mercaptopurine and inhibits MYCN-amplified tumor growth. Biochem Pharmacol. 2019 Dec 17;:113770 Authors: Huynh T, Murray J, Flemming CL, Kamili A, Hofmann U, Cheung L, Roundhill EA, Yu DMT, Webber HT, Schwab M, Henderson MJ, Haber M, Norris MD, Fletcher JI Abstract The antimetabolite 6-mercaptopurine (6-MP) is an important component in the treatment of specific cancer subtypes, however, the development of...
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Related ArticlesNitric oxide and tumor metabolic reprogramming. Biochem Pharmacol. 2019 Dec 17;:113769 Authors: López-Sánchez LM, Aranda E, Rodríguez-Ariza A Abstract Nitric oxide (NO) has been highlighted as an important agent in tumor processes. However, a complete understanding of the mechanisms by which this simple diatomic molecule contributes in tumorigenesis is lacking. Evidence is rapidly accumulating that metabolic reprogramming is a major new...
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Related ArticlesA mutation of cysteine 46 in IKK-β promotes mPGES-1 and caveolin-1 expression to exacerbate osteoclast differentiation and osteolysis. Biochem Pharmacol. 2019 Dec 13;:113762 Authors: Zou B, Zhang Y, Li T, Liu J, Deng W, Tan Y, Yang Q, Ding Z, Liao K, Xu J, Pan H, Li X, Liu L Abstract IKK-β is indispensable for inflammatory osteolysis, the functional residues of IKK-β are therapeutic drug targets for developing inhibitors to treat multiple...
Dec 2019
Related ArticlesPhysiologically relevant screening of polyphenol-rich commercial preparations for bioactivity in vascular endothelial cells and application to healthy volunteers: a viable workflow and a cautionary tale. Biochem Pharmacol. 2019 Dec 11;:113754 Authors: Jones HS, Papageorgiou M, Gordon A, Ehtesham, Javed Z, Wells LK, Greetham S, Doyle B, Hayes N, Rigby A, Atkin SL, Courts FL, Sathyapalan T Abstract This study describes the screening of...
Dec 2019
Related ArticlesInsight into Tartrate Inhibition Patterns in vitro and in vivo Based on Cocrystal Structure with UDP-glucuronosyltransferase 2B15. Biochem Pharmacol. 2019 Dec 11;:113753 Authors: Zhang L, Zhu L, Qu W, Wu F, Hu M, Xie W, Liu Z, Wang C Abstract Glucuronidation, catalyzed by UDP-glucuronosyltransferases (UGTs), is a crucial substance metabolism and elimination process that mostly occurs in the liver to protect the body from toxic substances...
Dec 2019
Related ArticlesRIPK1 inhibitor ameliorates colitis by directly maintaining intestinal barrier homeostasis and regulating following IECs-Immuno crosstalk. Biochem Pharmacol. 2019 Dec 11;:113751 Authors: Lu H, Li H, Fan C, Qi Q, Yan Y, Wu Y, Feng C, Wu B, Gao Y, Zuo J, Tang W Abstract BACKGROUND: The receptor-interacting protein kinase 1 (RIPK1) has emerged as a key upstream regulator that controls the inflammatory response via its kinase-dependent and...
Dec 2019
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