• Thus, when topoisomerase I inhibition occurs with agents such as SN-38 in cell lines, the cells compensate by increasing expression of topoisomerase II and vice versa. (cancernetwork.com)
  • 3] This antagonism might be related to topoisomerase I inhibition of DNA synthesis, which is required for the cytotoxic effect of topoisomerase II-induced cleavable complexes. (cancernetwork.com)
  • A correlation was seen among bortezomib dose, proteasome inhibition, and positive modulation of serum prostate-specific antigen. (aacrjournals.org)
  • 2005 Genovese 2009 Many drug discovery programs have focused on the inhibition of the α-form but essentially all p38α MAPK inhibitors also interact with the β-isoform. (conferencedequebec.org)
  • A powerful and suffered inhibition of inflammatory procedures within this compartment may be pivotal for the efficiency of p38α/β MAPK inhibitors and for that reason the right and dependable in vitro chondrocyte model may deliver important info for determining the molecular properties needed of clinical applicants. (conferencedequebec.org)
  • One is the inhibition of the initial binding of topo II to DNA as in the case of chloroquine (3) and aclarubicin (4,5). (allindianpatents.com)
  • Human type II topoisomerases (TopoII) are essential for controlling DNA topology within the cell. (h-its.org)
  • In cell lines, the cytotoxic effect of topoisomerase I and II is scheduledependent. (cancernetwork.com)
  • A receptor tyrosine kinase inhibitor and chemotherapeutic agent used for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). (drugbank.com)
  • Revers ible lysine acetylation represents a common modification of proteins that is carried out by histone acetyl trans ferases and Inhibitors,Modulators,Libraries histone deacetylases. (ampk-signal.com)
  • Figure 2: PAR is the direct target of histone macroH2A1.1's macrodomain. (nature.com)
  • Panobinostat is a histone deacetylase (HDAc) inhibitor. (medscape.com)
  • A non-selective histone deacetylase inhibitor used to treat multiple myeloma in combination with other antineoplastic agents. (drugbank.com)
  • We describe areas where major inroads were initially achieved by targeting angiogenesis and by unraveling pathways in the heterogeneous tumors of mesenchymal origin-spurred by the identification of c-Kit-activating mutations in GIST and the regressions that ensued when tumors harboring these mutations were exposed to the tyrosine kinase inhibitor imatinib (Gleevec). (cancernetwork.com)
  • Here, in Part I, we describe areas where major inroads were initially achieved by targeting angiogenesis (central to the biology of renal cell carcinoma and hepatocellular cancer) and by unraveling pathways in the heterogeneous tumors of mesenchymal origin-spurred by the identification of c-Kit-activating mutations in gastrointestinal stromal tumors (GIST) and the regressions that ensued when tumors harboring these mutations were exposed to the tyrosine kinase inhibitor imatinib (Gleevec). (cancernetwork.com)
  • Studies with bortezomib (VELCADE, formerly known as PS-341) and other proteasome inhibitors indicate that cancer cells are especially dependent on the proteasome for survival, and several mechanisms used by prostate cancer cells require proteasome function. (aacrjournals.org)
  • Bortezomib is the first drug approved in the group of anticancer agents known as proteasome inhibitors. (medscape.com)
  • The Hsp90 inhibitors geldanamycin, 17-AAG (17-allylamino-17-demethoxygeldanamycin) and radicicol significantly enhanced the activity of the topoisomerase II poisons etoposide and mitoxantrone in vitro and in vivo. (uea.ac.uk)
  • [2] Artemisinin dimer oxime (Ox) - dimer molecule synthesized from artemisinin possesses high bioavailability and marked in vitro anticancer activities compared to its monomers. (wjtcm.net)
  • Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. (epigenetics-modulation-frontier.com)
  • AZD5582 dihydrochloride CAS No. : 1883545-51-4 Biological Activity:AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. (epigenetics-modulation-frontier.com)
  • MV1 CAS No. : 1001600-54-9 Biological Activity:MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand. (epigenetics-modulation-frontier.com)
  • Selected flavonoids were tested for their ability to inhibit the catalytic activity of DNA topoisomerase (topo) I and II. (ucy.ac.cy)
  • Six members of Class II are further sub grouped into Class IIa and Class IIb, based on whether they possess one or two catalytic sites, re spectively. (ampk-signal.com)
  • In particular, the invention relates to the use of a topo II catalytic inhibitor such as the bisdioxopiperazine ICRF-187 for the manufacture of a medicament for the treatment of an accidental extravasation of a topoisomerase II poison and a method for treatment of such extravasation of a topoisomerase poison such as the anthracyclines daunorubicin, doxorubicin, epirubicin, or idarubicin. (allindianpatents.com)
  • The present invention relates to a pharmaceutical composition for the prevention or treatment of tissue damage due to extravasation caused by a topoisomerase II poison in a patient receiving treatment with saved poisons and to the use of said topo II catalytic inhibitor for the manufacture of a medicament for the prevention or treatment of said tissue damage due to extravasation caused by said topoisomerase II poison. (allindianpatents.com)
  • Topoisomerase II, topoisomerase II poisons, and topoisomerase H catalytic inhibitors The topoisomerase II (topo II) enzymes belong to a system of nuclear enzymes involved in the processing of DNA during the cell cycles. (allindianpatents.com)
  • Drugs acting on topo II are divided into two main categories, topo II poi¬sons and topo II catalytic inhibitors. (allindianpatents.com)
  • The topo II poisons shift the equilibrium of the catalytic cycle towards cleavage, thereby increasing the concentration of the transient protein-associated breaks in the genome (1) (see Fig.1). (allindianpatents.com)
  • The topo II catalytic inhibitor is an entirely different group of drugs. (allindianpatents.com)
  • They act by in¬terfering with the overall catalytic function, which can be accomplished in at least two ways. (allindianpatents.com)
  • Dovitinib (TKI258) is a small molecule multi-kinase inhibitor currently in clinical phase I/II/III development for the treatment of various types of cancers. (molcells.org)
  • A kinase inhibitor used to treat patients with Erdheim-Chester Disease who have the BRAF V600 mutation, and melanoma in patients who have the BRAF V600E mutation. (drugbank.com)
  • In this systematic review, cases of HLH reported after COVID-19 vaccination have been examined to understand the relationship between the two and propose effective therapeutic strategies. (bvsalud.org)
  • KEGG pathway term mTOR signaling pathway is observed to be meliorated in this tricluster and has been reported to be associated Inhibitors,Modulators,Libraries with estrogen induced breast cancer cell. (ampk-signal.com)
  • The present invention relates to a method and a medicament for pharmacological treatment of accidental extravasation of topoisomerase II poisons such as anthracyclines. (allindianpatents.com)
  • Examples of such topoisomerase II poisons include anthracyclines. (allindianpatents.com)
  • Thus, the anthra¬cyclines are classified as topo II poisons. (allindianpatents.com)
  • One such strategy is to target topoisomerase II-interacting proteins. (uea.ac.uk)
  • Here we report the identification of potential topoisomerase II-associated proteins using immunoprecipitation, followed by 1-D and 2-D gel electrophoresis and MALDI-TOF mass spectrometry. (uea.ac.uk)
  • A total of 23 proteins were identified and, of these, 17 were further validated as topoisomerase IIα-associated proteins by coimmunoprecipitation and Western blot. (uea.ac.uk)
  • Six of the interacting proteins were cellular chaperones, including 3 members of the heat shock protein-90 (Hsp90) family, and so the effect of Hsp90 modulation on the antitumor activity of topoisomerase II drugs was tested using the sulforhodamine B assay, clonogenic assays and a xenograft model. (uea.ac.uk)
  • Thus, our method of identifying topoisomerase II-interacting proteins appears to be effective, and at least 1 novel topoisomerase IIα-associated protein, Hsp90, may represent a valid drug target in the context of topoisomerase II-directed chemotherapy. (uea.ac.uk)
  • The central role of p38MAP kinases (p38MAPK) foremost the α-isoform in the production of inflammatory response proteins such as TNF-α interleukin-1β (IL-1β) COX-2 and microsomal prostaglandin E synthase (mPGES1) is well noted (Masuko-Hongo et al. (conferencedequebec.org)
  • It was previously reported that proadifen (SKF-525A), a well-known cytochrome P450 monooxygenase inhibitor, not only has anti-proliferative potential in some cancer cell lines, but it is also able to inhibit BCRP and MRP1 transporter proteins ( 8 ). (spandidos-publications.com)
  • Various reports implicated host cellular proteins as a key factor that either interact directly with HIV-1 integrase (IN) or get involved in the integration process of virus resulting in the modulation of integration step. (biomedcentral.com)
  • Biological Activity: Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. (epigenetics-modulation-frontier.com)
  • Azilsartan CAS No. : 147403-03-0 Biological Activity:Azilsartan (TAK-536) is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. (epigenetics-modulation-frontier.com)
  • Irbesartan CAS No. : 138402-11-6 Biological Activity:Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). (epigenetics-modulation-frontier.com)
  • Tumor cell resistance to anthracyclines and epipodophyllotoxins can be due to reduced drug accumulation and/or alterations in the activity of topoisomerase II (TOPO II). (ucy.ac.cy)
  • The effects of WR-1065 (2-((aminopropyl)amino)ethanethiol) on cell cycle progression, topoisomerase (topo) IIα activity, and topo IIα phosphorylation in Chinese hamster ovary (CHO) cells have been investigated. (ucy.ac.cy)
  • Dr. Yalowich's lab focuses on the mechanisms of action and resistance to DNA topoisomerase II (topo II)-targeted agents, such as the anticancer agent etoposide (VP-16). (osu.edu)
  • Recent work has characterized alternative RNA processing of topo IIα pre-mRNA that results in decreased expression of full-length topo II in acquired resistance to VP-16. (osu.edu)
  • Finally, the use of nutritional antioxidants (such as vitamin C) is under investigation as a strategy to prevent cancer-causing effects of topo II-targeted agents, which can arise in patients years after therapy is complete. (osu.edu)
  • That is, they trap the cleavable complexes, which converts the essential topo II enzyme into a lethal one(2). (allindianpatents.com)
  • The other is by locking topo II in its closed-clamp step after religation as appears to be the case for the ICRF-187 and its analogues (6-9). (allindianpatents.com)
  • The antitumor effect is explained by the ability to inhibit the nuclear enzyme DNA topo II. (allindianpatents.com)
  • hsa-miR-9-3p and hsa-miR-9-5p as Post-Transcriptional Modulators of DNA Topoisomerase II in Human Leukemia K562 Cells with Acquired Resistance to Etoposide. (osu.edu)
  • An increase of fluor escent intensity yields a positive fold change and a de crease, accordingly Inhibitors,Modulators,Libraries a negative fold change. (ampk-signal.com)
  • Inhibitors,Modulators,Libraries Consistent with chromatin structure dependent activation of gene expression, many transcriptional co activators possess HAT activity whereas transcriptional co repressors are associated with HDACs. (ampk-signal.com)
  • The mammalian HDACs are Inhibitors,Modulators,Libraries divided into the classical family of 11 zinc dependent hydrolases and the non classical family of seven NAD dependent HDACs called sirtuins. (ampk-signal.com)
  • The HDAC members of class I contain a central deacetylase domain surrounded by short Inhibitors,Modulators,Libraries NH2 and COOH termini. (ampk-signal.com)
  • Eigengene of tri cluster 7 has been found to be di?erentially expressed between 0 hour 6 hours, 0 hour 12 hours, 3 hours 12 hours and 6 hours Inhibitors,Modulators,Libraries 12 hours. (ampk-signal.com)
  • Consequently, ROS-modulation has emerged as an anticancer strategy with synthesis of various ROS-inducing or responsive agents that target cancer cells. (degruyter.com)
  • Using these models, we attempted treatment of xenografts with topotecan - a known anticancer drug and artemisinin dimer oxime or combination of these two drugs. (wjtcm.net)
  • Other valuable properties of the chimeric polymerases TopoTaq and PfuC2 include enhanced thermostability, specificity and resistance to contaminants and inhibitors. (wikipedia.org)
  • This invention relates to methods of inducing differential stress resistance in a subject with cancer by starving the subject for a short term, administering a cell growth inhibitor to the subject, or reducing the caloric or glucose intake by the subject. (justia.com)
  • In particular, the present invention provides methods for enhancing the effectiveness of chemotherapy by inducing differential stress resistance in normal cells and cancer cells via short-term starvation, cell growth inhibitors, or reduced caloric or glucose intake. (justia.com)
  • CRISPR/Cas9 Genome Editing of the Human Topoisomerase II Intron 19 5' Splice Site Circumvents Etoposide Resistance in Human Leukemia K562 Cells. (osu.edu)
  • Effects of DNA topoisomerase IIα splice variants on acquired drug resistance. (osu.edu)
  • As we previously described, proadifen, a P450 monooxygenase inhibitor, might also be able to inhibit some ABC transporters, including breast cancer resistance protein (BCRP). (spandidos-publications.com)
  • Moreover, the identification of fork protection as a key mechanism of resistance to chemo- and poly (ADP-ribose) polymerase inhibitor therapy in ovarian cancer further increases the priority that should be accorded to the development of strategies targeting replicative stress. (bmj.com)
  • Small molecule inhibitors designed to target the DNA damage sensors, such as inhibitors of ataxia telangiectasia-mutated (ATM), ATR, CHK1 and WEE1, impair smooth cell cycle modulation and disrupt efficient DNA repair, or a combination of the above, have demonstrated interesting monotherapy and combinatorial activity, including the potential to reverse drug resistance and have entered developmental pipelines. (bmj.com)
  • This natural 8-ring 24-membered macroheterocycle (Figure 2 ) displays high affinity for quadruplex and most importantly has no affinity for duplex DNA ( vide infra ). (hindawi.com)
  • Herein, we investigated the effect of dovitinib on human recombinant bone morphogenetic protein (BMP)-2-induced osteoblast differentiation in a cell culture model. (molcells.org)
  • Dovitinib enhanced the BMP-2-induced alkaline phosphatase (ALP) induction, which is a representative marker of osteoblast differentiation. (molcells.org)
  • Our results suggest that dovitinib has a potent stimulating effect on BMP-2-induced osteoblast differentiation and this existing drug has potential for repositioning in the treatment of bone-related disorders. (molcells.org)
  • VEGF inhibitors directly bind to the VEGF protein to disrupt angiogenesis. (medscape.com)
  • It is described as an angiogenesis inhibitor and a phytoestrogen . (wikipedia.org)
  • Smoothed Potential MD Simulations for Dissociation Kinetics of Etoposide To Unravel Isoform Specificity in Targeting Human Topoisomerase II. (h-its.org)
  • The topoisomerase II-Hsp90 complex: A new chemotherapeutic target? (uea.ac.uk)
  • The modulation of DNA topology by topoisomerase II plays a crucial role during chromosome condensation and segregation in mitosis and has thus become a highly attractive target for chemotherapeutic drugs. (uea.ac.uk)
  • Jenkins, John R. / The topoisomerase II-Hsp90 complex: A new chemotherapeutic target? . (uea.ac.uk)
  • An ACE inhibitor prodrug used to treat hypertension, mild to moderate congestive heart failure, and to reduce cardiovascular risk in patients with hypertension or post-myocardial infarction. (drugbank.com)
  • Chemical PARP1 inhibitors, PARP1 knockdown and mutation of ADP-ribose-binding residues in macroH2A1.1 abrogate macrodomain recruitment. (nature.com)
  • these 2 events, in turn, can inhibit growth of neoplastic cells. (medscape.com)
  • T opoisomerase enzymes I and II play a critical role in preserving DNA topology by producing transient single- and double-strand DNA breaks that relieve supercoiling during replication, recombination, chromosomal decondensation, and RNA transcription. (cancernetwork.com)
  • Topoisomerase I/II inhibitor 3 can be used for liver cancer research. (epigenetics-modulation-frontier.com)
  • This combination regimen in patients with upper gastrointestinalmalignancies and breast cancer will be investigated as partof phase II studies, once the dose-limiting toxicity is determined. (cancernetwork.com)
  • For each cancer discussed in the first part of our overview, as well as in Part II, which will deal with more common cancers, we briefly cover the tumor biology, how targeting was achieved, the introduction of immune modulation or immune-conjugates, and the impact these therapies are having in the disease. (cancernetwork.com)
  • Cancer cells also enhance glucose-uptake to fuel these enhanced metabolic activities [ 2 ]. (degruyter.com)
  • ROS-modulation in normal vs. cancer cell. (degruyter.com)
  • Two human papillomavirus (HPV) vaccines are now available for prevention of HPV-associated dysplasias and neoplasias, including cervical cancer, genital warts (condylomata acuminata), and precancerous genital lesions. (medscape.com)
  • Pancreatic cancer is an aggressive malignancy with less than 5% of the patients alive at 5 years and 92% of the patients dead at 2 years[ 1 , 2 ]. (wjgnet.com)
  • Often the cancer is eliminated (as evidenced by no remission) in a period of no more than several days to about two-three months and does not recur. (justia.com)
  • The International Association for the Study of Lung Cancer defines limited-stage SCLC (LS-SCLC) as: "disease restricted to one hemithorax with regional lymph node metastases, including hilar, ipsilateral and contralateral mediastinal, and ipsilateral and contralateral supraclavicular nodes and should also include patients with ipsilateral pleural effusion independent of whether cytology is positive or negative" 2 . (ersjournals.com)
  • With the addition of granulocytecolony-stimulating factor (G-CSF [Neupogen]) to the regimen,patients received epirubicin at clinically relevant doses after dose-escalation.Results of the topoisomerase activity will be reported with thefinal results of this phase I study. (cancernetwork.com)
  • Results of the topoisomerase activity will be reported with the final results of this phase I study. (cancernetwork.com)
  • Two-fold elevation in metabolic activity of platelets stimulated by thrombin as compared to untreated cells was observed. (ukrbiochemjournal.org)
  • The interaction of human topoisomerase 1B and dimethylmyricacene, a compound prepared semisynthetically from myricanol extracted from Myrica cerifera root bark, was investigated using enzymatic activity assays and molecular docking procedures. (mdpi.com)
  • Microtubule inhibitors potently decreased FXR reporter gene activity. (nature.com)
  • β MAPK inhibitor either only or in combination with methotrexate a significant benefit was not observed. (conferencedequebec.org)
  • For example the p38α/β MAPK inhibitors SB239063 and SD-282 (Smith et al. (conferencedequebec.org)
  • 2006 Very similar results had been obtained once the efficiency of p38α/β MAPK inhibitors was looked into by high-content evaluation in SW1353 chondrocytes and baby hamster kidney cells (Ross et al. (conferencedequebec.org)
  • 2005 To handle the complex connections in chondrocyte signalling and its own assumed relevance for the anti-arthritic efficiency of p38α/β MAPK 511-28-4 IC50 inhibitors a worldwide gene appearance evaluation in primary individual chondrocytes after arousal with IL-1β within the lack and existence of SB203580 (Joos et al. (conferencedequebec.org)
  • Multidrug-resistant clinical isolate Klebsiella pneumoniae BM4686 was highly resistant to 4,6-disubstituted 2-deoxystreptamines and to fortimicin. (pasteur.fr)
  • The HIV-1 life cycle includes two essential processes, reverse transcription, forming the linear double stranded DNA (cDNA) and the integration of viral dsDNA into host genome. (biomedcentral.com)
  • They are involved in DNA repair during retroviral integration process as well as viral Long terminal repeat (2-LTR) formation, which occurs in the absence of viral DNA integration. (biomedcentral.com)
  • 2009 To characterize 511-28-4 IC50 the pharmacological profile of different p38α/β inhibitors in IL-1β-activated chondrocytes in line with the microarray evaluation a -panel of 511-28-4 IC50 genes was chosen and quantitative real-time PCR assays had been developed. (conferencedequebec.org)
  • The aminothiol 2-[(aminopropyl)amino]ethanethiol (WR-1065) is the active thiol of the clinically studied radioprotective agent S-2-(3- aminopropylamino)ethylphosphorothioic acid (WR-2721). (ucy.ac.cy)
  • Another method of the invention comprises administering a cell growth inhibitor to the subject and administering to the subject a chemotherapy agent. (justia.com)
  • 3,5] The additive/synergistic effect of sequential topoisomerase I and II inhibitor administration has been examined in vivo in several phase I and II human trials that explored their sequential administration. (cancernetwork.com)
  • New treatments and modulation of established treatment regimens ( i.e ., restoring sensitivity to chemotherapy) are therefore being sought. (aacrjournals.org)
  • Androgens are necessary for normal prostate cell growth (1) , and in animal models, androgen ablation causes cell atrophy and death of prostate epithelial cells (2) . (aacrjournals.org)
  • The method may further comprise administering to the subject a cell growth inhibitor. (justia.com)
  • Topoisomerase-inhibiting antineoplastic agents prevent cell growth and proliferation. (medscape.com)
  • Human topoisomerase 1B regulates the topological state of supercoiled DNA enabling all fundamental cell processes. (mdpi.com)
  • Many genes which were up-regulated by IL-1β and counter-regulated with the inhibitors had been discovered (Joos et al. (conferencedequebec.org)
  • In today's paper the consequences of different p38α/β inhibitors within the manifestation of selected genes are offered and the 511-28-4 IC50 potential relevance of this model 511-28-4 IC50 like a screening tool that specifically addresses OA-relevant processes is discussed. (conferencedequebec.org)
  • Two well-known examples for polyposis and HNPCC are familial adenomatous polyposis (FAP) and Lynch syndrome, respectively, in which occurs as a result of mutations in DNA repair genes ( Lynch and de la Chapelle, 2003 ). (frontiersin.org)
  • Breast tumors can be divided into subtypes using two parameters: (I) At the molecular level based on the protein expression of three receptors: estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER2) [ 2 ]. (biomedcentral.com)
  • In thisopen-label phase I study, irinotecan was administered IV at a fixeddose of 250 mg/m2 on day 1 in combination with capecitabine at a fixeddose of 1,500 mg/m2 for days 2 to 7 and epirubicin starting at a dose of40 mg/m2 and escalating by 10 mg/m2 in cohorts of three patients forthose with metastatic adenocarcinomas. (cancernetwork.com)
  • INT-747 is being tested as a monotherapy in a Phase 3 clinical trial and as a combination therapy with UDCA in a Phase 2 clinical trial for treating patients with PBC (ClinicalTrial.gov identifier: NCT01473524 and NCT00550862). (nature.com)
  • This has important clinical implications as, in contrast to advanced-stage NSCLC, chemotherapy can also be offered to patients with SCLC and a poor or bad performance status (World Health Organization performance status of 2-3), since a rapid amelioration of the patient's symptoms and general condition can be expected together with an improved outcome 7 . (ersjournals.com)