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modulators of sensitivity and resistance to inhibition of

modulators of sensitivity and resistance to inhibition of

modulators of sensitivity and resistance to inhibition of

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Modulators of Sensitivity and Resistance to Inhibition of ...These results demonstrate that OGT and DDN are novel in vitro regulators of cellular response to inhibition of PI3K signaling and highlight their potential roles as additional predictive biomarkers for de novo resistance to GDC-0941 and other PI3K inhibitors. We also found that GDC-0941 has broad anti-proliferative activity amongst the nine tumor types represented in the NCI-60 cell panel, suggesting its …Cited by: 37Publish Year: 2012Author: Kevin A. Kwei, Joffre B. Baker, Robert J. Pelham

Response and resistance to BET bromodomain inhibitors in modulators of sensitivity and resistance to inhibition of

Jan 06, 2016 · BET inhibitors that target bromodomain chromatin readers such as BRD4 are being explored as potential therapeutics in cancer; here triple-negative breast cancer cell lines are shown to Resistance-Modifying Agents. 11. Pyrimido[5,4-d]pyrimidine modulators of sensitivity and resistance to inhibition ofThe cardiovascular and antithrombotic agent dipyridamole (DP) has potential therapeutic utility as a modulator of the activity of antimetabolite antitumor agents by virtue of its inhibition of nucleoside transport. However, the activity of DP can be compromised by binding to the acute phase serum protein, 1-acid glycoprotein (AGP).Research Article Identication of phosphatase 2A-like caffeine sensitivity of rts3, but not that of sds23/24 or hse1 strains, to inhibition of the TORC1 kinase complex, a central regulator of cell growth and a known caffeine target. Epistasis experiments support a model in which Rts3 and Sds23/24 act in parallel to negatively regulate Sit4, while Hse1 confers caffeine resistance via a separate pathway.

PARP inhibitors in ovarian cancer: Sensitivity prediction modulators of sensitivity and resistance to inhibition of

Jan 22, 2019 · The deletion of PARP1 has been demonstrated to cause resistance to all PARP inhibitors in ovarian cancer cell lines in vitro. 103 The PARP1 expression level is positively correlated with PARP inhibitor sensitivity. 104 For example, an acquired low expression level of PARP1 is a potential cause of resistance to PARP inhibitors in PDX models. 103 Furthermore, cells with PARP1 mutations were 100fold more resistant to PARP inhibitors PARP inhibitor resistance: the underlying mechanisms and modulators of sensitivity and resistance to inhibition ofJun 20, 2020 · In this review, we reviewed the underlying mechanisms of PARP inhibitor resistance in detail and summarized the potential strategies to overcome PARPi resistance and increase PARPi sensitivity. Due to the DNA repair defect, BRCA1/2 deficient tumor cells are more sensitive to PARP inhibitors (PARPi) through the mechanism of synthetic lethality.Overcoming Platinum and PARP-Inhibitor Resistance in modulators of sensitivity and resistance to inhibition ofPlatinum chemotherapy remains the cornerstone of treatment for epithelial ovarian cancer (OC) and Poly (ADP-ribose) polymerase inhibitors (PARPi) now have an established role as maintenance therapy. The mechanisms of action of these agents is, in many ways, complementary, and crucially reliant on the intracellular DNA Damage Repair (DDR) response. Here, we review mechanisms of primary and modulators of sensitivity and resistance to inhibition of

Modulators of sensitivity and resistance to inhibition of modulators of sensitivity and resistance to inhibition of

Modulators of sensitivity and resistance to inhibition of PI3K identified in a pharmacogenomic screen of the NCI-60 human tumor cell line collection. PLoS One. 2012; 7(9):e46518 (ISSN: 1932-6203) Kwei KA; Baker JB; Pelham RJModulators of Sensitivity and Resistance to Inhibition of modulators of sensitivity and resistance to inhibition ofThese results demonstrate that OGT and DDN are novel in vitro regulators of cellular response to inhibition of PI3K signaling and highlight their potential roles as additional predictive biomarkers for de novo resistance to GDC-0941 and other PI3K inhibitors. We also found that GDC-0941 has broad anti-proliferative activity amongst the nine tumor types represented in the NCI-60 cell panel, suggesting its Cited by: 37Publish Year: 2012Author: Kevin A. Kwei, Joffre B. Baker, Robert J. PelhamModulators of Sensitivity and Resistance to Inhibition of modulators of sensitivity and resistance to inhibition ofSep 01, 2012 · Modulators of Sensitivity and Resistance to Inhibition of PI3K Identified in a Pharmacogenomic Screen of the NCI-60 Human Tumor Cell Line Cited by: 37Publish Year: 2012Author: Kevin A. Kwei, Joffre B. Baker, Robert J. Pelham

Modulators of Sensitivity and Resistance to Inhibition of modulators of sensitivity and resistance to inhibition of

Citation: Kwei KA, Baker JB, Pelham RJ (2012) Modulators of Sensitivity and Resistance to Inhibition of PI3K Identified in a Pharmacogenomic Screen of the NCI-60 Human Tumor Cell Line Collection.Mechanisms of stearoyl CoA desaturase inhibitor modulators of sensitivity and resistance to inhibition ofThe lipogenic enzyme stearoyl CoA desaturase (SCD) plays a key role in tumor lipid metabolism and membrane architecture. SCD is often up-regulated and a therapeutic target in cancer. Here, we report the unexpected finding that median expression of SCD is low in glioblastoma relative to normal brain due to hypermethylation and unintentional monoallelic co-deletion with phosphatase and tensin modulators of sensitivity and resistance to inhibition ofMechanisms of resistance to selective RET tyrosine kinase modulators of sensitivity and resistance to inhibition ofDec 01, 2020 · MET amplification is an established mechanism of resistance to EGFR inhibitors in EGFR-mutant NSCLC and has been identified in up to 20% of EGFR TKI-resistant biopsies.23, 24, 25 Notably, a combination of EGFR and MET inhibitors, such as osimertinib plus savolitinib or osimertinib plus capmatinib, is able to effectively overcome this MET-driven resistance in clinic. 33, 34 Similarly, MET amplification can mediate resistance to next-generation ALK inhibitors

Mechanisms of Sensitivity and Resistance to CDK4/6 Inhibition

Apr 13, 2020 · Here, through an integrative analysis of sensitivity and resistance mechanisms, we discuss the use of CDK4/6 inhibitors in combination with available targeted therapies, immunotherapy, or classical chemotherapy with the aim of improving future therapeutic uses of CDK4/6 inhibition in a variety of cancers.MRP1 modulators synergize with buthionine sulfoximine to modulators of sensitivity and resistance to inhibition ofMembers of the ABC transporter family, particularly P-glycoprotein (P-gp, ABCB1), breast cancer resistance protein (BCRP, ABCG2) and multidrug resistance protein 1 (MRP1, ABCC1) are well characterized mediators of multidrug resistance, however their pharmacological inhibition has so Loss of TRIM33 causes resistance to BET bromodomain modulators of sensitivity and resistance to inhibition ofAug 02, 2016 · Inhibitors of bromodomain and extraterminal domain family proteins (BETi) have generated considerable excitement and are in clinical trials for treatment of several cancers. Cancers treated with targeted therapies eventually become resistant, yet molecular mechanisms underlying resistance to BETi are poorly understood. To discover novel molecular mechanisms mediating resistance

Irreversible inhibitors of the EGF receptor may circumvent modulators of sensitivity and resistance to inhibition of

May 24, 2005 · Non-small cell lung cancers (NSCLCs) with activating mutations in the kinase domain of the epidermal growth factor receptor (EGFR) demonstrate dramatic, but transient, responses to the reversible tyrosine kinase inhibitors gefitinib (Iressa) and erlotinib (Tarceva). Some recurrent tumors have a common secondary mutation in the EGFR kinase domain, T790M, conferring drug resistance, Immunization with mannosylated nanovaccines and Immunization with mannosylated nanovaccines and inhibition of the immune-suppressing microenvironment sensitizes melanoma to immune checkpoint modulators A low response rate, acquired resistance and severe side effects have limited the clinical outcomes of immune checkpoint therapy.Genetic screening for single-cell variability modulators modulators of sensitivity and resistance to inhibition ofJan 04, 2021 · A genetic screen designed to capture modulators of single-cell state variability identifies a new mode of altering resistance to BRAF inhibition in melanoma that pushes cells toward a more modulators of sensitivity and resistance to inhibition of

Genetic and Non-Genetic Mechanisms of Resistance to BCR modulators of sensitivity and resistance to inhibition of

Oct 26, 2020 · Figure 1 The genetic and non-genetic mechanisms of resistance to BTK or PI3K inhibition in B cell malignancies. The * indicates genetic mechanisms of resistance to ibrutinib (BTK inhibitor), the red arrows indicate non-genetic mechanisms of resistance/adaptation to ibrutinib, the blue arrows indicate mechanisms of resistance/adaptation to idelalisib (PI3K inhibitor), and the green Genetic Modulators of Niclosamide Sensitivity and modulators of sensitivity and resistance to inhibition ofIntroductionAcute myeloid leukemia (AML) is a malignancy of myeloid progenitor cells that leads to the accumulation of immature blasts in the blood and bone marAuthor: Anna Wojcicki, Hee-Don Chae, Kyuho Han, Minyoung Youn, Mark C Wilkes, Norman J. Lacayo, Michael Bass modulators of sensitivity and resistance to inhibition ofPublish Year: 2020Functional genomics identifies predictive markers and modulators of sensitivity and resistance to inhibition ofJul 22, 2019 · CDK4/6 inhibitors are a promising treatment strategy in tumor therapy but are hampered by resistance mechanisms. This study was performed to reveal predictive markers, mechanisms of resistance and to develop rational combination therapies for a personalized therapy approach in bladder cancer. A genome-scale CRISPR-dCas9 activation screen for resistance to the CDK4/6 inhibitor

Dual MET and SMO Negative Modulators Overcome

Tyrosine kinase inhibitors (TKIs) of the EGF receptor (EGFR) have provided a significant improvement in the disease outcome of nonsmall cell lung cancer (NSCLC). Unfortunately, resistance to these agents frequently occurs, and it is often related to the activation of the Hedgehog (Hh) and MET signaling cascades driving the epithelial-to-mesenchymal transition (EMT). Because the concomitant modulators of sensitivity and resistance to inhibition ofCited by: 14Publish Year: 2017Author: Floriana Morgillo, Giorgio Amendola, Carminia Maria Della Corte, Chiara Giacomelli, Lorenzo Botta, S modulators of sensitivity and resistance to inhibition ofDual MET and SMO Negative Modulators Overcome Sep 14, 2017 · Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. Morgillo F (1), Amendola G (2), Della Corte CM (1), Giacomelli C (3), Botta L (4), Di Maro S (2), Messere A (2), Ciaramella V (1), Taliani S (3), Marinelli L (4), Trincavelli ML (3), Martini C (3), Novellino E (4), Ciardiello F (1), Cosconati S (2).Cited by: 14Publish Year: 2017Author: Floriana Morgillo, Giorgio Amendola, Carminia Maria Della Corte, Chiara Giacomelli, Lorenzo Botta, S modulators of sensitivity and resistance to inhibition ofDiscovering Natural Product Modulators to Overcome modulators of sensitivity and resistance to inhibition ofTitle: Discovering Natural Product Modulators to Overcome Multidrug Resistance in Cancer Chemotherapy VOLUME: 12 ISSUE: 4 Author(s):Chung-Pu Wu, Shinobu Ohnuma and Suresh V. Ambudkar Affiliation:Laboratory of Cell Biology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA. Keywords:ATP-binding cassette transporters, bioavailability, chemotherapy, modulators modulators of sensitivity and resistance to inhibition ofCited by: 159Publish Year: 2011Author: Chung-Pu Wu, Shinobu Ohnuma, Suresh V. Ambudkar

Discovering Natural Product Modulators to Overcome modulators of sensitivity and resistance to inhibition of

Title: Discovering Natural Product Modulators to Overcome Multidrug Resistance in Cancer Chemotherapy VOLUME: 12 ISSUE: 4 Author(s):Chung-Pu Wu, Shinobu Ohnuma and Suresh V. Ambudkar Affiliation:Laboratory of Cell Biology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA. Keywords:ATP-binding cassette transporters, bioavailability, chemotherapy, modulators modulators of sensitivity and resistance to inhibition ofCDK12-Specific Modulators and Methods for the CDK12-Specific Modulators and Methods for the Treatment of Cancer INVENTION: Investigators at Salk have identified a novel protein that binds to the cyclin-dependent kinase CDK12 in a specific manner. This binding partner provides an effective and selective inhibition of CDK12 kinase activity.Activity of fungicides and modulators of membrane drug modulators of sensitivity and resistance to inhibition ofDec 19, 2012 · MDR3 strains combined the overexpression of both transporters and exhibited the widest spectrum of cross resistance and the highest resistance levels. The four transport modulators, amitriptyline, chlorpromazine, diethylstilbestrol, and verapamil, known to affect some ABC transporters, were tested in B. cinerea. In our experimental conditions, the activity of several fungicides was only

A MicroRNA Screen to Identify Modulators of Sensitivity to modulators of sensitivity and resistance to inhibition of

Nov 01, 2010 · miRNAs could modulate sensitivity to ABT-263 through several mechanisms: by directly targeting the MCL1 gene 3-UTR and repressing protein translation or by targeting other genes involved in regulating MCL1 expression or function. In addition, some miRNAs may modulate ABT-263 sensitivity in an MCL1-independent fashion.Cited by: 69Publish Year: 2010Author: Lloyd T Lam, Xin Lu, Haichao Zhang, Richard R Lesniewski, Saul H Rosenberg, Dimitri Semizarov(PDF) Modulators of Sensitivity and Resistance to modulators of sensitivity and resistance to inhibition ofModulators of Sensitivity and Resistance to Inhibition of PI3K Identified in a Pharmacogenomic Screen of the NCI-60 Human Tumor Cell Line Coll ection.pdf Content available from CC BY 4.0:

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