Search results for: Frances J. Sharom

Items from 1 to 20 out of 37 results

chapter

GPI-anchored Protein Cleavage in the Regulation of Transmembrane Signals

Frances J. Sharom, Galina Radeva

Subcellular Biochemistry > Membrane Dynamics and Domains > Regulation of Domain Formation > 285-315

The structure of covalently-linked glycosylphosphatidylinositol (GPI) anchors of membrane proteins displayed on the cell surface is described. Evidence of how the GPI-anchors are sorted into membrane rafts in the plasma membrane is reviewed. Proteins are released by hydrolysis of the linkage to the GPI anchor and phospholipases from different sources involved in this process are characterised. The...

article

Synthesis and evaluation of Strychnos alkaloids as MDR reversal agents for cancer cell eradication

Surendrachary Munagala, Gopal Sirasani, Praveen Kokkonda, Manali Phadke, more

Bioorganic & Medicinal Chemistry > 2014 > 22 > 3 > 1148-1155

Natural products represent the fourth generation of multidrug resistance (MDR) reversal agents that resensitize MDR cancer cells overexpressing P-glycoprotein (Pgp) to cytotoxic agents. We have developed an effective synthetic route to prepare various Strychnos alkaloids and their derivatives. Molecular modeling of these alkaloids docked to a homology model of Pgp was employed to optimize ligand–protein...

article

A semisynthetic taxane Yg-3-46a effectively evades P-glycoprotein and β-III tubulin mediated tumor drug resistance in vitro

Pei Cai, Peihua Lu, Frances J. Sharom, Wei-Shuo Fang

Cancer Letters > 2013 > 341 > 2 > 214-223

Tumor resistance, especially that mediated by P-glycoprotein (P-gp) and β-III tubulin, is a major obstacle to the efficacy of most microtubule-targeting anticancer drugs in clinics. A novel semisynthetic taxane, 2-debenzoyl-2-(3-azidobenzyl)-10-propionyldocetaxel (Yg-3-46a) was shown to be highly cytotoxic to breast cancer cell lines MCF-7 and MCF/ADR which overexpressed P-gp via long term culture...

article

9. Phenotypic variability in Mabry syndrome: Hyperphosphatasia with seizures and neurologic deficit

Miles D. Thompson, Frances J. Sharom, John A. Phillips, Peter N. Robinson, more

Clinical Neurophysiology > 2013 > 124 > 6 > e4

Hyperphosphatasia with neurologic deficit (Mabry syndrome) was first described in a single family (OMIM#239300) by Mabry et al. (1970). Although considered rare at the time, more than 20 individuals with the triad of developmental disability, seizures, and hyperphosphatasia have been identified world-wide. The 1–6 mannosyltransferase 2, phosphatidylinositol glycan V (PIGV) gene has been found to be...

article

Determining P-glycoprotein–drug interactions: Evaluation of reconstituted P-glycoprotein in a liposomal system and LLC-MDR1 polarized cell monolayers

Donald L. Melchior, Frances J. Sharom, Raymond Evers, George E. Wright, more

Journal of Pharmacological and Toxicological Methods > 2012 > 65 > 2 > 64-74

P-Glycoprotein (ABCB1, MDR1) is a multidrug efflux pump that is a member of the ATP-binding cassette (ABC) superfamily. Many drugs in common clinical use are either substrates or inhibitors of this transporter. Quantitative details of P-glycoprotein inhibition by pharmaceutical agents are essential for assessment of their pharmacokinetic behavior and prevention of negative patient reactions. Cell-based...

article

Fluorescent probe partitioning in GUVs of binary phospholipid mixtures: Implications for interpreting phase behavior

Janos Juhasz, James H. Davis, Frances J. Sharom

BBA - Biomembranes > 2012 > 1818 > 1 > 19-26

The phase behavior of membrane lipids is known to influence the organization and function of many integral proteins. Giant unilamellar vesicles (GUVs) provide a very useful model system in which to examine the details of lipid phase separation using fluorescence imaging. The visualization of domains in GUVs of binary and ternary lipid mixtures requires fluorescent probes with partitioning preference...

article

Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport

Xi Xiao, Ju Wu, Chiara Trigili, Hui Chen, more

Bioorganic & Medicinal Chemistry Letters > 2011 > 21 > 16 > 4852-4856

Some C-7 modified analogs of 3, a taxane with high affinity for binding to microtubules, were prepared through multistep transformations. Most of the analogs, bearing less lipophilic C-7 substituents than propionyl in 3, exhibited comparable binding affinities to microtubules but less cytotoxicity against drug-sensitive as well as multidrug-resistant tumor cells overexpressing P-glycoprotein. In addition,...

article

Transient Kinetics of Nucleotide Binding to the P-glycoprotein Multidrug Transporter

Miguel R. Lugo, Joseph W.K. Chu, Frances J. Sharom

Biophysical Journal > 2011 > 100 > 3 Supplement 1 > 549a

article

Differential interactions between statins and P‐glycoprotein: Implications for exploiting statins as anticancer agents

Carolyn A. Goard, Richard G. Mather, Balpreet Vinepal, James W. Clendening, more

International Journal of Cancer > 127 > 12 > 2936 - 2948

Statins, prescribed for decades to control cholesterol, have more recently been shown to have promising anticancer activity. Statins induce tumor‐selective apoptosis by inhibiting the mevalonate (MVA) pathway. In addition, we have recently demonstrated that lovastatin modulates drug accumulation in a MVA‐independent manner in multidrug‐resistant (MDR) tumor cells overexpressing the P‐glycoprotein...

article

Interaction of Bacterial PI-Specific Phospholipase C With Lipid Bilayer Surfaces

Ashley D. Parfitt, Frances J. Sharom

Biophysical Journal > 2010 > 98 > 3 Supplement 1 > 87a

article

Quantitative characterization of coexisting phases in DOPC/DPPC/cholesterol mixtures: Comparing confocal fluorescence microscopy and deuterium nuclear magnetic resonance

Janos Juhasz, Frances J. Sharom, James H. Davis

BBA - Biomembranes > 2009 > 1788 > 12 > 2541-2552

The differential miscibility of membrane lipids is thought to be the basis for the formation of dynamic microdomain assemblies in cell membranes known as membrane rafts. Because of their relevance to the existence of rafts, there has been much interest in recent years in model membrane systems that display coexisting liquid ordered (l _o ) and liquid disordered phases (l _d ), such as...

article

Interaction of LDS-751 with the drug-binding site of P-glycoprotein: A Trp fluorescence steady-state and lifetime study

Miguel R. Lugo, Frances J. Sharom

Archives of Biochemistry and Biophysics > 2009 > 492 > 1-2 > 17-28

P-glycoprotein (ABCB1) is an ATP-driven efflux pump which binds drugs within a large flexible binding pocket. Intrinsic Trp fluorescence was used to probe the interactions of LDS-751 (2-[4-(4-[dimethylamino]phenyl)-1,3-butadienyl]-3-ethylbenzo-thiazolium perchlorate) with purified P-glycoprotein, using steady-state/lifetime measurements and collisional quenching. The fast decay component of P-glycoprotein...

article

ABC Efflux Pump-Based Resistance to Chemotherapy Drugs

Paul D. W. Eckford, Frances J. Sharom

Chemical Reviews > 2009 > 109 > 7 > 2989 - 3011

article

Interaction of the P-Glycoprotein Multidrug Efflux Pump with Cholesterol: Effects on ATPase Activity, Drug Binding and Transport ^†

Paul D. W. Eckford, Frances J. Sharom

Biochemistry > 2008 > 47 > 51 > 13686 - 13698

article

Interaction of insecticides with mammalian P-glycoprotein and their effect on its transport function

K. Sreeramulu, Ronghua Liu, Frances J. Sharom

BBA - Biomembranes > 2007 > 1768 > 7 > 1750-1757

We studied the effects of four commonly used insecticides (methylparathion, endosulfan, cypermethrin and fenvalerate) on P-glycoprotein isolated from multidrug-resistant cells. All the pesticides stimulated P-glycoprotein ATPase activity, with maximum stimulation of up to 213% in a detergent-solubilized preparation, and up to 227% in reconstituted liposomes. The ATPase stimulation profiles were biphasic,...

article

Combined Chemical and Enzymatic Stable Isotope Labeling for Quantitative Profiling of Detergent-Insoluble Membrane Proteins Isolated Using Triton X-100 and Brij-96

Josip Blonder, Li-Rong Yu, Galina Radeva, King C. Chan, more

Journal of Proteome Research > 2006 > 5 > 2 > 349 - 360

article

Interaction of LDS-751 and Rhodamine 123 with P-Glycoprotein: Evidence for Simultaneous Binding of Both Drugs ^†

Miguel R. Lugo, Frances J. Sharom

Biochemistry > 2005 > 44 > 42 > 14020 - 14029

article

Time-Resolved Fluorescence Resonance Energy Transfer Shows that the Bacterial Multidrug ABC Half-Transporter BmrA Functions as a Homodimer ^†

Olivier Dalmas, Marie-Ange Do Cao, Miguel R. Lugo, Frances J. Sharom, more

Biochemistry > 2005 > 44 > 11 > 4312 - 4321

article

Interaction of LDS-751 with P-Glycoprotein and Mapping of the Location of the R Drug Binding Site ^†

Miguel R. Lugo, Frances J. Sharom

Biochemistry > 2005 > 44 > 2 > 643 - 655

article

New Insights into the Drug Binding, Transport and Lipid Flippase Activities of the P-Glycoprotein Multidrug Transporter

Frances J. Sharom, Miguel R. Lugo, Paul D. W. Eckford

Journal of Bioenergetics and Biomembranes > 2005 > 37 > 6 > 481-487

The MDR1 P-glycoprotein, an ATP-binding cassette (ABC) superfamily member that functions as an ATP-driven drug efflux pump, has been linked to resistance of human tumors to multiple chemotherapeutic agents. P-glycoprotein binds and actively transports a large variety of hydrophobic drugs and peptides. P-glycoprotein in reconstituted proteoliposomes is also an outwardly directed flippase for membrane...

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Search results for: Frances J. Sharom

GPI-anchored Protein Cleavage in the Regulation of Transmembrane Signals

Synthesis and evaluation of Strychnos alkaloids as MDR reversal agents for cancer cell eradication

A semisynthetic taxane Yg-3-46a effectively evades P-glycoprotein and β-III tubulin mediated tumor drug resistance in vitro

9. Phenotypic variability in Mabry syndrome: Hyperphosphatasia with seizures and neurologic deficit

Determining P-glycoprotein–drug interactions: Evaluation of reconstituted P-glycoprotein in a liposomal system and LLC-MDR1 polarized cell monolayers

Fluorescent probe partitioning in GUVs of binary phospholipid mixtures: Implications for interpreting phase behavior

Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport

Transient Kinetics of Nucleotide Binding to the P-glycoprotein Multidrug Transporter

Differential interactions between statins and P‐glycoprotein: Implications for exploiting statins as anticancer agents

Interaction of Bacterial PI-Specific Phospholipase C With Lipid Bilayer Surfaces

Quantitative characterization of coexisting phases in DOPC/DPPC/cholesterol mixtures: Comparing confocal fluorescence microscopy and deuterium nuclear magnetic resonance

Interaction of LDS-751 with the drug-binding site of P-glycoprotein: A Trp fluorescence steady-state and lifetime study

ABC Efflux Pump-Based Resistance to Chemotherapy Drugs

Interaction of the P-Glycoprotein Multidrug Efflux Pump with Cholesterol: Effects on ATPase Activity, Drug Binding and Transport ^†

Interaction of insecticides with mammalian P-glycoprotein and their effect on its transport function

Combined Chemical and Enzymatic Stable Isotope Labeling for Quantitative Profiling of Detergent-Insoluble Membrane Proteins Isolated Using Triton X-100 and Brij-96

Interaction of LDS-751 and Rhodamine 123 with P-Glycoprotein: Evidence for Simultaneous Binding of Both Drugs ^†

Time-Resolved Fluorescence Resonance Energy Transfer Shows that the Bacterial Multidrug ABC Half-Transporter BmrA Functions as a Homodimer ^†

Interaction of LDS-751 with P-Glycoprotein and Mapping of the Location of the R Drug Binding Site ^†

New Insights into the Drug Binding, Transport and Lipid Flippase Activities of the P-Glycoprotein Multidrug Transporter

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