Open Access. Powered by Scholars. Published by Universities.®

Cell Biology Commons

Open Access. Powered by Scholars. Published by Universities.®

Articles 1 - 5 of 5

Full-Text Articles in Cell Biology

Reversal Of P-Glycoprotein And Breast Cancer Resistance Protein Mediated Multidrug Resistance In Vitro Using In Silico Identified Novel Compounds, Amila Nanayakkara May 2019

Reversal Of P-Glycoprotein And Breast Cancer Resistance Protein Mediated Multidrug Resistance In Vitro Using In Silico Identified Novel Compounds, Amila Nanayakkara

Biological Sciences Theses and Dissertations

Multidrug resistance (MDR) is a major cause of chemotherapy failure. Overexpression of ATP-binding cassette (ABC) transporters, P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) are two well-studied drug transporters which are associated with MDR. These two transporters also act as a major functional unit of the blood brain barrier to protect the brain from xenobiotics and toxins. Lack of clinically approved P-gp and BCRP inhibitors renders chemotherapy treatments of many MDR cancers ineffective and obstructs drug uptake into the brain.

Using computational methods, we have identified new compounds that inhibit P-gp (Brewer et al., Mol. Pharmacol. 2014). Several of these ...


Modelling Β2ar Regulation, Sharat J. Vayttaden Dec 2011

Modelling Β2ar Regulation, Sharat J. Vayttaden

UT GSBS Dissertations and Theses (Open Access)

The β2 adrenergic receptor (β2AR) regulates smooth muscle relaxation in the vasculature and airways. Long- and Short-acting β-agonists (LABAs/SABAs) are widely used in treatment of chronic obstructive pulmonary disorder (COPD) and asthma. Despite their widespread clinical use we do not understand well the dominant β2AR regulatory pathways that are stimulated during therapy and bring about tachyphylaxis, which is the loss of drug effects. Thus, an understanding of how the β2AR responds to various β-agonists is crucial to their rational use. Towards that end we have developed deterministic models that explore the mechanism of drug- induced β2AR regulation. These mathematical ...


Mechanisms Of Somatostatin-Induced Paradoxical Increase In Insulin Secretion In The Presence Of Arginine Vasopressin In Clonal [Beta]-Cell Hit-T15 , Henrique Cheng Jan 2002

Mechanisms Of Somatostatin-Induced Paradoxical Increase In Insulin Secretion In The Presence Of Arginine Vasopressin In Clonal [Beta]-Cell Hit-T15 , Henrique Cheng

Retrospective Theses and Dissertations

We investigated the mechanism underlying somatostatin-induced increase in [Ca2+]i leading to insulin release in the presence of arginine vasopressin (AVP) in clonal beta-cell HIT-T15. Somatostatin increased [Ca2+]i and insulin release in a biphasic pattern, characterized by a sharp and transient increase followed by a rapid decline to the sub-basal level. Pretreatment with pertussis toxin, which inactivates Gi/Go, abolished the effects of somatostatin. U-73122, an inhibitor of phospholipase C, antagonized somatostatin-induced increase in [Ca2+] i. In Ca2+-free environment, somatostatin still increased [Ca2+]i, whereas depletion of intracellular Ca 2+ stores with thapsigargin, a microsomal Ca2+ ATPase inhibitor ...


Comparison Of Beta-Adrenoceptor Coupled Camp Production In Cultured Human Mononuclear Leukocytes And Myometrial Cells, Yu-Li Liu Dec 1997

Comparison Of Beta-Adrenoceptor Coupled Camp Production In Cultured Human Mononuclear Leukocytes And Myometrial Cells, Yu-Li Liu

Electronic Theses and Dissertations

$\beta\sb2$-Adrenoceptor ($\beta\sb2$-AR) agonists, such as terbutaline, are used as tocolytic agents in the treatment of preterm labor. $\beta$-Adrenoceptor stimulation relaxes myometrium through specific receptors coupled through Gs to adenylyl cyclase (AC) that catalyzes the conversion of ATP to cAMP. The purpose of this study was to compare $\beta$-adrenoceptors and cAMP production in cultured human leukocytes and myometrial cells, and to determine the importance of $\beta$-adrenoceptors and cAMP production in isoproterenol-induced myometrial relaxation. $\sp{125}$I-iodopindolol was used to assess $\beta$-adrenoceptor affinity and number cAMP levels were analyzed before and after stimulation by ...


Utilization Of Fatigued And Non-Fatigued Isolated Guinea-Pig Papillary Muscles And Ventricular Myocytes On The Comparison Of Inotropic, Chronotropic And Intracellular Calcium Changes Induced By Monensin And Digoxin , Ismail Meral Jan 1996

Utilization Of Fatigued And Non-Fatigued Isolated Guinea-Pig Papillary Muscles And Ventricular Myocytes On The Comparison Of Inotropic, Chronotropic And Intracellular Calcium Changes Induced By Monensin And Digoxin , Ismail Meral

Retrospective Theses and Dissertations

Experiment 1. We investigated the effects of monensin and digoxin on contraction force (CF), initial contraction velocity (ICV), average contraction velocity (ACV), initial relaxation velocity (IRV) and stimulus to response time (ST) change in fatigued (defined as the level at which papillary muscle contraction had lost 30% of its original contraction force with the elapse of time) and non-fatigued guinea-pig papillary muscles. The five hours of measurement in Experiment 3 were divided into five periods (T0 was equilibration, T1, T2, T3, and T4 were respectively one, two, three, and four hours after drug administration). We found that both monensin and ...