Showing papers in "Biochemical Pharmacology in 2012"

TL;DR: The development of multidrug-loaded nanoparticles against drug resistant cancers and the recent advances in nanoparticle-based combination strategies against clinical cancer drug resistance are highlighted, including co-encapsulation of drugs with different physicochemical properties, ratiometric control over drug loading, and temporal sequencing on drug release.

TL;DR: Quercetin can be considered the prototype of a naturally-occurring chemopreventive agent because of its key roles in triggering the "hallmarks of cancer" and several critical points must be taken into account when considering the potential therapeutic use of this molecule.

TL;DR: Although much of the focus has been on PARP1 in DNA repair, recent advances highlight the emergence of other DNA-dependent PARPs (i.e. PARP2, PARP3 and possibly Tankyrase) in this process.

TL;DR: The anti-oxidant/anti-inflammatory and anticancer effects of thymoquinone are summarized with a focus on its molecular targets, and its possible role in the treatment of inflammatory diseases and cancer.

TL;DR: An overview of the current state of the science in the burgeoning field of exosome biology is provided to provide an overview of how exosomes have been implicated in the spread of neurodegenerative diseases.

TL;DR: Evidence is mounting that many cancers display subpopulations of stem cells that are responsible for tumor self-renewal, and stem cells frequently manifest the "side population" phenotype characterized by expression of BCRP and other ABC transporters, which may contribute to the inherent resistance of these neoplasms and their failure to be cured.

TL;DR: Mechanisms of NADPH oxidase/ROS in the expression of inflammatory target proteins involved in airway and lung diseases are discussed.

TL;DR: Apremilast is an orally available targeted PDE4 inhibitor that modulates a wide array of inflammatory mediators involved in psoriasis and psoriatic arthritis, including decreases in the expression of inducible nitric oxide synthase, TNF-α, and interleukin (IL)-23 and increases IL-10.

TL;DR: A growing body of reports supports the evidence that berberine has anticancer effects, being able to block the proliferation of and to kill cancer cells.

TL;DR: It is believed that the future development of low-toxicity, small-molecule CRM1 inhibitors may provide a new approach to treating cancer.

TL;DR: The role of NQO1 in the sensitivity and resistance of human cancers to the quinone antitumor drugs mitomycin C, β-lapachone and the benzoquinone ansamycin class of Hsp90 inhibitors including 17-AAG is discussed.

TL;DR: This review focuses on the role of SB in OA pathogenesis, describing relevant underlying mechanisms involved in the process and examining the potential activity as disease-modifying anti-osteoarthritic drugs (DMOADs) of certain SB-targeting agents currently under study.

TL;DR: PXR/CAR expression levels and/or activation statuses may predict prognosis and identify the risk of drug resistance in patients subjected to chemotherapy, and PXR-CAR antagonists, when used in combination with existing chemotherapeutics that activate PXr/CAR, are feasible and promising options that could be utilized to overcome or, at least, attenuate MDR in cancer cells.

TL;DR: This review provides a decisive insight on the molecular basis of the health-promoting potential of Withaferin A.

TL;DR: The data demonstrate that ROT can induce autophagy which leads to cell death in pancreatic CSCs and that gene silencing of Atg7 and Beclin1, or cotreatment of the autophagosome inhibitor, 3-methyladenine, inhibited ROT-inducedAutophagy and accelerated Rottlerin-induced apoptosis.

TL;DR: Insight is provided into the beneficial role of metformin as a novel therapeutic drug for chronic asthma by reducing both airway inflammation and remodeling at least partially through the induction of AMPK activation and decreased oxidative stress.

TL;DR: Advances in the understanding of the mechanisms of drug resistance and patient selection based on biomarker profiles will be crucial to adapt therapeutic strategies and improve outcomes for patients with primary malignant brain tumors.

TL;DR: Berberine-induced AMPK activation inhibits the metastatic potential of tumor cells through a reduction in the activity of the ERK signaling pathway and COX-2 protein levels and a decrease in ERK activity and protein levels of cyclooxygenase-2 by a berberine -induced AM PK activation.

TL;DR: It is demonstrated that fisetin acts as a dual inhibitor of the PI3K/Akt and the mTOR pathways, which is a significant finding considering the fact that mTOR is phosphorylated and its activation is more frequent in tumors with overexpression of PI3 kAkt.

TL;DR: The activation of renal NLRP3 inflammasome may play an important role in the link among renal inflammation, JAK2/STAT3/PAPR-α and IR/IRS1/Akt/ERK1/2 signaling impairment, and lipid accumulation driven by fructose.

TL;DR: Evidence is provided that miR-139 might function as a metastasis suppressor in CRC by targeting type I insulin-like growth factor receptor (IGF-IR) and directing migration inactivation of CRC cells involves down-regulation of matrix metalloproteinase 2 (MMP-2).

TL;DR: Several viral proteins, such as the viral 3C protease, the putative 2C helicase and the 3D RNA-dependent RNA polymerase may be/are excellent targets for inhibition of viral replication.

TL;DR: The present study indicates that further work examining the physiological effects of synthetic cannabinoid metabolism is warranted, and suggests that a complex mix of metabolically produced CB1R ligands may contribute to the adverse effect profile of JWH-073-containing products.

TL;DR: The emerging interest for HDAC6-selective inhibitors is related to the modulation of acetylation of nonhistone regulatory proteins implicated in cancer-relevant processes, including cell migration, metastasis, angiogenesis and stress-response pathways.

TL;DR: An experimental strategy is described to biochemically characterize the pharmacological induction of CREB phosphorylation as a mechanistic marker across different pharmacological classes of compounds for the potential treatment of AD that include: α7 nicotinic agonists, H3 antagonists and 11β HSD1 inhibitors.

TL;DR: Combined ET(A)R/ET(B)R antagonists could be more efficacious in the management of conditions involving upregulation of ET( a)R and ET(b)R in VSM, and the role of alterations in endothelial ET(B).

TL;DR: This review summarizes the data based on various in vitro and in vivo studies related to the effects of zerumbone on numerous pivotal molecular targets in cancer and its reported chemopreventive/therapeutic effects in different models of cancer.

TL;DR: An important endogenous molecule that has the potential to interact in complex and elegant ways with its host environment and foreign organisms, SCN's diverse properties as both host defense and antioxidant agent make it a potentially useful therapeutic.

TL;DR: Buspirone has been identified as a viable candidate for clinical trials and will provide a better understanding of the role D3R plays in addiction and whether or not antagonists or partial agonists that are D 3R selective are effective in achieving abstinence in this patient population.

TL;DR: This commentary will provide a review of the JAK kinase field as it pertains to small molecule inhibition for the treatment of cancer and autoimmune diseases with an emphasis on JAK2.