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Expert Opinion on Therapeutic Targets

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https://www.readbyqxmd.com/read/28333549/ksr-as-a-therapeutic-target-for-ras-dependent-cancers
#1
Beth K Neilsen, Danielle E Frodyma, Robert E Lewis, Kurt W Fisher
Targeting downstream effectors required for oncogenic Ras signaling is a potential alternative or complement to the development of more direct approaches targeting Ras in the treatment of Ras-dependent cancers. Areas covered: Here we review literature pertaining to the molecular scaffold Kinase Suppressor of Ras (KSR) and its role in promoting signals critical to tumor maintenance. We summarize the phenotypes in knockout models, describe the role of KSR in cancer, and outline the structure and function of the KSR1 and KSR2 proteins...
March 23, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28332852/corrigendum
#2
(no author information available yet)
No abstract text is available yet for this article.
March 23, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28326864/role-of-the-notch-signaling-in-cholangiocarcinoma
#3
Antonio Cigliano, Jingxiao Wang, Xin Chen, Diego F Calvisi
Cholangiocarcinoma (CCA) is an emerging cancer entity of the liver, associated with poor outcome and characterized by resistance to conventional chemotherapeutic treatments. In the last decade, many signaling pathways associated with CCA development and progression have been identified and are currently under intense investigation. Cumulating evidence indicates that the Notch cascade, a highly-conserved pathway in most multicellular organisms, is a critical player both in liver malignant transformation and tumor aggressiveness, thus representing a potential therapeutic target in this pernicious disease...
March 22, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28323497/potential-mechanisms-underlying-cdk5-related-osteosarcoma-progression
#4
Hang-Xing Bao, Qing Bi, Yong Han, Chen Zhao, Hai Zou
OBJECTIVES: Identification of new prognostic biomarkers and therapeutic targets is of crucial importance for patients with osteosarcoma. Cyclin-dependent kinase 5 (CDK5) is overexpressed in several tumor types. However, the exact role CDK5 plays in osteosarcoma is still unknown. METHODS: In this study, we explored the association between CDK5 expression and the prognosis of osteosarcoma patients using publicly available gene expression datasets. Potential molecular mechanisms underlying its pro-malignant role in cancer progression were also discussed...
March 21, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28317405/corrigendum
#5
(no author information available yet)
No abstract text is available yet for this article.
March 20, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28292200/therapeutic-effects-of-methionine-sulfoximine-in-multiple-diseases-include-and-extend-beyond-inhibition-of-glutamine-synthetase
#6
William S A Brusilow, Tyler J Peters
Methionine sulfoximine (MSO), a well-characterized inhibitor of glutamine synthetase, displays significant therapeutic benefits in animal models for several human diseases. This amino acid might therefore be a viable candidate for drug development to treat diseases for which there are few effective therapies. Areas covered: We describe the effects of MSO on brain swelling occurring in overt hepatic encephalopathy resulting from liver failure, the effects of MSO on excitotoxic damage involved in amyotrophic lateral sclerosis (ALS) or resulting from stroke, and the effects of MSO on a model for an inflammatory immune response involved in a range of diseases...
March 15, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28282502/signaling-pathways-as-therapeutic-targets-in-biliary-tract-cancer
#7
Jennifer Yang, Matthew R Farren, Daniel Ahn, Tanios Bekaii-Saab, Gregory B Lesinski
The incidence of biliary tract cancer (BTC) is increasing, and the disease is frequently diagnosed during advanced stages, leading to poor overall survival. Limited treatment options are currently available and novel therapeutic approaches are needed. A number of completed clinical trials have evaluated the role of chemotherapy for BTC, demonstrating a marginal benefit. Thus, there is increased interest in applying targeted therapies for this disease. Areas Covered: This review article summarizes the role of chemotherapeutic regimens for the treatment of BTC, and highlights key signal transduction pathways of interest for targeted inhibition...
March 10, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28127991/tshr-as-a-therapeutic-target-in-graves-disease
#8
Terry J Smith
Graves' disease (GD) and thyroid-associated ophthalmopathy (TAO) are thought to result from actions of pathogenic antibodies mediated through the thyrotropin receptor (TSHR). This leads to the unregulated consequences of the antibody-mediated receptor activity in the thyroid and connective tissues of the orbit. Recent studies reveal antibodies that appear to be directed against the insulin-like growth factor-I receptor (IGF-IR). Areas covered: In this brief article, I attempt to review the fundamental characteristics of the TSHR, its role in GD and TAO, and its relationship to IGF-IR...
February 6, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28127990/animal-models-suggest-the-trip8b-hcn-interaction-is-a-therapeutic-target-for-major-depressive-disorder
#9
Kyle A Lyman, Ye Han, Dane M Chetkovich
No abstract text is available yet for this article.
January 27, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28081641/vessel-pruning-or-healing-endothelial-metabolism-as-a-novel-target
#10
Anna Rita Cantelmo, Andreas Pircher, Joanna Kalucka, Peter Carmeliet
Antiangiogenic drugs were originally designed to starve tumors by cutting off their vascular supply. Unfortunately, when these agents are used as monotherapy or in combination with chemotherapy, they provide only modest survival benefits in the order of weeks to months in most cancer patients. Strategies normalizing the disorganized tumor vasculature offer the potential to increase tumor perfusion and oxygenation, and to improve the efficacy of radio-, chemo- and immunotherapy, while reducing metastasis. Areas covered: This review discusses tumor vascular normalization (TVN) as an alternative strategy for anti-angiogenic cancer treatment...
January 27, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28092722/synthetic-and-natural-peroxisome-proliferator-activated-receptor-ppar-agonists-as-candidates-for-the-therapy-of-the-metabolic-syndrome
#11
Chek Kun Tan, Yan Zhuang, Walter Wahli
Peroxisome proliferator-activated receptors (PPARs) are the molecular targets of hypolipidemic and insulin-sensitizing drugs and implicated in a multitude of processes that fine-tune the functions of all organs in vertebrates. As transcription factors they sense endogenous and exogenous lipid signaling molecules and convert these signals into intricate gene responses that impact health and disease. The PPARs act as modulators of cellular, organ, and systemic processes, such as lipid and carbohydrate metabolism, making them valuable for understanding body homeostasis influenced by nutrition and exercise...
January 25, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28076698/emerging-role-of-setdb1-as-a-therapeutic-target
#12
Archana Venkataramana Karanth, Radhika Radha Maniswami, Seema Prashanth, Hemalatha Govindaraj, Ramya Padmavathy, Sooriya Kumar Jegatheesan, Ramesh Mullangi, Sriram Rajagopal
Epigenetic changes lead to aberrant gene expression in cancer. SETDB1, a histone lysine methyltransferase plays an important role in methylation and gene silencing. Aberrant histone methylation at H3K9 by SETDB1 promotes silencing of tumor suppressor genes and thus contributes to carcinogenesis. Recent studies indicate that SETDB1 is abnormally expressed in various human cancer conditions which contributed to enhanced tumor growth and metastasis. Hence, SETDB1 appears to be a promising epigenetic target for therapeutic intervention...
January 20, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28081644/reactive-nitrogen-species-as-therapeutic-targets-for-autophagy-implication-for-ischemic-stroke
#13
Jinghan Feng, Xingmiao Chen, Jiangang Shen
Roles of autophagy/mitophagy activation in ischemic stroke remain controversial. To elucidate potential reasons, we analyze the factors responsible for divergent results in literatures. Reactive nitrogen species (RNS) are important cytotoxic factors in ischemic stroke. Herein, we particularly discuss the roles played by RNS in autophagy/mitophagy and ischemic brain injury. Areas covered: Following factors should be considered in the studies on autophagy/mitophagy in ischemic stroke: (1) Protocols for administration of autophagy regulators including administration time points, routes and doses, etc...
January 19, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28064545/androgen-receptor-activation-a-prospective-therapeutic-target-for-bladder-cancer
#14
Taichi Mizushima, Kathleen A Tirador, Hiroshi Miyamoto
Patients with non-muscle-invasive or muscle-invasive bladder cancer undergoing surgery and currently available conventional therapy remain having a high risk of tumor recurrence or progression, respectively. Novel targeted molecular therapy is therefore expected to improve patient outcomes. Meanwhile, substantially higher incidence of bladder cancer in men has prompted research on androgen-mediated androgen receptor (AR) signaling in this malignancy. Indeed, preclinical evidence has suggested that AR signaling plays an important role in urothelial carcinogenesis and tumor outgrowth as well as resistance to some of the currently available conventional non-surgical therapies...
January 19, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28052702/the-potential-of-inhibiting-glutamine-uptake-as-a-therapeutic-target-for-multiple-myeloma
#15
Nicola Giuliani, Martina Chiu, Marina Bolzoni, Fabrizio Accardi, Massimiliano G Bianchi, Denise Toscani, Franco Aversa, Ovidio Bussolati
No abstract text is available yet for this article.
January 18, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28064546/targeting-protein-kinase-b3-akt3-signaling-in-melanoma
#16
SubbaRao V Madhunapantula, Gavin P Robertson
Deregulated Akt activity leading to apoptosis inhibition, enhanced proliferation and drug resistance has been shown to be responsible for 35-70% of advanced metastatic melanomas. Of the three isoforms, the majority of melanomas have elevated Akt3 expression and activity. Hence, potent inhibitors targeting Akt are urgently required, which is possible only if (a) the factors responsible for the failure of Akt inhibitors in clinical trials is known; and (b) the information pertaining to synergistically acting targeted therapeutics is available...
January 16, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28052701/potential-for-targeting-dopamine-darpp-32-signaling-in-neuropsychiatric-and-neurodegenerative-disorders
#17
Akinori Nishi, Takahide Shuto
Alterations in dopamine neurotransmission has been implicated in pathophysiology of neuropsychiatric and neurodegenerative disorders, and DARPP-32 plays a pivotal role in dopamine neurotransmission. DARPP-32 likely influences dopamine-mediated behaviors in animal models of neuropsychiatric and neurodegenerative disorders and therapeutic effects of pharmacological treatment. Areas covered: We will review animal studies on the biochemical and behavioral roles of DARPP-32 in drug addiction, schizophrenia and Parkinson's disease...
January 13, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28055275/the-nr4a-subfamily-of-nuclear-receptors-potential-new-therapeutic-targets-for-the-treatment-of-inflammatory-diseases
#18
Ricardo Rodríguez-Calvo, Marta Tajes, Manuel Vázquez-Carrera
Prolonged inflammatory response contributes to the pathogenesis of chronic disease-related disturbances. Among nuclear receptors (NRs), the orphan NR4A subfamily, which includes Nur77 (NR4A1), Nurr1 (NR4A2) and NOR1 (NR4A3), has recently emerged as a therapeutic target for the treatment of inflammation. Areas covered: This review focuses on the capacity of NR4A receptors to counter-regulate the development of the inflammatory response, with a special focus on the molecular transrepression mechanisms. Expert opinion: Recent studies have highlighted the role of NR4A receptors as significant regulators of the inflammatory response...
January 12, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28019725/the-kcc3-cotransporter-as-a-therapeutic-target-for-peripheral-neuropathy
#19
Eric Delpire, Kristopher T Kahle
No abstract text is available yet for this article.
January 5, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28001437/garp-as-a-therapeutic-target-for-modulation-of-t-regulatory-cell-function
#20
Ethan M Shevach
Foxp3(+) T regulatory cells (Tregs) play critical roles in immune homeostasis primarily by suppressing many aspects of the immune response. Tregs uniquely express GARP on their cell surface and GARP functions as a delivery system for latent TGF-β. As Treg-derived TGF-β may mediate the suppressive functions of Tregs, GARP may represent a target to inhibit Treg suppression in cancer or augment suppression in autoimmunity. Areas covered: This article will focus on 1) the role of Treg-derived TGF-β in the suppressive activity of Treg, 2) the cellular and molecular regulation of expression of GARP on mouse and human Tregs, 3) the role of integrins in the activation of latent-TGF-β/GARP complex, 4) an overview of our present understanding of the function of the latent-TGF-β/GARP complex...
December 29, 2016: Expert Opinion on Therapeutic Targets
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