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Pharmacology & Therapeutics

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https://www.readbyqxmd.com/read/29966598/post-translational-modifications-of-transporters
#1
REVIEW
Lindsay C Czuba, Kathleen M Hillgren, Peter W Swaan
Drug transporter proteins are critical to the distribution of a wide range of endogenous compounds and xenobiotics such as hormones, bile acids, peptides, lipids, sugars, and drugs. There are two classes of drug transporters- the solute carrier (SLC) transporters and ATP-binding cassette (ABC) transporters -which predominantly differ in the energy source utilized to transport substrates across a membrane barrier. Despite their hydrophobic nature and residence in the membrane bilayer, drug transporters have dynamic structures and adopt many conformations during the translocation process...
June 29, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29964125/structural-and-clinical-consequences-of-activation-loop-mutations-in-class-iii-receptor-tyrosine-kinases
#2
REVIEW
Lillian R Klug, Jason D Kent, Michael C Heinrich
Mutations within the activation loop of members of the class III receptor tyrosine kinase (RTK) subfamily, which includes KIT, PDGFRA, and FLT3, have been observed in multiple human tumor types. These mutations confer constitutive activation as well as resistance to the type II tyrosine kinase inhibitors (TKI) that are currently clinically available, such as imatinib and sunitinib. It is now understood that activation loop mutations in class III RTKs shift the activation state equilibrium away from inactive states, to which type II TKIs bind, to the active state by destabilizing the inactive conformation...
June 28, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29964124/cardiotoxicity-mechanisms-of-the-combination-of-braf-inhibitors-and-mek-inhibitors
#3
REVIEW
Enrico Bronte, Giuseppe Bronte, Giuseppina Novo, Gaetana Rinaldi, Fabrizio Bronte, Francesco Passiglia, Antonio Russo
Many new drugs have appeared in last years in the oncological treatment scenario. Each drug carries an important set of adverse events, not less, cardiovascular adverse events. This aspect is even more important considering the increasing use of combination therapies with two drugs, or three drugs as in some ongoing clinical trials. Besides it represents a growing problem for Cardiologists, that face it in every day clinical practice and that will face it probably more and more in the coming years. This work reviews the mechanism of action of BRAF-inhibitors and MEK-inhibitors used together, the pathophysiological mechanisms that lead to cardiovascular toxicity...
June 28, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29964123/prospective-for-cytochrome-p450-epoxygenase-cardiovascular-and-renal-therapeutics
#4
REVIEW
John D Imig
Therapeutics for arachidonic acid pathways began with the development of non-steroidal anti-inflammatory drugs that inhibit cyclooxygenase (COX). The enzymatic pathways and arachidonic acid metabolites and respective receptors have been successfully targeted and therapeutics developed for pain, inflammation, pulmonary and cardiovascular diseases. These drugs target the COX and lipoxygenase pathways but not the third branch for arachidonic acid metabolism, the cytochrome P450 (CYP) pathway. Small molecule compounds targeting enzymes and CYP epoxy-fatty acid metabolites have evolved rapidly over the last two decades...
June 28, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29953902/molecular-targets-of-atypical-antipsychotics-from-mechanism-of-action-to-clinical-differences
#5
REVIEW
Stefano Aringhieri, Marco Carli, Shivakumar Kolachalam, Valeria Verdesca, Enrico Cini, Mario Rossi, Peter J McCormick, Giovanni U Corsini, Roberto Maggio, Marco Scarselli
The introduction of atypical antipsychotics (AAPs) since the discovery of its prototypical drug clozapine has been a revolutionary pharmacological step for treating psychotic patients as these allow a significant recovery not only in terms of hospitalization and reduction in severity symptoms, but also in terms of safety, socialization and better rehabilitation in the society. Regarding the mechanism of action, AAPs are weak D2 receptor antagonists and they act beyond D2 antagonism, involving other receptor targets which regulate dopamine and other neurotransmitters...
June 25, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29953901/novel-therapeutic-strategy-for-cancer-and-autoimmune-conditions-modulating-cell-metabolism-and-redox-capacity
#6
REVIEW
Xing-Xing Fan, Hu-Dan Pan, Ying Li, Rui-Jin Guo, Elaine Lai-Han Leung, Liang Liu
Dysregulation of cell metabolism and redox balance is implicated in the pathogenesis and progression of cancer and autoimmune diseases. Because the cell proliferation and apoptotic regulatory pathways are interconnected with metabolic and redox signalling pathways, the current mono-target treatment is ineffective, and multi-drug resistance remains common. Complex diseases are often implicated in a network-based context of pathology; therefore, a new holistic intervention approach is required to block multi-crosstalk in such complicated circumstances...
June 25, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29953900/neurosteroids-non-genomic-pathways-in-neuroplasticity-involvement-in-neurological-diseases
#7
REVIEW
Marina Schverer, Laurence Lanfumey, Etienne-Emile Baulieu, Nicolas Froger, Isabelle Villey
Neurosteroids are neuroactive brain-born steroids. They can act through non-genomic and/or through genomic pathways. Genomic pathways are largely described for steroid hormones: the binding to nuclear receptors leads to transcription regulation. Pregnenolone, Dehydroepiandrosterone, their respective sulfate esters and Allopregnanolone have no corresponding nuclear receptor identified so far whereas some of their non-genomic targets have been identified. Neuroplasticity is the capacity that neuronal networks have to change their structure and function in response to biological and/or environmental signals; it is regulated by several mechanisms, including those that involve neurosteroids...
June 25, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29953899/more-than-fishing-for-a-cure-the-promises-and-pitfalls-of-high-throughput-cancer-cell-line-screens
#8
REVIEW
Alexander Ling, Robert F Gruener, Jessica Fessler, R Stephanie Huang
High-throughput screens in cancer cell lines (CCLs) have been used for decades to help researchers identify compounds with the potential to improve the treatment of cancer and, more recently, to identify genomic susceptibilities in cancer via genome-wide shRNA and CRISPR/Cas9 screens. Additionally, rich genomic and transcriptomic data of these CCLs has allowed researchers to pair this screening data with biological features, enabling efforts to identify biomarkers of treatment response and gene dependencies...
June 25, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29909238/autophagy-as-an-emerging-target-in-cardiorenal-metabolic-disease-from-pathophysiology-to-management
#9
REVIEW
Yingmei Zhang, Adam T Whaley-Connell, James R Sowers, Jun Ren
Although advances in medical technology and health care have improved the early diagnosis and management for cardiorenal metabolic disorders, the prevalence of obesity, insulin resistance, diabetes, hypertension, dyslipidemia, and kidney disease remains high. Findings from numerous population-based studies, clinical trials, and experimental evidence have consolidated a number of theories for the pathogenesis of cardiorenal metabolic anomalies including resistance to the metabolic action of insulin, abnormal glucose and lipid metabolism, oxidative and nitrosative stress, endoplasmic reticulum (ER) stress, apoptosis, mitochondrial damage, and inflammation...
June 21, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29933033/progress-and-challenges-of-selective-farnesoid-x-receptor-modulation
#10
REVIEW
Vittoria Massafra, Roberto Pellicciari, Antimo Gioiello, Saskia W C van Mil
Bile acids are amphipathic molecules that were previously known to serve as fat solubilizers in the intestine in postprandial conditions. In the last two decades, bile acids have been recognized as signaling molecules regulating energy metabolism pathways via, amongst others, the farnesoid X receptor (FXR). Upon bile acid activation, FXR controls expression of genes involved in bile acid, lipid, glucose and amino acid metabolism. In addition, FXR activation has been shown to limit the inflammatory response...
June 20, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29933035/two-decades-of-research-in-discovery-of-anticancer-drugs-targeting-stat3-how-close-are-we
#11
REVIEW
Jenny Beebe, Jing-Yuan Liu, Jian-Ting Zhang
Signal transducer and activator of transcription 3 (STAT3) controls many biological processes including differentiation, survival, proliferation, and angiogenesis. In normal healthy cells, STAT3 is tightly regulated to maintain a momentary active state. However, aberrant or constitutively activated STAT3 has been observed in many different cancers and constitutively activated STAT3 has been shown to associate with poor prognosis and tumor progression. For this reason, STAT3 has been studied as a possible target in the treatment of many different types of cancers...
June 19, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29933034/cdk4-6-inhibitors-in-breast-cancer-therapy-current-practice-and-future-opportunities
#12
REVIEW
Filipa Lynce, Ayesha N Shajahan-Haq, Sandra M Swain
Dysregulation of the cyclin dependent kinase pathway in luminal breast cancer creates a new therapeutic opportunity for estrogen receptor positive breast cancer. Initial pan-CDK inhibitors were associated with extensive toxicities but in recent years, the development of potent specific CDK inhibitors with favorable tolerability has driven renewed interests in this class of targeted therapies. Palbociclib, ribociclib and abemaciclib are specific CDK4/6 inhibitors that have been approved by the U.S. Food and Drug Administration for use in combination with endocrine therapy for women with advanced hormone receptor positive breast cancer...
June 19, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29932886/chloroquine-and-nanoparticle-drug-delivery-a-promising-combination
#13
REVIEW
Joe Pelt, Sara Busatto, Mauro Ferrari, E Aubrey Thompson, Kabir Mody, Joy Wolfram
Clinically approved cancer therapies include small molecules, antibodies, and nanoparticles. There has been major progress in the treatment of several cancer types over recent decades. However, many challenges remain for optimal use of conventional and nanoparticle-based therapies in oncology including poor drug delivery, rapid clearance, and drug resistance. The antimalarial agent chloroquine has been found to mitigate some of these challenges by modulating cancer cells and the tissue microenvironment. Particularly, chloroquine was recently found to reduce immunological clearance of nanoparticles by resident macrophages in the liver, leading to increased tumor accumulation of nanodrugs...
June 19, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29909237/glycosylation-as-new-pharmacological-strategies-for-diseases-associated-with-excessive-angiogenesis
#14
REVIEW
Simon Bousseau, Luisa Vergori, Raffaella Soleti, Guy Lenaers, M Carmen Martinez, Ramaroson Andriantsitohaina
Angiogenesis is a complex process describing the growth of new blood vessels from existing vasculature, and is triggered by local pro-angiogenic factors, such as vascular endothelial growth factor (VEGF), which increase the metabolism of endothelial cells (ECs). Angiogenesis takes part in various physiological conditions such as embryogenesis, placental growth, and in pathological conditions such as tumor growth, diabetic retinopathy, rheumatoid arthritis (RA) and ischemic diseases. Current therapies against excessive angiogenesis target vascular growth signaling...
June 19, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29909239/approaches-to-target-ige-antibodies-in-allergic-diseases
#15
REVIEW
Bianca Balbino, Eva Conde, Thomas Marichal, Philipp Starkl, Laurent L Reber
IgE is the antibody isotype found at the lowest concentration in the circulation. However IgE can undeniably play an important role in mediating allergic reactions; best exemplified by the clinical benefits of anti-IgE monoclonal antibody (omalizumab) therapy for some allergic diseases. This review will describe our current understanding of the interactions between IgE and its main receptors FcεRI and CD23 (FcεRII). We will review the known and potential functions of IgE in health and disease: in particular, its detrimental roles in allergic diseases and chronic spontaneous urticaria, and its protective functions in host defense against parasites and venoms...
June 26, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29909236/antiepileptic-drugs-as-analgesics-adjuvants-in-inflammatory-pain-current-preclinical-evidence
#16
REVIEW
Tomić Maja, Pecikoza Uroš, Micov Ana, Vučković Sonja, Stepanović-Petrović Radica
Inflammatory pain is the most common type of pain that is treated clinically. The use of currently available treatments (classic analgesics - NSAIDs, paracetamol and opioids) is limited by insufficient efficacy and/or side effects/tolerance development. Antiepileptic drugs (AEDs) are widely used in neuropathic pain treatment, but there is substantial preclinical evidence on their efficacy against inflammatory pain, too. In this review we focus on gabapentinoids (gabapentin and pregabalin) and dibenzazepine AEDs (carbamazepine, oxcarbazepine, and recently introduced eslicarbazepine acetate) and their potential for relieving inflammatory pain...
June 15, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29909235/regulation-of-prostate-cancer-by-hormone-responsive-g-protein-coupled-receptors
#17
REVIEW
Wei Wang, Zhao-Xia Chen, Dong-Yu Guo, Ya-Xiong Tao
Regulation of prostate cancer by androgen and androgen receptor (AR), and blockade of AR signaling by AR antagonists and steroidogenic enzyme inhibitors have been extensively studied. G protein-coupled receptors (GPCRs) are a family of membrane receptors that regulate almost all physiological processes. Nearly 40% of FDA-approved drugs in the market target GPCRs. A variety of GPCRs that mediate reproductive function have been demonstrated to be involved in the regulation of prostate cancer. These GPCRs include gonadotropin-releasing hormone receptor, luteinizing hormone receptor, follicle-stimulating hormone receptor, relaxin receptor, ghrelin receptor, and kisspeptin receptor...
June 15, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29890115/from-chemo-prevention-to-epigenetic-regulation-the-role-of-isothiocyanates-in-skin-cancer-prevention
#18
REVIEW
Melina Mitsiogianni, Tom Amery, Rodrigo Franco, Vasilis Zoumpourlis, Aglaia Pappa, Mihalis I Panayiotidis
Skin cancer incidence is rapidly growing over the last decades and is generally divided into malignant melanoma and non-melanoma (NMSC) with the latter being subdivided into squamous (SCC) and basal cell carcinoma (BCC). Among them, melanoma is the most aggressive type with high mortality rates. On the other hand, aberrant gene expression is a critical step towards malignant transformation. To this end, epigenetic modifications like changes in DNA methylation patterns and miRNA expression profile as well as histone modifications are all capable of inducing an altered gene expression profile involved in various cellular cascades including cell cycle, proliferation and apoptosis...
June 8, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29859177/targeting-phosphatases-of-regenerating-liver-prls-in-cancer
#19
REVIEW
Min Wei, Konstantin V Korotkov, Jessica S Blackburn
The phosphatase of regenerating liver (PRL) family, also known as protein tyrosine phosphatase 4A (PTP4A), are dual-specificity phosphatases with largely unknown cellular functions. However, accumulating evidence indicates that PRLs are oncogenic across a broad variety of human cancers. PRLs are highly expressed in advanced tumors and metastases compared to early stage cancers or matched healthy tissue, and high expression of PRLs often correlates with poor patient prognosis. Consequentially, PRLs have been considered potential therapeutic targets in cancer...
June 4, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29842917/therapeutic-targeting-of-cathepsin-c-from-pathophysiology-to-treatment
#20
REVIEW
Brice Korkmaz, George H Caughey, Iain Chapple, Francis Gauthier, Josefine Hirschfeld, Dieter E Jenne, Ralph Kettritz, Gilles Lalmanach, Anne-Sophie Lamort, Conni Lauritzen, Monika Łȩgowska, Adam Lesner, Sylvain Marchand-Adam, Sarah J McKaig, Celia Moss, John Pedersen, Helen Roberts, Adrian Schreiber, Seda Seren, Nalin S Thakker
Cathepsin C (CatC) is a highly conserved tetrameric lysosomal cysteine dipeptidyl aminopeptidase. The best characterized physiological function of CatC is the activation of pro-inflammatory granule-associated serine proteases. These proteases are synthesized as inactive zymogens containing an N-terminal pro-dipeptide, which maintains the zymogen in its inactive conformation and prevents premature activation, which is potentially toxic to the cell. The activation of serine protease zymogens occurs through cleavage of the N-terminal dipeptide by CatC during cell maturation in the bone marrow...
May 26, 2018: Pharmacology & Therapeutics
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