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Trends in Pharmacological Sciences

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https://www.readbyqxmd.com/read/28818333/li-fraumeni-syndrome-disease-model-a-platform-to-develop-precision-cancer-therapy-targeting-oncogenic-p53
#1
REVIEW
Ruoji Zhou, An Xu, Julian Gingold, Louise C Strong, Ruiying Zhao, Dung-Fang Lee
Li-Fraumeni syndrome (LFS) is a rare hereditary autosomal dominant cancer disorder. Germline mutations in TP53, the gene encoding p53, are responsible for most cases of LFS. TP53 is also the most commonly mutated gene in human cancers. Because inhibition of mutant p53 is considered to be a promising therapeutic strategy to treat these diseases, LFS provides a perfect genetic model to study p53 mutation-associated malignancies as well as to screen potential compounds targeting oncogenic p53. In this review we briefly summarize the biology of LFS and current understanding of the oncogenic functions of mutant p53 in cancer development...
August 14, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28807369/an-interview-with-ruth-nussinov
#2
(no author information available yet)
No abstract text is available yet for this article.
August 11, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28784329/targeting-mechanisms-linking-copd-to-type-2-diabetes-mellitus
#3
REVIEW
Mario Cazzola, Paola Rogliani, Luigino Calzetta, Davide Lauro, Clive Page, Maria Gabriella Matera
Chronic obstructive pulmonary disease (COPD) and type 2 diabetes mellitus (T2DM) often coexist. The mechanistic links between these two diseases are complex, multifactorial, and not entirely understood, but they can influence the approach to treatment. Understanding whether COPD comes first followed by T2DM or vice versa, or whether the two diseases develop simultaneously due to common underlying mechanisms, is important for the development of novel therapeutic approaches to these two important diseases. In this review, we discuss the potential links between COPD and T2DM and pharmacological approaches that might target these links...
August 4, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28760488/genetically-engineered-bacteria-for-treating-human-disease
#4
Buyun Ma, Qiuwei Pan, Maikel P Peppelenbosch
Bacteria have now been harnessed to combat human diseases, especially to meet the challenge of antimicrobial resistance. Modulating the microbiome, particularly by genetically engineering the bacteria, has provided proof-of-concept as potential pharmacotherapy, but those involved in this field should engage in discussion as how to move forward.
July 28, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28734639/ffa4-gpr120-pharmacology-and-therapeutic-opportunities
#5
REVIEW
Graeme Milligan, Elisa Alvarez-Curto, Brian D Hudson, Rudi Prihandoko, Andrew B Tobin
Free Fatty Acid receptor 4 (FFA4), also known as GPR120, is a G-protein-coupled receptor (GPCR) responsive to long-chain fatty acids that is attracting considerable attention as a potential novel therapeutic target for the treatment of type 2 diabetes mellitus (T2DM). Although no clinical studies have yet been initiated to assess efficacy in this indication, a significant number of primary publications and patents have highlighted the ability of agonists with potency at FFA4 to improve glucose disposition and enhance insulin sensitivity in animal models...
July 19, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28728963/structural-principles-of-fluorescent-rna-aptamers
#6
REVIEW
Robert J Trachman, Lynda Truong, Adrian R Ferré-D'Amaré
Several aptamer RNAs have been selected in vitro that bind to otherwise weakly fluorescent small molecules and enhance their fluorescence several thousand-fold. By genetically tagging cellular RNAs of interest with these aptamers and soaking cells in their cell-permeable cognate small-molecule fluorophores, it is possible to use them to study RNA localization and trafficking. These aptamers have also been fused to metabolite-binding RNAs to generate fluorescent biosensors. The 3D structures of three unrelated fluorogenic RNAs have been determined, and reveal a shared reliance on base quadruples (tetrads) to constrain the photo-excited chromophore...
July 17, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28711156/towards-a-structural-view-of-drug-binding-to-herg-k-channels
#7
REVIEW
Jamie I Vandenberg, Eduardo Perozo, Toby W Allen
The human ether-a-go-go-related gene (hERG) K(+) channel is of great medical and pharmaceutical relevance. Inherited mutations in hERG result in congenital long-QT syndrome which is associated with a markedly increased risk of cardiac arrhythmia and sudden death. hERG K(+) channels are also remarkably susceptible to block by a wide range of drugs, which in turn can cause drug-induced long-QT syndrome and an increased risk of sudden death. The recent determination of the near-atomic resolution structure of the hERG K(+) channel, using single-particle cryo-electron microscopy (cryo-EM), provides tremendous insights into how these channels work...
July 12, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28709554/lessons-learned-from-two-decades-of-anticancer-drugs
#8
REVIEW
Zhichao Liu, Brian Delavan, Ruth Roberts, Weida Tong
Tremendous efforts have been made to elucidate the basis of cancer biology with the aim of promoting anticancer drug development. Especially over the past 20 years, anticancer drug development has developed from conventional cytotoxic agents to target-based and immune-related therapies. Consequently, more than 200 anticancer drugs are available on the market. However, anticancer drug development still suffers high attrition during the later phases of clinical development and is considered to be a difficult and risky therapeutic category within the drug development arena...
July 11, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28687272/interstrand-crosslink-repair-as-a-target-for-hdac-inhibition
#9
REVIEW
Teodora Nikolova, Nicole Kiweler, Oliver H Krämer
DNA interstrand crosslinks (ICLs) covalently connect complementary DNA strands. Consequently, DNA replication and transcription are hampered, DNA damage responses (DDR) are initiated, and cell death is triggered. Therefore, drugs inducing ICLs are effective against rapidly growing cancer cells. However, tumors engage a complicated enzymatic machinery to repair and survive ICLs. Several factors, including the post-translational acetylation/deacetylation of lysine residues within proteins, control this network...
July 4, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28668224/the-future-of-cysteine-cathepsins-in-disease-management
#10
REVIEW
Lovro Kramer, Dušan Turk, Boris Turk
Since the discovery of the key role of cathepsin K in bone resorption, cysteine cathepsins have been investigated by pharmaceutical companies as drug targets. The first clinical results from targeting cathepsins by activity-based probes and substrates are paving the way for the next generation of molecular diagnostic imaging, whereas the majority of antibody-drug conjugates currently in clinical trials depend on activation by cathepsins. Finally, cathepsins have emerged as suitable vehicles for targeted drug delivery...
June 28, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28668223/an-overview-of-novel-adjuvants-designed-for-improving-vaccine-efficacy
#11
REVIEW
Srinivasa Reddy Bonam, Charalambos D Partidos, Sampath Kumar M Halmuthur, Sylviane Muller
Adjuvants incorporated in prophylactic and/or therapeutic vaccine formulations impact vaccine efficacy by enhancing, modulating, and/or prolonging the immune response. In addition, they reduce antigen concentration and the number of immunizations required for protective efficacy, therefore contributing to making vaccines more cost effective. Our better understanding of the molecular mechanisms of immune recognition and protection has led research efforts to develop new adjuvants that are currently at various stages of development or clinical evaluation...
June 28, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28651847/the-cardiovascular-pharmacology-of-nonsteroidal-anti-inflammatory-drugs
#12
REVIEW
Tilo Grosser, Emanuela Ricciotti, Garret A FitzGerald
The principal molecular mechanisms underlying the cardiovascular (CV) and renal adverse effects of nonsteroidal anti-inflammatory drugs (NSAIDs), such as myocardial infarction and hypertension, are understood in more detail than most side effects of drugs. Less is known, however, about differences in the CV safety profile between chemically distinct NSAIDs and their relative predisposition to complications. In review article, we discuss how heterogeneity in the pharmacokinetics and pharmacodynamics of distinct NSAIDs may be expected to affect their CV risk profile...
June 23, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28648527/targeting-the-thioredoxin-system-for-cancer-therapy
#13
REVIEW
Junmin Zhang, Xinming Li, Xiao Han, Ruijuan Liu, Jianguo Fang
Thioredoxin (Trx) and thioredoxin reductase (TrxR) are essential components of the Trx system which plays pivotal roles in regulating multiple cellular redox signaling pathways. In recent years TrxR/Trx have been increasingly recognized as an important modulator of tumor development, and hence targeting TrxR/Trx is a promising strategy for cancer treatment. In this review we first discuss the structural details of TrxR, the functions of the Trx system, and the rational of targeting TrxR/Trx for cancer treatment...
June 22, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28648526/applying-structure-based-drug-design-approaches-to-allosteric-modulators-of-gpcrs
#14
REVIEW
Miles Congreve, Christine Oswald, Fiona H Marshall
Structural insights have been revealed from X-ray co-complexes of a range of G protein-coupled receptors (GPCRs) and their allosteric ligands. The understanding of how small molecules can modulate the function of this important class of receptors by binding to a diverse range of pockets on and inside the proteins has had a profound impact on the structure-based drug design (SBDD) of new classes of therapeutic agents. The types of allosteric pockets and the mode of modulation as well as the advantages and disadvantages of targeting allosteric pockets (as opposed to the natural orthosteric site) are considered in the context of these new structural findings...
June 22, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28645833/binding-kinetics-and-pathways-of-ligands-to-gpcrs
#15
REVIEW
Andrea Strasser, Hans-Joachim Wittmann, Roland Seifert
Previously, drugs were developed focusing on target affinity and selectivity. However, it is becoming evident that the drug-target residence time, related to the off-rate, is an important parameter for successful drug development. The residence time influences both the on-rate and overall effectiveness of drugs. Furthermore, ligand binding is now appreciated to be a multistep process because metastable and/or intermediate binding sites in the extracellular region have been identified. In this review, we summarize experimental ligand-binding data for G-protein-coupled receptors (GPCRs), and their binding pathways, analyzed by molecular dynamics (MD)...
June 20, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28629580/folding-underlies-bidirectional-role-of-gpr37-pael-r-in-parkinson-disease
#16
REVIEW
Lina Leinartaité, Per Svenningsson
Since conformational flexibility, which is required for the function of a protein, comes at the expense of structural stability, many proteins, including G-protein-coupled receptors (GPCRs), are under constant risk of misfolding and aggregation. In this regard GPR37 (also named PAEL-R and ETBR-LP-1) takes a prominent role, particularly in relation to Parkinson disease (PD). GPR37 is a substrate for parkin and accumulates abnormally in autosomal recessive juvenile parkinsonism, contributing to endoplasmic reticulum stress and death of dopaminergic neurons...
June 16, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28625497/pitfalls-and-opportunities-for-epigenomic-analyses-focused-on-disease-diagnosis-prognosis-and-therapy
#17
REVIEW
Volker M Lauschke, Maxim Ivanov, Magnus Ingelman-Sundberg
No abstract text is available yet for this article.
June 15, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28606480/sphingosine-kinase-2-in-autoimmune-inflammatory-disease-and-the-development-of-sphingosine-kinase-2-inhibitors
#18
REVIEW
Nigel J Pyne, David R Adams, Susan Pyne
The purpose of this Opinion is to present a case for targeting sphingosine kinase 2 (SK2) in autoimmune/inflammatory disease. Data obtained using Sphk2(-/-) mice suggest that SK2 is an anti-inflammatory enzyme, although this might be misleading because of a compensatory increase in the expression of a second isoform, sphingosine kinase 1 (SK1), which functions as a proinflammatory enzyme. SK2 is involved in regulating interleukin (IL)-12/interferon gamma (IFN-γ) and histone deacetylase-1/2 (HDAC-1/2) signalling and, potentially, retinoid-related orphan receptor gamma t (ROR-γt) stability linked with T helper (Th) 17 cell polarisation...
June 9, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28606479/therapeutic-potential-of-ranibizumab-in-corneal-neovascularization
#19
Marianne L Shahsuvaryan
Ranibizumab is a humanized, affinity-matured vascular endothelial growth factor (VEGF) antibody fragment that neutralizes all isoforms of VEGF and is FDA approved for use in ophthalmology. Recently it was suggested that ranibizumab may be useful in the treatment of corneal neovascularization, but in reality this therapy is not yet evidence based.
June 9, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28602395/reprogramming-of-the-tumor-in-the-hypoxic-niche-the-emerging-concept-and-associated-therapeutic-strategies
#20
REVIEW
Guan-Zhong Qiu, Ming-Zhu Jin, Jin-Xiang Dai, Wei Sun, Ji-Hong Feng, Wei-Lin Jin
Hypoxia exerts a profound impact on diverse aspects of cancer biology. Increasing evidence has revealed novel functions of hypoxia in cancer cell epigenomics, epitranscriptomics, metabolism, and intercellular communication, all hotspots of cancer research. Several drugs have been developed to target intratumoral hypoxia and have entered clinical trials to treat refractory tumors. However, direct targeting of hypoxia signaling still has limitations in the clinic with regard to cancer progression and resistance to therapy...
June 8, 2017: Trends in Pharmacological Sciences
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