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https://www.readbyqxmd.com/read/29458108/the-relaxin-receptor-as-a-therapeutic-target-perspectives-from-evolution-and-drug-targeting
#1
REVIEW
Ross A D Bathgate, Martina Kocan, Daniel J Scott, M Akhter Hossain, Sara V Good, Sergey Yegorov, Jan Bogerd, Paul Gooley
The peptide relaxin was first identified as an important circulating hormone during pregnancy over 90 years ago. Research over many years defined the numerous biological roles that relaxin plays throughout pregnancy in many mammalian species. These important biological actions have led to the testing of relaxin as a therapeutic agent for a number of indications. The discovery of the relaxin receptor, RXFP1, in 2002 facilitated the better understanding of the cellular targets of relaxin, its mechanism of action and enabled the development of relaxin mimetics and screening for small molecule agonists...
February 16, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29456802/hts-by-nmr-for-the-identification-of-potent-and-selective-inhibitors-of-metalloenzymes
#2
Carlo Baggio, Linda Cerofolini, Marco Fragai, Claudio Luchinat, Maurizio Pellecchia
We have recently proposed a novel drug discovery approach based on biophysical screening of focused positional scanning libraries in which each element of the library contained a common binding moiety for the given target or class of targets. In this Letter, we report on the implementation of this approach to target metal containing proteins. In our implementation, we first derived a focused positional scanning combinatorial library of peptide mimetics (of approximately 100,000 compounds) in which each element of the library contained the metal-chelating moiety hydroxamic acid at the C-terminal...
February 8, 2018: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29456512/local-injections-of-superoxide-dismutase-attenuate-the-exercise-pressor-reflex-in-rats-with-femoral-artery-occlusion
#3
Jihong Xing, Jian Lu, Jiahao Liu, Jianhua Li
The exercise pressor reflex is amplified in patients with peripheral artery disease (PAD) and in an experimental PAD model of rats induced by femoral artery occlusion. Heightened blood pressure worsens the restricted blood flow directed to the limbs in this disease. The purpose of this study was to determine the role played by muscle oxidative stress in regulating the augmented pressor response to static exercise in PAD. We hypothesized that limb ischemia impairs muscle superoxide dismutase (SOD) thereby leading to abnormal autonomic responsiveness observed in PAD animals, and a chronic compensation of SOD for anti-oxidation improves the exaggerated exercise pressor reflex...
2018: Frontiers in Physiology
https://www.readbyqxmd.com/read/29455885/vincristine-resistance-in-relapsed-neuroblastoma-can-be-efficiently-overcome-by-smac-mimetic-lcl161-treatment
#4
Kristin Frommann, Birgit Appl, Patrick Hundsdoerfer, Konrad Reinshagen, Georg Eschenburg
PURPOSE: In spite of good initial therapy response neuroblastomas often spread to distant organs or relapse after periods of remission. Dysregulation of apoptosis, a hallmark of cancer, is often effected by elevated levels of antiapoptotic signals leading to resistance against chemotherapeutic drugs. Inhibitors of apoptosis proteins (IAPs) are crucial cellular apoptosis regulators. Targeting IAPs with Smac mimetics has been demonstrated as a promising strategy for treatment of neuroblastoma and other tumors...
January 31, 2018: Journal of Pediatric Surgery
https://www.readbyqxmd.com/read/29455203/absence-of-nicotinamide-nucleotide-transhydrogenase-in-c57bl-6j-mice-exacerbates-experimental-atherosclerosis
#5
Aimee E Vozenilek, Matthew Vetkoetter, Jonette M Green, Xinggui Shen, James G Traylor, Ronald L Klein, A Wayne Orr, Matthew D Woolard, David M Krzywanski
BACKGROUND: Mitochondrial reactive oxygen species (ROS) contribute to inflammation and vascular remodeling during atherosclerotic plaque formation. C57BL/6N (6N) and C57BL/6J (6J) mice display distinct mitochondrial redox balance due to the absence of nicotinamide nucleotide transhydrogenase (NNT) in 6J mice. We hypothesize that differential NNT expression between these animals alters plaque development. METHODS: 6N and 6J mice were treated with AAV8-PCSK9 (adeno-associated virus serotype 8/proprotein convertase subtilisin/kexin type 9) virus leading to hypercholesterolemia, increased low-density lipoprotein, and atherosclerosis in mice fed a high-fat diet (HFD)...
February 16, 2018: Journal of Vascular Research
https://www.readbyqxmd.com/read/29454855/signalling-pathways-regulating-galactosaminoglycan-synthesis-and-structure-in-vascular-smooth-muscle-implications-for-lipoprotein-binding-and-atherosclerosis
#6
REVIEW
Rizwana Afroz, Yingnan Cao, Muhamad Ashraf Rostam, Hang Ta, Suowen Xu, Wenhua Zheng, Narin Osman, Danielle Kamato, Peter J Little
Atherosclerosis commences with the trapping of low density lipoproteins (LDLs) in blood vessels by modified proteoglycans (PGs) with hyperelongated glycosaminoglycan (GAG) chains. GAG chain synthesis and growth factor mediated hyperelongation regulates the composition and size of PGs in a manner that would cause low density lipoprotein (LDLs) retention in vessel wall. Galactosaminoglycans are a class of GAGs, commonly observed on PGs. Multiple enzymes are involved in galactosaminoglycan biosynthesis. Galactosaminoglycan synthesis is regulated by various signalling pathways which are amenable to pharmacological manipulation to treat atherosclerosis...
February 15, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29454280/8-chrysoeriol-as-a-potential-bcl-2-inhibitor-triggers-apoptosis-of-sw1990-pancreatic-cancer-cells
#7
Yiwen Zhang, Zhimei Li, Qiuxia Min, Abulizi Palida, Yiyuan Zhang, Ruotian Tang, Lixia Chen, Hua Li
8-Chrysoeriol, a bioactive flavanoid, was firstly identified to bind directly to BCL-2 as BH3 mimetics by structure-based virtual ligand screening. And 3D docking model revealed the molecular basis of 8-Chrysoeriol targeting to BCL-2. The interaction between 8-Chrysoeriol and BCL-2 was further confirmed using Microscale Thermophoresis (MST) technique. Meanwhile, high expression level of antiapoptotic protein BCL-2 was detected in SW1990 pancreatic cancer cells and 8-Chrysoeriol showed obvious proapoptosis effect against SW1990 in vitro...
February 2, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29453454/a-microvascularized-tumor-mimetic-platform-for-assessing-anti-cancer-drug-efficacy
#8
Shantanu Pradhan, Ashley M Smith, Charles J Garson, Iman Hassani, Wen J Seeto, Kapil Pant, Robert D Arnold, Balabhaskar Prabhakarpandian, Elizabeth A Lipke
Assessment of anti-cancer drug efficacy in in vitro three-dimensional (3D) bioengineered cancer models provides important contextual and relevant information towards pre-clinical translation of potential drug candidates. However, currently established models fail to sufficiently recapitulate complex tumor heterogeneity. Here we present a chip-based tumor-mimetic platform incorporating a 3D in vitro breast cancer model with a tumor-mimetic microvascular network, replicating the pathophysiological architecture of native vascularized breast tumors...
February 16, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29449668/rhinovirus-3c-protease-suppresses-apoptosis-and-triggers-caspase-independent-cell-death
#9
Mark Lötzerich, Pascal S Roulin, Karin Boucke, Robert Witte, Oleg Georgiev, Urs F Greber
Apoptosis and programmed necrosis (necroptosis) determine cell fate, and antagonize infection. Execution of these complementary death pathways involves the formation of receptor-interacting protein kinase 1 (RIPK1) containing complexes. RIPK1 binds to adaptor proteins, such as TRIF (Toll-IL-1 receptor-domain-containing-adaptor-inducing interferon-beta factor), FADD (Fas-associated-protein with death domain), NEMO (NF-κB regulatory subunit IKKγ), SQSTM1 (sequestosome 1/p62), or RIPK3 (receptor-interacting protein kinase 3), which are involved in RNA sensing, NF-κB signaling, autophagosome formation, apoptosis, and necroptosis...
February 15, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29448566/highly-efficient-electrochemical-detection-of-phenolic-compounds-utilizing-superior-catalytic-activity-of-nanohybrids-consisting-of-magnetic-nanoparticles-and-gold-nanoclusters
#10
Seong-Rok Kim, Seongyeon Cho, Moon Il Kim
Although Fe3O4 magnetic nanoparticles (MNPs) have gathered particular interest as potent peroxidase mimetics, their practical utility has been critically limited by their low catalytic activity. Here, we have developed a nanohybrid material to significantly enhance the catalytic activity of MNPs by incorporating other enzyme mimetics, gold nanoclusters (AuNCs), through electrostatic attraction. Owing to the synergistic effect of MNPs and AuNCs, the constructed nanohybrid yielded highly enhanced peroxidase-like activity and higher resolution in electrochemical detection of H2O2 than bare MNPs...
February 1, 2018: Journal of Nanoscience and Nanotechnology
https://www.readbyqxmd.com/read/29448519/peroxidase-like-activity-of-gold-nanoparticles-and-their-gold-staining-enhanced-elisa-application
#11
Doudou Lou, Yanyan Tian, Yu Zhang, Junjie Yin, Ting Yang, Chuan He, Ming Ma, Wei Yu, Ning Gu
We found that the peroxidase-like activity of gold nanoparticles (GNPs) followed the Michaelis-Menten kinetic model and was dependent on environmental pH and temperature, which was very similar to natural Horseradish Peroxidase (HRP). However, unlike HRP, which needs a lower H2O2 concentration with a very narrow range to reach a maximum reaction rate and avoid enzyme poisoning, GNPs have very high activity, even at an H2O2 concentration two orders of magnitude higher than HRP. It was demonstrated that H2O2 treatment could enhance the peroxidase-like activity of GNPs, resulting thus in the activity increase in a circular catalytic reaction by the reduplicative use of GNPs...
February 1, 2018: Journal of Nanoscience and Nanotechnology
https://www.readbyqxmd.com/read/29448510/preparation-and-in-vivo-biodistribution-of-ultra-small-superparamagnetic-iron-oxide-nanoparticles-with-high-magnetic-targeting-response
#12
Xiaoyu Han, Pingping Yao, Chao Cheng, Hongmin Yuan, Yuxiang Yang, Chaoying Ni
The ultra-small superparamagnetic iron oxide (USPIO) particles with high saturation magnetization and good superparamagnetism were prepared by reverse micro-emulsions using novel C16E15 as surfactant, which can reduce magnetic dipole-dipole interaction, hence decreasing the critical blocking temperature (TB). Powder X-ray diffraction (XRD), Infrared spectrum (FT-IR), Transmission electron microscope (TEM), X-ray photoelectron spectroscopy (XPS), and Vibrating sample magnetometer (VSM) were used to characterize the magnetic particles...
February 1, 2018: Journal of Nanoscience and Nanotechnology
https://www.readbyqxmd.com/read/29447964/botulinum-toxin-type-a-relieves-sternocleidomastoid-muscle-fibrosis-in-congenital-muscular-torticollis
#13
Banghong Jiang, Wenxuan Zu, Jing Xu, Zhuyou Xiong, Yichao Zhang, Song Gao, Shuxing Ge, Li Zhang
Congenital muscular torticollis (CMT) is a neck deformity that involves shortening of sternocleidomastoid muscle (SCM) characterized by muscle atrophy and interstitial fibrosis. To investigate wheatear Botulinum toxin type A (BTA) has anti-fibrotic effects in CMT, we established acquired muscular torticollis that mimetics CMT in rabbit by intra-SCM injection of anhydrous alcohol. The treatment groups received BTA (2.5 units or 5 units) injection into the fibrotic SCM. The shortening and thickening of SCM were recorded by B-mode ultrasound...
February 12, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29447234/folic-acid-derived-p5779-mimetics-regulate-damp-mediated-inflammation-through-disruption-of-hmgb1-tlr4-md-2-axes
#14
Shan Sun, Mingzhu He, Yongjun Wang, Huan Yang, Yousef Al-Abed
High mobility group box 1 (HMGB1) is a damage-associated molecular pattern (DAMP) protein that mediates inflammatory responses after infection or injury. Previously, we reported a peptide inhibitor of HMGB1 (P5779) that acts by directly interrupting HMGB1/MD-2 binding. Here, fingerprint similarity search and docking studies suggest folic acid derived-drugs function as P5779 mimetopes. Molecular dynamic (MD) simulation studies demonstrate that folic acid mimics the binding of P5779 at the TLR4 and MD-2 intersection...
2018: PloS One
https://www.readbyqxmd.com/read/29446719/dna-double-strand-breaks-repair-inhibitors-relevance-as-potential-new-anticancer-therapeutics
#15
Paulina Kopa, Anna Macieja, Grzegorz Galita, Zbigniew J Witczak, Tomasz Poplawski
DNA Double-strand breaks are considered one of the most lethal form of DNA damage. Many effective anticancer therapeutic approaches used chemical and physical methods to generate DNA double-strand breaks in the cancer cells. They include: IR and drugs which mimetic its action, topoisomerase poisons, some alkylating agents or drugs which affected DNA replication process. On the other hand, cancer cells are mostly characterized by highly effective systems of DNA damage repair. There are two main DNA repair pathways used to fix double-strand breaks: NHEJ and HRR...
February 13, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29446104/heparin-mimetics-with-anticoagulant-activity
#16
REVIEW
Abdullah Al Nahain, Vera Ignjatovic, Paul Monagle, John Tsanaktsidis, Vito Ferro
Heparin, a sulfated polysaccharide belonging to the glycosaminoglycan family, has been widely used as an anticoagulant drug for decades and remains the most commonly used parenteral anticoagulant in adults and children. However, heparin has important clinical limitations and is derived from animal sources which pose significant safety and supply problems. The ever growing shortage of the raw material for heparin manufacturing may become a very significant issue in the future. These global limitations have prompted much research, especially following the recent well-publicized contamination scandal, into the development of alternative anticoagulants derived from non-animal and/or totally synthetic sources that mimic the structural features and properties of heparin...
February 15, 2018: Medicinal Research Reviews
https://www.readbyqxmd.com/read/29443506/peptoid-backbone-flexibility-dictates-its-interaction-with-water-and-surfaces-a-molecular-dynamics-investigation
#17
Arushi Prakash, Marcel D Baer, Christopher J Mundy, Jim Pfaendtner
Peptoids are peptide-mimetic biopolymers that are easy-to-synthesize and adaptable for use in drugs, chemical scaffolds, and coatings. However, there is insufficient information about their structural preferences and interactions with the environment in various applications. We conducted a study to understand the fundamental differences between peptides and peptoids using molecular dynamics simulations with semi-empirical (PM6) and empirical (AMBER) potentials, in conjunction with metadynamics enhanced sampling...
February 14, 2018: Biomacromolecules
https://www.readbyqxmd.com/read/29441961/clinically-relevant-interactions-of-anti-apoptotic-bcl-2-protein-inhibitors-with-abc-transporters
#18
E Ruzickova, R Janska, P Dolezel, P Mlejnek
In this work we studied clinically relevant interactions between the BH3 mimetics and the ABCB1 and ABCG2 transporters. We observed that the intracellular levels of ABT-263 and ABT-199, but not ABT-737, might be reduced by ABCB1 or ABCG2. Importantly, this effect was proportional to the transporter expression level. High transporter expression levels decreased the intracellular levels of ABT-263 and ABT-199 substantially. Low transporter expression levels, which are clinically relevant, affected the intracellular level of ABT-263 slightly but significantly, however, they failed to decrease the intracellular level of ABT-199 below the control level in parental cells...
December 1, 2017: Die Pharmazie
https://www.readbyqxmd.com/read/29440748/structural-properties-of-apolipoprotein-a-i-mimetic-peptides-that-promote-abca1-dependent-cholesterol-efflux
#19
Rafique M Islam, Mohsen Pourmousa, Denis Sviridov, Scott M Gordon, Edward B Neufeld, Lita A Freeman, B Scott Perrin, Richard W Pastor, Alan T Remaley
Peptides mimicking the major protein of highdensity lipoprotein (HDL), apolipoprotein A-I (apoA-I), are promising therapeutics for cardiovascular diseases. Similar to apoA-I, their atheroprotective property is attributed to their ability to form discoidal HDL-like particles by extracting cellular cholesterol and phospholipids from lipid microdomains created by the ABCA1 transporter in a process called cholesterol efflux. The structural features of peptides that enable cholesterol efflux are not well understood...
February 13, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29440169/oncogenic-kinase-induced-pkm2-tyrosine-105-phosphorylation-converts-non-oncogenic-pkm2-to-a-tumor-promoter-and-induces-cancer-stem-like-cells
#20
Zhifen Zhou, Min Li, Lin Zhang, Hong Zhao, Özgür Şahin, Jing Chen, Jean J Zhao, Zhou Songyang, Dihua Yu
The role of pyruvate kinase M2 isoform (PKM2) in tumor progression has been controversial. Previous studies showed that PKM2 promoted tumor growth in xenograft models; however, depletion of PKM2 in the Brca1-loss-driven mammary tumor mouse model accelerates tumor formation. Since oncogenic kinases are frequently activated in tumors and PKM2 phosphorylation promotes tumor growth, we hypothesized that phosphorylation of PKM2 by activated kinases in tumor cells confers PKM2 oncogenic function, whereas non-phosphorylated PKM2 is non-oncogenic...
February 12, 2018: Cancer Research
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