Genomes and Genes
Summary: A genus of the family Muridae consisting of eleven species. C. migratorius, the grey or Armenian hamster, and C. griseus, the Chinese hamster, are the two species used in biomedical research.
- Velez Suberbie M, Tarrant R, Tait A, Spencer D, Bracewell D. Impact of aeration strategy on CHO cell performance during antibody production. Biotechnol Prog. 2013;29:116-26 pubmed publisher..These physiological changes only result in a difference in continuous centrifugation performance under high flow rate conditions. Product quality was more strongly affected by culture age than the hydrodynamic conditions tested...
- Takagi S, Sato S, Oh hara T, Takami M, Koike S, Mishima Y, et al. Platelets promote tumor growth and metastasis via direct interaction between Aggrus/podoplanin and CLEC-2. PLoS ONE. 2013;8:e73609 pubmed publisher..Our results indicate that molecular target drugs inhibiting specific platelet-tumor interactions can be developed as antitumor drugs that suppress both metastasis and proliferation of tumors such as lung squamous cell carcinoma. ..
- Dong M, Xu X, Ball A, Makhoul J, Lam P, Pinon D, et al. Mapping spatial approximations between the amino terminus of secretin and each of the extracellular loops of its receptor using cysteine trapping. FASEB J. 2012;26:5092-105 pubmed publisher..Key spatial approximations between peptide and receptor predicted by this model (H(1)-W(274), D(3)-N(268), G(4)-F(258)) were supported by mutagenesis and residue-residue complementation studies...
- Jung J, Ladd T, Kukar T, Price A, Moore B, Koo E, et al. Steroids as ?-secretase modulators. FASEB J. 2013;27:3775-85 pubmed publisher..They also indicate that acidic steroids might serve as potential therapeutic leads for drug optimization/development...
- Matsumura N, Takami M, Okochi M, Wada Kakuda S, Fujiwara H, Tagami S, et al. ?-Secretase associated with lipid rafts: multiple interactive pathways in the stepwise processing of ?-carboxyl-terminal fragment. J Biol Chem. 2014;289:5109-21 pubmed publisher..These observations indicate that multiple interactive pathways for stepwise successive processing by ?-secretase define the species and quantity of A? produced. ..
- Templeton N, Dean J, Reddy P, YOUNG J. Peak antibody production is associated with increased oxidative metabolism in an industrially relevant fed-batch CHO cell culture. Biotechnol Bioeng. 2013;110:2013-24 pubmed publisher..Overall, we found that a highly oxidative state of metabolism corresponded with peak antibody production, whereas peak cell growth was characterized by a highly glycolytic metabolic state...
- Kouprina N, Samoshkin A, Erliandri I, Nakano M, Lee H, Fu H, et al. Organization of synthetic alphoid DNA array in human artificial chromosome (HAC) with a conditional centromere. ACS Synth Biol. 2012;1:590-601 pubmed..The knowledge of the alphoid(tetO)-HAC structure provides a tool to control HAC integrity during different manipulations. Our results also shed light on a mechanism for de novo HAC formation in human cells...
- Wootten D, Savage E, Willard F, Bueno A, Sloop K, Christopoulos A, et al. Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecule ligands. Mol Pharmacol. 2013;83:822-34 pubmed publisher..This could enable the design and development of improved therapeutics that have the ability to fine-tune receptor signaling, leading to beneficial therapeutic outcomes while reducing side effect profiles...
- Baycin Hizal D, Tabb D, Chaerkady R, Chen L, Lewis N, Nagarajan H, et al. Proteomic analysis of Chinese hamster ovary cells. J Proteome Res. 2012;11:5265-76 pubmed publisher..This first large-scale proteomic analysis will enhance the knowledge base about CHO capabilities for recombinant expression and provide information useful in cell engineering efforts aimed at modifying CHO cellular functions...
- Ran Y, Cruz P, Ladd T, Fauq A, Jung J, Matthews J, et al. ?-Secretase processing and effects of ?-secretase inhibitors and modulators on long A? peptides in cells. J Biol Chem. 2014;289:3276-87 pubmed publisher..These studies also raise interesting issues about the solubility and detection of long A?, as well as the use of truncated substrates for assessing relative potency of ?-secretase inhibitors. ..
- Bailey L, Hatton D, Field R, Dickson A. Determination of Chinese hamster ovary cell line stability and recombinant antibody expression during long-term culture. Biotechnol Bioeng. 2012;109:2093-103 pubmed..Definition of the mechanisms, regulatory events, and linkages underpinning cellular phenotype changes require further detailed analysis at a molecular level...
- Edros R, McDonnell S, Al Rubeai M. Using molecular markers to characterize productivity in Chinese hamster ovary cell lines. PLoS ONE. 2013;8:e75935 pubmed publisher..Since the correlation varied from day to day during batch cultivation, single-point measurement was of limited use in making a reliable prediction. ..
- Augustin E, Borowa Mazgaj B, Kikulska A, Kordalewska M, Pawłowska M. CYP3A4 overexpression enhances the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in CHO cells. Acta Pharmacol Sin. 2013;34:146-56 pubmed publisher..To examine how the higher expression level of CYP3A4 isoenzyme influenced the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in Chinese hamster ovary (CHO) cells...
- Bayliss A, Evans P. Characterisation of AmphiAmR4, an amphioxus (Branchiostoma floridae) ??-adrenergic-like G-protein-coupled receptor. Invert Neurosci. 2013;13:71-84 pubmed publisher..Pharmacological studies with a wide range of agonists and antagonists suggest that AmphiAmR4 functions as an ??-adrenergic-like receptor when expressed in CHO cells...
- Druz A, Son Y, Betenbaugh M, Shiloach J. Stable inhibition of mmu-miR-466h-5p improves apoptosis resistance and protein production in CHO cells. Metab Eng. 2013;16:87-94 pubmed publisher..The above results demonstrate the potential of this novel approach to create more productive cell lines through stable manipulation of specific miRNA expression. ..
- Evdokimov A, Petruseva I, Tsidulko A, Koroleva L, Serpokrylova I, Silnikov V, et al. New synthetic substrates of mammalian nucleotide excision repair system. Nucleic Acids Res. 2013;41:e123 pubmed publisher..The new synthetic extended linear DNA containing bulky non-nucleoside modifications will be useful for NER mechanism study and for applications...
- Makarikov A, Mel nikova Y, Tkach V. Description and phylogenetic affinities of two new species of Nomadolepis (Eucestoda, Hymenolepididae) from Eastern Palearctic. Parasitol Int. 2015;64:453-63 pubmed publisher..Nomadolepis fareasta n. sp. is described from the striped dwarf hamster Cricetulus barabensis in Amurskaya Oblast' and Nomadolepis shiloi n. sp...
- Fracassi C, Postiglione L, Fiore G, di Bernardo D. Automatic Control of Gene Expression in Mammalian Cells. ACS Synth Biol. 2016;5:296-302 pubmed publisher..We demonstrated that both the relay and PI controllers can regulate gene expression at the desired level, despite oscillations (dampened in the case of the PI controller) around the chosen set point. ..
- He H, Deng K, Siddiq M, Pyie A, Mellado W, Hannila S, et al. Cyclic AMP and Polyamines Overcome Inhibition by Myelin-Associated Glycoprotein through eIF5A-Mediated Increases in p35 Expression and Activation of Cdk5. J Neurosci. 2016;36:3079-91 pubmed publisher..Our findings reveal a previously unknown mechanism by which polyamines may encourage regeneration after CNS injury. ..
- Sezgin E, Azbazdar Y, Ng X, Teh C, Simons K, Weidinger G, et al. Binding of canonical Wnt ligands to their receptor complexes occurs in ordered plasma membrane environments. FEBS J. 2017;284:2513-2526 pubmed publisher..We thus conclude that ordered plasma membrane environments are essential for binding of canonical Wnts to their receptor complexes and downstream signaling activity. ..
- Treiber A, de Kanter R, Roch C, Gatfield J, Boss C, von Raumer M, et al. The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468. J Pharmacol Exp Ther. 2017;362:489-503 pubmed publisher..PBPK-PD modeling applied early in drug discovery, therefore, has great potential to assist in the identification of drug molecules when specific pharmacokinetic and pharmacodynamic requirements need to be met. ..
- Patil R, Xu S, Van Hoek A, Rusinko A, Feng Z, May J, et al. Rapid Identification of Novel Inhibitors of the Human Aquaporin-1 Water Channel. Chem Biol Drug Des. 2016;87:794-805 pubmed publisher..Validation of these lead compounds, by the three independent assays, establishes a set of attractive AQP1 blockers for developing novel, small-molecule functional modulators of human AQP1. ..
- Mistry S, Lim H, Jörg M, Capuano B, Christopoulos A, Lane J, et al. Novel Fused Arylpyrimidinone Based Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor. ACS Chem Neurosci. 2016;7:647-61 pubmed publisher..As such, the quinazolin-4(3H)-one core represents a novel scaffold to further explore M1 mAChR PAMs with improved physicochemical properties. ..
- Damavandi N, Raigani M, Joudaki A, Davami F, Zeinali S. Rapid characterization of the CHO platform cell line and identification of pseudo attP sites for PhiC31 integrase. Protein Expr Purif. 2017;140:60-64 pubmed publisher..The characterized platform cell lines are stable, and because of single-copy, site-specific R4 recognition attP site, the cell lines could be retargeted for recombinant protein production and drug discovery applications. ..
- Hu K, He S, Xiao J, Li M, Luo S, Zhang M, et al. Interaction between herpesvirus entry mediator and HSV-2 glycoproteins mediates HIV-1 entry of HSV-2-infected epithelial cells. J Gen Virol. 2017;98:2351-2361 pubmed publisher..Our findings provide a potential new mechanism underlying HSV-2 infection-enhanced HIV-1 mucosal transmission and may shed light on HIV-1 prevention. ..
- Erli F, Guerrieri E, Ben Haddou T, Lantero A, Mairegger M, Schmidhammer H, et al. Highly Potent and Selective New Diphenethylamines Interacting with the ?-Opioid Receptor: Synthesis, Pharmacology, and Structure-Activity Relationships. J Med Chem. 2017;60:7579-7590 pubmed publisher..The new diphenethylamines displayed antinociceptive efficacies with increased potencies than U50,488, 1 and 2 in the writhing assay and without inducing motor dysfunction after sc administration in mice. ..
- Eyer K, Doineau R, Castrillon C, Briseño Roa L, Menrath V, Mottet G, et al. Single-cell deep phenotyping of IgG-secreting cells for high-resolution immune monitoring. Nat Biotechnol. 2017;35:977-982 pubmed publisher..This system will not only enable immune monitoring and optimization of immunization and vaccination protocols but also potentiate antibody screening. ..
- ZieliÅ„ski M, WÃ³jtowicz Krawiec A, Mikiewicz D, KÄ™sik Brodacka M, Cecuda Adamczewska V, Marciniak Rusek A, et al. Expression of recombinant human bifunctional peptidylglycine Î±-amidating monooxygenase in CHO cells and its use for insulin analogue modification. Protein Expr Purif. 2016;119:102-9 pubmed publisher..GKR-NH2 is a candidate for a hypoglycemic drug product in diabetes care. In addition, this work also provides a valuable alternative method for preparing any other recombinant bioactive peptides with C-terminal amidation. ..
- Okazaki H, Takeda S, Matsuo S, Matsumoto M, Furuta E, Kohro Ikeda E, et al. Inhibitory modulation of human estrogen receptor ? and ? activities by dicyclohexyl phthalate in human breast cancer cell lines. J Toxicol Sci. 2017;42:417-425 pubmed publisher..The results of the present study suggest that PAEs (DCHP) function not only as an anti-estrogen for ER?, but also for ER?, at least in human breast cancer cell lines. ..
- Kudlinzki D, Linhard V, Saxena K, Sreeramulu S, Gande S, Schieborr U, et al. High-resolution crystal structure of cAMP-dependent protein kinase from Cricetulus griseus. Acta Crystallogr F Struct Biol Commun. 2015;71:1088-93 pubmed publisher..In order to resolve such minor structural differences, very high resolution structures are required. Here, the high-resolution X-ray structure of PKAc from Cricetulus griseus is reported.
- Bjerregaard Olesen C, Ghisari M, Kjeldsen L, WielsÃ¸e M, Bonefeld JÃ¸rgensen E. Estrone sulfate and dehydroepiandrosterone sulfate: Transactivation of the estrogen and androgen receptor. Steroids. 2016;105:50-8 pubmed publisher..The AR transactivity of the sulfated steroids in the extracts was abolished by STX64 to obtain the net PFAA induced xenohormone transactivity, but further cleanup might be needed at high concentrations of E1S. ..
- Arawaka S, Sato H, Sasaki A, Koyama S, Kato T. Mechanisms underlying extensive Ser129-phosphorylation in Î±-synuclein aggregates. Acta Neuropathol Commun. 2017;5:48 pubmed publisher..However, Ser129-phosphorylation may provide an ineffective signal for degradation-resistant aggregates, causing extensive phosphorylation in aggregates. ..
- Stoyle C, Stephens P, Humphreys D, Heywood S, Cain K, Bulleid N. IgG light chain-independent secretion of heavy chain dimers: consequence for therapeutic antibody production and design. Biochem J. 2017;474:3179-3188 pubmed publisher..This discovery will have an impact on the efficient production of both humanised antibodies and the design of novel antibody formats. ..
- Peng L, Yu X, Li C, Cai Y, Chen Y, He Y, et al. Enhanced recombinant factor VII expression in Chinese hamster ovary cells by optimizing signal peptides and fed-batch medium. Bioengineered. 2016;7:189-97 pubmed publisher..Our data may be used to improve the production of other therapeutic proteins in fed-batch culture. ..
- Deng R, Bumbaca D, Pastuskovas C, Boswell C, West D, Cowan K, et al. Preclinical pharmacokinetics, pharmacodynamics, tissue distribution, and tumor penetration of anti-PD-L1 monoclonal antibody, an immune checkpoint inhibitor. MAbs. 2016;8:593-603 pubmed publisher..These data also allowed for estimation of the target clinical dose for further development of MPDL3280A. ..
- Burger K, Ilicic K, Dierolf M, Günther B, Walsh D, Schmid E, et al. Increased cell survival and cytogenetic integrity by spatial dose redistribution at a compact synchrotron X-ray source. PLoS ONE. 2017;12:e0186005 pubmed publisher..Our findings provide valuable insight into the mechanisms of microbeam radiotherapy and prove its applicability at a compact synchrotron, which contributes to its future clinical translation...
- Diana T, Krause J, Olivo P, Konig J, Kanitz M, Decallonne B, et al. Prevalence and clinical relevance of thyroid stimulating hormone receptor-blocking antibodies in autoimmune thyroid disease. Clin Exp Immunol. 2017;189:304-309 pubmed publisher..Functional TSHR antibodies impact thyroid status. TBAb determination is helpful in the evaluation and management of patients with AITD. The TBAb assay is a relevant and important tool to identify potentially reversible hypothyroidism. ..
- Console Bram L, Ciuciu S, Zhao P, Zipkin R, Brailoiu E, Abood M. N-arachidonoyl glycine, another endogenous agonist of GPR55. Biochem Biophys Res Commun. 2017;490:1389-1393 pubmed publisher..To our knowledge this is the first report identifying GPR55 as a target of the endogenous lipoamino acid, NAGly. ..
- Zavec A, Kralj IgliÄ V, Brinc M, TrÄek T, Kuzman D, Schweiger A, et al. Extracellular vesicles concentration is a promising and important parameter for industrial bioprocess monitoring. Biotechnol J. 2016;11:603-9 pubmed publisher..Therefore, we suggest EV concentration as a new and important parameter for the monitoring of industrial bioprocesses. ..
- Zhironkina O, Kurchashova S, Pozharskaia V, Cherepanynets V, Strelkova O, Hozak P, et al. Mechanisms of nuclear lamina growth in interphase. Histochem Cell Biol. 2016;145:419-32 pubmed publisher..We suggest that in somatic cells lamin B1 meshwork growth is coordinated with replication of LADs, and lamin A meshwork assembly seems to be chromatin-independent process. ..
- Uchida R, Namiguchi S, Ishijima H, Tomoda H. Therapeutic effects of three trichothecenes in the silkworm infection assay with Candida albicans. Drug Discov Ther. 2016;10:44-8 pubmed publisher..These results strongly suggest that trichodermin and epiisororidin E are the lead compounds for developing a new antifungal agent. ..
- Panicker S, Mehta D souza P, Zhang N, Klopocki A, Shao B, McEver R. Circulating soluble P-selectin must dimerize to promote inflammation and coagulation in mice. Blood. 2017;130:181-191 pubmed publisher..Furthermore, transgenic mice that overexpressed monomeric sP-selectin did not exhibit increased inflammation or thrombosis. We conclude that elevated plasma sP-selectin is a consequence rather than a cause of cardiovascular disease. ..
- Rençber S, Karavana S, Yilmaz F, Erac B, Nenni M, Ozbal S, et al. Development, characterization, and in vivo assessment of mucoadhesive nanoparticles containing fluconazole for the local treatment of oral candidiasis. Int J Nanomedicine. 2016;11:2641-53 pubmed publisher..This study has shown that the mucoadhesive NP formulation containing fluconazole is a promising candidate with once-a-day application for the local treatment of oral candidiasis. ..
- Yuksel M, Biberoglu K, Onder S, Akbulut K, Tacal O. Effects of phenothiazine-structured compounds on APP processing in Alzheimer's disease cellular model. Biochimie. 2017;138:82-89 pubmed publisher..Taken together, our results represent the first report demonstrating that TBO and TH can affect amyloid metabolism in vitro. ..
- Brown P, Bromberg L, Rial Hermida M, Wasbrough M, Hatton T, Alvarez Lorenzo C. Magnetic Surfactants and Polymers with Gadolinium Counterions for Protein Separations. Langmuir. 2016;32:699-705 pubmed publisher..Importantly, the toxicity of the magnetic surfactants and polymers is, in some cases, lower than that of their halide analogues. ..
- Chatterjee S, Lesniak W, Gabrielson M, Lisok A, Wharram B, Sysa Shah P, et al. A humanized antibody for imaging immune checkpoint ligand PD-L1 expression in tumors. Oncotarget. 2016;7:10215-27 pubmed publisher..Specificity of NIR-PD-L1-mAb indicates the potential for optical imaging of PD-L1 expression in tumors in relevant pre-clinical as well as clinical settings. ..
- Chromikova V, Zaragoza M, Krammer F. Generation of a serum free CHO DG44 cell line stably producing a broadly protective anti-influenza virus monoclonal antibody. PLoS ONE. 2017;12:e0183315 pubmed publisher..Here, we report the development of a serum-free CHO DG44 cell line, stably producing a CR9114-like antibody with a potential to become a useful influenza virus research tool...
- Wu J, Han D, Wei M, Zheng G, Jiao D, Xi W, et al. [Domestication of suspension CHO cells and its application in the expression of anti-PSMA antibody]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2016;32:1-4 pubmed..CHO-S cel s were successful y domesticated from adherent CHO cells, and could be used for antibody expression. This study provided a useful tool for further antibody expression, purification and function study. ..
- Zouaoui N, Mallebrera B, Berrada H, Abid Essefi S, Bacha H, Ruiz M. Cytotoxic effects induced by patulin, sterigmatocystin and beauvericin on CHO-K1 cells. Food Chem Toxicol. 2016;89:92-103 pubmed publisher..Our results indicate that the co-occurrence of low concentrations of mycotoxin in food may increase their toxic effects. ..
- Doornbos M, Cid J, Haubrich J, Nunes A, van de Sande J, Vermond S, et al. Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2. J Med Chem. 2017;60:6704-6720 pubmed publisher..These results show that affinity-only driven selection would have resulted in mGlu2 PAMs with high values for kon but not necessarily optimized RT, which is key to predicting optimal efficacy in vivo...
- Nagata N, Iwanari H, Kumagai H, Kusano Arai O, Ikeda Y, Aritake K, et al. Generation and characterization of an antagonistic monoclonal antibody against an extracellular domain of mouse DP2 (CRTH2/GPR44) receptors for prostaglandin D2. PLoS ONE. 2017;12:e0175452 pubmed publisher..This monoclonal antibody will be very useful for in vitro and in vivo studies on DP2-mediated diseases...
- Hanigan D, Truong L, Simonich M, Tanguay R, Westerhoff P. Zebrafish embryo toxicity of 15 chlorinated, brominated, and iodinated disinfection by-products. J Environ Sci (China). 2017;58:302-310 pubmed publisher..We find zebrafish development to be a viable in vivo alternative or confirmatory assay to mammalian in vitro cell assays. ..
- Ahmadi S, Davami F, Davoudi N, Nematpour F, Ahmadi M, Ebadat S, et al. Monoclonal antibodies expression improvement in CHO cells by PiggyBac transposition regarding vectors ratios and design. PLoS ONE. 2017;12:e0179902 pubmed publisher..The results were dependent on both donor vector design and vectors ratios. ..
- Houde D, Nazari Z, Bou Assaf G, Weiskopf A, Rand K. Conformational Analysis of Proteins in Highly Concentrated Solutions by Dialysis-Coupled Hydrogen/Deuterium Exchange Mass Spectrometry. J Am Soc Mass Spectrom. 2016;27:669-76 pubmed publisher..Such a method could pave the way for a deeper understanding of the unusual behavior of proteins at high concentrations, which is highly relevant for development of biopharmaceuticals in industry. Graphical Abstract á…Ÿ. ..
- Gao Z, Zhang H, Hu F, Yang L, Yang X, Zhu Y, et al. Glycan-deficient PrP stimulates VEGFR2 signaling via glycosaminoglycan. Cell Signal. 2016;28:652-62 pubmed publisher..Based on these findings, we propose a model in which glycan-deficient PrP, GAG, and VEGFR2 interact, activating VEGFR2 and resulting in changes in cellular behavior. ..
- Potluri P, Procaccio V, Scheffler I, Wallace D. High throughput gene complementation screening permits identification of a mammalian mitochondrial protein synthesis (Ï(-)) mutant. Biochim Biophys Acta. 2016;1857:1336-1343 pubmed publisher..This article is part of a Special Issue entitled 'EBEC 2016: 19th European Bioenergetics Conference, Riva del Garda, Italy, July 2-6, 2016', edited by Prof. Paolo Bernardi. ..
- Ishikawa K, Karaki F, Tayama K, Higashi E, Hirayama S, Itoh K, et al. C-Homomorphinan Derivatives as Lead Compounds to Obtain Safer and More Clinically Useful Analgesics. Chem Pharm Bull (Tokyo). 2017;65:920-929 pubmed publisher..From these results, we concluded that cyclized C-homomorphinan would be a possible lead compound to obtain novel analgesics with buprenorphine-like properties...
- Oyane A, Araki H, Nakamura M, Shimizu Y, Shubhra Q, Ito A, et al. Controlled superficial assembly of DNA-amorphous calcium phosphate nanocomposite spheres for surface-mediated gene delivery. Colloids Surf B Biointerfaces. 2016;141:519-527 pubmed publisher..As demonstrated herein, controlling the coprecipitation conditions is important for designing a cell-stimulating and biocompatible scaffold surface consisting of an assembly of DNA-ACP nanocomposite spheres. ..
- Li D, Wei J, Yang F, Liu H, Zhu Z, Cao W, et al. Foot-and-mouth disease virus structural protein VP3 degrades Janus kinase 1 to inhibit IFN-Î³ signal transduction pathways. Cell Cycle. 2016;15:850-60 pubmed publisher..Taken together, the results reveal a novel mechanism used by which FMDV VP3 counteracts the type II IFN signaling pathways. ..
- Hecklau C, Pering S, Seibel R, Schnellbaecher A, Wehsling M, Eichhorn T, et al. S-Sulfocysteine simplifies fed-batch processes and increases the CHO specific productivity via anti-oxidant activity. J Biotechnol. 2016;218:53-63 pubmed publisher..Finally, we propose that the increase in specific productivity obtained in the S-sulfocysteine process results from the anti-oxidative properties of the molecule. ..
- Kim Y, Kwak M, Park J, Lee S, Choi J, Cho H, et al. N-linked glycosylation plays a crucial role in the secretion of HMGB1. J Cell Sci. 2016;129:29-38 pubmed publisher..Taken together, we propose that HMGB1 is N-glycosylated, and that this is important for its DNA interaction and is a prerequisite for its nucleocytoplasmic transport and extracellular secretion. ..
- Yan Q, Ding N, Li Y. Synthesis and biological evaluation of novel dioxa-bicycle C-aryl glucosides as SGLT2 inhibitors. Carbohydr Res. 2016;421:1-8 pubmed publisher..Among the compounds tested, compound 6a showed moderate SGLT2 inhibition activities at 700â€‰nM. The results could benefit the discovery of new SGLT2 inhibitors. ..
- Zhang J, Li X, Zhou Y, Cui L, Li J, Wu C, et al. The interaction of MC3R and MC4R with MRAP2, ACTH, ?-MSH and AgRP in chickens. J Endocrinol. 2017;234:155-174 pubmed publisher..Furthermore, our data provide novel proof for the involvement of MRAP2 (and MRAP) in fine-tuning the constitutive activity and ligand sensitivity and selectivity of both MC3R and MC4R in vertebrates. ..
- Yadav R, Bansal R, Rohilla S, Kachler S, Klotz K. Synthesis and pharmacological characterization of novel xanthine carboxylate amides as A2A adenosine receptor ligands exhibiting bronchospasmolytic activity. Bioorg Chem. 2016;65:26-37 pubmed publisher..06Î¼M. Similarly potent and highly A2A-selective are the isovanillin derivatives 16a and 16d. In addition, the newly synthesized xanthine derivatives showed good in vivo bronchospasmolytic activity when tested in guinea pigs. ..
- Lan H, Hong P, Li R, L S, Anshan S, Li S, et al. Internal image anti-idiotypic antibody: A new strategy for the development a new category of prolactin receptor (PRLR) antagonist. Mol Immunol. 2017;87:86-93 pubmed publisher..In addition, this work also suggests that the internal image anti-idiotypic antibody may represent a novel strategy for the development of PRLR antagonist. ..
- Maiwald A, Bauer O, Gimpl G. Synthesis and characterization of a novel rhodamine labeled cholesterol reporter. Biochim Biophys Acta Biomembr. 2017;1859:1099-1113 pubmed publisher..Instead, it translocated to endosomes/lysosomes with some transient contacts to peroxisomes. Thus, RChol is considered as a useful probe to study the endosomal/lysosomal pathway of cholesterol. ..
- Prabhu A, Luu W, Sharpe L, Brown A. Cholesterol-mediated Degradation of 7-Dehydrocholesterol Reductase Switches the Balance from Cholesterol to Vitamin D Synthesis. J Biol Chem. 2016;291:8363-73 pubmed publisher..Thus, these findings highlight DHCR7 as an important regulatory switch between cholesterol and vitamin D synthesis. ..
- Adams M, Barnard L, de Kock C, Smith P, Wiesner L, Chibale K, et al. Cyclopalladated organosilane-tethered thiosemicarbazones: novel strategies for improving antiplasmodial activity. Dalton Trans. 2016;45:5514-20 pubmed publisher..Cyclopalladation of the thiosemicarbazones resulted in antiplasmodial activities in the low micromolar range. ..
- Lu X, He L, Zhou Q, Wang M, Shen W, Azhar S, et al. NHERF1 and NHERF2 regulation of SR-B1 stability via ubiquitination and proteasome degradation. Biochem Biophys Res Commun. 2017;490:1168-1175 pubmed publisher..NHERF1 and NHERF2 promote SR-B1 ubiquitination at sites K508 and K500, respectively. These results suggest that NHERF1 and NHERF2 down-regulated SR-B1 at least in part via the ubiquitin/proteasome pathway. ..
- Kerr A, Tam L, Hale A, Cioroch M, Douglas G, Agkatsev S, et al. A Genomic DNA Reporter Screen Identifies Squalene Synthase Inhibitors That Act Cooperatively with Statins to Upregulate the Low-Density Lipoprotein Receptor. J Pharmacol Exp Ther. 2017;361:417-428 pubmed publisher..Overall, we demonstrated here a novel series of small molecules with the potential to be further developed to treat patients either alone or in combination with statins. ..
- Dangoumau A, Marouillat S, Burlaud Gaillard J, Uzbekov R, Veyrat Durebex C, Blasco H, et al. Inhibition of Pathogenic Mutant SOD1 Aggregation in Cultured Motor Neuronal Cells by Prevention of Its SUMOylation on Lysine 75. Neurodegener Dis. 2016;16:161-71 pubmed publisher..These results support the need for further research on the SUMOylation pathways, which may be a potential therapeutic target in ALS. ..
- González Tarragó V, Elosegui Artola A, Bazellieres E, Oria R, Pérez González C, Roca Cusachs P. Binding of ZO-1 to ?5?1 integrins regulates the mechanical properties of ?5?1-fibronectin links. Mol Biol Cell. 2017;28:1847-1852 pubmed publisher..Taken together, our results unveil a new mode of integrin regulation through modification of the mechanical properties of integrin-ECM links, which may be harnessed by cells to control adhesion and migration. ..