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Journal articles on the topic 'Ligene'

Author: Grafiati

Published: 18 August 2021

Last updated: 29 July 2025

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1

Fanucci, Francesco. "Quaternary shorelines and continental shelf of the Ligurian coast." Zeitschrift für Geomorphologie 31, no. 4 (1987): 463–72. http://dx.doi.org/10.1127/zfg/31/1987/463.

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2

Pearson, Margot N., and George F. Rohrmann. "Characterization of a Baculovirus-Encoded ATP-Dependent DNA Ligase." Journal of Virology 72, no. 11 (1998): 9142–49. http://dx.doi.org/10.1128/jvi.72.11.9142-9149.1998.

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ABSTRACT Sequence analysis of the Lymantria dispar multicapsid nucleopolyhedrovirus (LdMNPV) genome identified an open reading frame (ORF) encoding a 548-amino-acid (62-kDa) protein that showed 35% amino acid sequence identity with vaccinia virus ATP-dependent DNA ligase. Ligase homologs have not been reported from other baculoviruses. The ligase ORF was cloned and expressed as an N-terminal histidine-tagged fusion protein. Incubation of the purified protein with [α-32P]ATP resulted in formation of a covalent enzyme-adenylate intermediate which ran as a 62-kDa labeled band on a sodium dodecyl

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3

Lee, Jaeseok, Youngjun Lee, Young Mee Jung, Ju Hyun Park, Hyuk Sang Yoo, and Jongmin Park. "Discovery of E3 Ligase Ligands for Target Protein Degradation." Molecules 27, no. 19 (2022): 6515. http://dx.doi.org/10.3390/molecules27196515.

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Target protein degradation has emerged as a promising strategy for the discovery of novel therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a cellular ubiquitin-dependent proteolysis system for the efficient degradation of a protein of interest. PROTAC consists of a target protein ligand and an E3 ligase ligand so that it enables the target protein degradation owing to the induced proximity with ubiquitin ligases. Although a great number of PROTACs has been developed so far using previously reported ligands of proteins for their degradation, E3 ligase ligand

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4

Lam, Polo C. H., Ruben Abagyan, and Maxim Totrov. "Ligand-biased ensemble receptor docking (LigBEnD): a hybrid ligand/receptor structure-based approach." Journal of Computer-Aided Molecular Design 32, no. 1 (2017): 187–98. http://dx.doi.org/10.1007/s10822-017-0058-x.

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5

Collantes, Ezequiel. "La estructura de entramado ligero como recurso proyectual en la obra de Frank O. Gehry (1978-1997)." VLC arquitectura. Research Journal 10, no. 1 (2023): 1–23. http://dx.doi.org/10.4995/vlc.2023.17086.

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Este artículo analiza el papel de la estructura ligera como recurso proyectual en la obra de Frank Gehry entre 1978 y 1997. El artículo realiza un análisis histórico-crítico de su obra en este periodo, en el que se identifican tres etapas diferentes. La primera etapa (1978-1987) incluye los proyectos domésticos en los que Gehry desarrolló diversas operaciones agregativas simples basadas en el entramado ligero. La segunda etapa (1983-1992) incluye los proyectos Fish, caracterizados por la búsqueda de formas complejas a través de la manipulación del entramado ligero. La tercera y última etapa (1

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Sharma, Chiranjeev, Myeong A. Choi, Yoojin Song, and Young Ho Seo. "Rational Design and Synthesis of HSF1-PROTACs for Anticancer Drug Development." Molecules 27, no. 5 (2022): 1655. http://dx.doi.org/10.3390/molecules27051655.

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PROTACs employ the proteosome-mediated proteolysis via E3 ligase and recruit the natural protein degradation machinery to selectively degrade the cancerous proteins. Herein, we have designed and synthesized heterobifunctional small molecules that consist of different linkers tethering KRIBB11, a HSF1 inhibitor, with pomalidomide, a commonly used E3 ligase ligand for anticancer drug development.

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Kounde, Cyrille S., Maria M. Shchepinova, Charlie N. Saunders, et al. "A caged E3 ligase ligand for PROTAC-mediated protein degradation with light." Chemical Communications 56, no. 41 (2020): 5532–35. http://dx.doi.org/10.1039/d0cc00523a.

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Cipriano Bautista, Johnny Gregorio. "Pronóstico del Caudal de La Cuenca del Rio Huaura Mediante un Sistema de Inferencia Difuso, Basado en Precipitaciones." Ciencia Latina Revista Científica Multidisciplinar 8, no. 3 (2024): 7358–66. http://dx.doi.org/10.37811/cl_rcm.v8i3.11929.

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El presente trabajo de investigación tiene como objetivo, pronosticar el caudal de la cuenca del rio Huaura mediante un sistema de inferencia difuso basado en precipitaciones. El Método de Investigación es Descriptivo – proposicional. El diseño de investigación es de tipo no experimental. En las precipitaciones pluviales se han considerado cuatro variables de entrada: Lluvias (muy ligero, ligero, moderada baja, moderada media, moderada, fuerte y muy fuerte), Llovizna (muy ligeras, ligero, moderada baja, moderada media, moderada, fuerte y muy fuerte), granizo (pequeño, mediano A, mediano B, med

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9

Gu, Jiafeng, Haihui Lu, Brigette Tippin, Noriko Shimazaki, Myron F. Goodman, and Michael R. Lieber. "XRCC4:DNA ligase IV can ligate incompatible DNA ends and can ligate across gaps." EMBO Journal 26, no. 4 (2007): 1010–23. http://dx.doi.org/10.1038/sj.emboj.7601559.

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10

Gu, Jiafeng, Haihui Lu, Brigette Tippin, Noriko Shimazaki, Myron F. Goodman, and Michael R. Lieber. "XRCC4:DNA ligase IV can ligate incompatible DNA ends and can ligate across gaps." EMBO Journal 26, no. 14 (2007): 3506–7. http://dx.doi.org/10.1038/sj.emboj.7601729.

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11

Ohtake, Fumiaki, Atsushi Baba, Ichiro Takada, et al. "Dioxin receptor is a ligand-dependent E3 ubiquitin ligase." Nature 446, no. 7135 (2007): 562–66. http://dx.doi.org/10.1038/nature05683.

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12

Kim, Kang Ho, Jeong Min Yoon, A. Hyun Choi, Woo Sik Kim, Gha Young Lee та Jae Bum Kim. "Liver X Receptor Ligands Suppress Ubiquitination and Degradation of LXRα by Displacing BARD1/BRCA1". Molecular Endocrinology 23, № 4 (2009): 466–74. http://dx.doi.org/10.1210/me.2008-0295.

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Abstract Liver X receptor (LXR) is a ligand-activated transcription factor that plays important roles in cholesterol and lipid homeostasis. However, ligand-induced posttranslational modification of LXR is largely unknown. Here, we show that ligand-free LXRα is rapidly degraded by ubiquitination. Without ligand, LXRα interacts with an ubiquitin E3-ligase protein complex containing breast and ovarian cancer susceptibility 1 (BRCA1)-associated RING domain 1 (BARD1). Interestingly, LXR ligand represses ubiquitination and degradation of LXRα, and the interaction between LXRα and BARD1 is inhibited

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Tateishi, Yukiyo, Raku Sonoo, Yu-ichi Sekiya та ін. "Turning Off Estrogen Receptor β-Mediated Transcription Requires Estrogen-Dependent Receptor Proteolysis". Molecular and Cellular Biology 26, № 21 (2006): 7966–76. http://dx.doi.org/10.1128/mcb.00713-06.

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ABSTRACT Recent studies have shed light on the ligand-dependent transactivation mechanisms of nuclear receptors (NRs). When the ligand dose is reduced, the transcriptional activity of NRs should be downregulated. Here we show that a ubiquitin-proteasome pathway plays a key role in turning off transcription mediated by estrogen receptor β (ERβ). ERβ shows estrogen-dependent proteolysis, and its degradation is regulated by two regions in the receptor. The N-terminal 37-amino acid-region is necessary for the recruitment of the ubiquitin ligase, i.e., the carboxyl terminus of HSC70-interacting pro

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Yan, Yuqian, Jingwei Shao, Donglin Ding, et al. "3-Aminophthalic acid, a new cereblon ligand for targeted protein degradation by O’PROTAC." Chemical Communications 58, no. 14 (2022): 2383–86. http://dx.doi.org/10.1039/d1cc06525d.

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In this study, we discovered 3-aminophthalic acid as a new ligand of cereblon (CRBN) E3 ubiquitin ligase and developed a phthalic acid-based O’PROTAC for ERG destruction, expanding the pool of ligands for development of PROTACs, especially O’PROTACs.

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Ziemienowicz, Alicja, Bruno Tinland, John Bryant, Veronique Gloeckler, and Barbara Hohn. "Plant Enzymes but Not AgrobacteriumVirD2 Mediate T-DNA Ligation In Vitro." Molecular and Cellular Biology 20, no. 17 (2000): 6317–22. http://dx.doi.org/10.1128/mcb.20.17.6317-6322.2000.

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ABSTRACT Agrobacterium tumefaciens, a gram-negative soil bacterium, transfers DNA to many plant species. In the plant cell, the transferred DNA (T-DNA) is integrated into the genome. An in vitro ligation-integration assay has been designed to investigate the mechanism of T-DNA ligation and the factors involved in this process. The VirD2 protein, which is produced in Agrobacterium and is covalently attached to T-DNA, did not, under our assay conditions, ligate T-DNA to a model target sequence in vitro. We tested whether plant extracts could ligate T-DNA to target oligonucleotides in our test sy

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16

Koo, Bon-Kyoung, Ki-Jun Yoon, Kyeong-Won Yoo, et al. "Mind Bomb-2 Is an E3 Ligase for Notch Ligand." Journal of Biological Chemistry 280, no. 23 (2005): 22335–42. http://dx.doi.org/10.1074/jbc.m501631200.

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The zebrafish gene, mind bomb (mib), encodes a protein that positively regulates of the Delta-mediated Notch signaling. It interacts with the intracellular domain of Delta to promote its ubiquitination and endocytosis. In our search for the mouse homologue of zebrafish mind bomb, we cloned two homologues in the mouse genome: a mouse orthologue (mouse mib1) and a paralogue, named mind bomb-2 (mib2), which is evolutionarily conserved from Drosophila to human. Both Mib1 and Mib2 have an E3 ubiquitin ligase activity in their C-terminal RING domain and interact with Xenopus Delta (XD) via their N-t

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Omari, Kamel El, Jingshan Ren, Louise E. Bird, et al. "Molecular Architecture and Ligand Recognition Determinants for T4 RNA Ligase." Journal of Biological Chemistry 281, no. 3 (2005): 1573–79. http://dx.doi.org/10.1074/jbc.m509658200.

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18

Reynders, Martin, Bryan S. Matsuura, Marleen Bérouti, et al. "PHOTACs enable optical control of protein degradation." Science Advances 6, no. 8 (2020): eaay5064. http://dx.doi.org/10.1126/sciadv.aay5064.

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PROTACs (PROteolysis TArgeting Chimeras) are bifunctional molecules that target proteins for ubiquitylation by an E3 ligase complex and subsequent degradation by the proteasome. They have emerged as powerful tools to control the levels of specific cellular proteins. We now introduce photoswitchable PROTACs that can be activated with the spatiotemporal precision that light provides. These trifunctional molecules, which we named PHOTACs (PHOtochemically TArgeting Chimeras), consist of a ligand for an E3 ligase, a photoswitch, and a ligand for a protein of interest. We demonstrate this concept by

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Koravovic, Mladen, Bojan Markovic, Milena Kovacevic, Milena Rmandic, and Gordana Tasic. "Protein degradation induced by PROTAC molecules as emerging drug discovery strategy." Journal of the Serbian Chemical Society, no. 00 (2022): 27. http://dx.doi.org/10.2298/jsc211209027k.

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The traditional concept of drug discovery is based on the occupancy-driven pharmacology model. It implies the development of inhibitors occupying binding sites that directly affect protein functions. Therefore, proteins that do not have such binding sites are generally considered as pharmacologically intractable. Furthermore, drugs that act in this way must be administered in dosage regimens that often result in high systemic drug exposures in order to maintain sufficient protein inhibition. Thus, there is a risk of off-target binding and side effects onset. The landscape of drug discovery has

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Nick McElhinny, Stephanie A., Carey M. Snowden, Joseph McCarville, and Dale A. Ramsden. "Ku Recruits the XRCC4-Ligase IV Complex to DNA Ends." Molecular and Cellular Biology 20, no. 9 (2000): 2996–3003. http://dx.doi.org/10.1128/mcb.20.9.2996-3003.2000.

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ABSTRACT Genetic experiments have determined that Ku, XRCC4, and ligase IV are required for repair of double-strand breaks by the end-joining pathway. The last two factors form a tight complex in cells. However, ligase IV is only one of three known mammalian ligases and is intrinsically the least active in intermolecular ligation; thus, the biochemical basis for requiring this ligase has been unclear. We demonstrate here a direct physical interaction between the XRCC4-ligase IV complex and Ku. This interaction is stimulated once Ku binds to DNA ends. Since XRCC4-ligase IV alone has very low DN

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21

Kitamura, Y., A. Ebihara, A. Shinkai, K. Hirotsu, and S. Kuramitsu. "Ligand-induced conformational change of D-alanine:D-alanine ligase fromThermus thermophilusHB8." Acta Crystallographica Section A Foundations of Crystallography 64, a1 (2008): C272. http://dx.doi.org/10.1107/s0108767308091307.

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22

Peng, Zhi, Taiping Shi, and Dalong Ma. "RNF122: A novel ubiquitin ligase associated with calcium-modulating cyclophilin ligand." BMC Cell Biology 11, no. 1 (2010): 41. http://dx.doi.org/10.1186/1471-2121-11-41.

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23

Purushothaman, Sudha, Garima Gupta, Richa Srivastava, Vasanthakumar Ganga Ramu, and Avadhesha Surolia. "Ligand Specificity of Group I Biotin Protein Ligase of Mycobacterium tuberculosis." PLoS ONE 3, no. 5 (2008): e2320. http://dx.doi.org/10.1371/journal.pone.0002320.

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24

Warr, Matthew R., Stephane Acoca, Zhiqian Liu, et al. "BH3-ligand regulates access of MCL-1 to its E3 ligase." FEBS Letters 579, no. 25 (2005): 5603–8. http://dx.doi.org/10.1016/j.febslet.2005.09.028.

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25

Ishikawa, Minoru, Shusuke Tomoshige, Yosuke Demizu, and Mikihiko Naito. "Selective Degradation of Target Proteins by Chimeric Small-Molecular Drugs, PROTACs and SNIPERs." Pharmaceuticals 13, no. 4 (2020): 74. http://dx.doi.org/10.3390/ph13040074.

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New therapeutic modalities are needed to address the problem of pathological but undruggable proteins. One possible approach is the induction of protein degradation by chimeric drugs composed of a ubiquitin ligase (E3) ligand coupled to a ligand for the target protein. This article reviews chimeric drugs that decrease the level of specific proteins such as proteolysis targeting chimeric molecules (PROTACs) and specific and nongenetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs), which target proteins for proteasome-mediated degradation. We cover strategies for incre

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26

Ciulli, Alessio. "Targeted Protein Degradation with Small Molecules: How PROTACs Work." Proceedings 22, no. 1 (2019): 115. http://dx.doi.org/10.3390/proceedings2019022115.

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Bivalent degrader molecules (also termed PROTACs) target proteins for degradation through recruitment to E3 ligases. PROTACs are a revolutionary new modality class with therapeutic potential. Formation of a ternary complex between the degrader, the ligase, and the target leads to tagging by ubiquitination and proteasomal degradation of the target protein. In 2015, we disclosed MZ1, a potent degrader made of a ligand we had previously discovered for the E3 ligase von Hippel–Lindau (VHL), and a pan-selective ligand for the BET proteins Brd2, Brd3, and Brd4. We made the unexpected but fascinating

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Baek, Suk-Hwan, Bin Huang, and Hyeun Wook Chang. "RNF144b is a negative regulator in TLR2-mediated NF-kB activation." Journal of Immunology 196, no. 1_Supplement (2016): 132.4. http://dx.doi.org/10.4049/jimmunol.196.supp.132.4.

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Abstract NF-κB regulates the expression of a various genes involved in diverse cellular processes including inflammation and immunity. Activation of NF-κB requires ubiquitination, a highly conserved and versatile modification that can regulate cell signaling through both proteasome dependent and independent mechanisms. Ubiquitination process is a representative of post-translational modification involved in NF-κB activation of TNFR and TLR signaling. We demonstrated that RNF144b, an E3 ubiquitin ligase, is important factor for the NF-κB regulation in macrophages upon stimulation with TNFa or T

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Kato, Koya, and George Chikenji. "1P266 Development of Ligand Based Virtual Screening considering protein-ligand interaction(22A. Bioinformatics: Structural genomics,Poster)." Seibutsu Butsuri 53, supplement1-2 (2013): S150. http://dx.doi.org/10.2142/biophys.53.s150_1.

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Yao, Tingting, Heng Xiao, Hong Wang, and Xiaowei Xu. "Recent Advances in PROTACs for Drug Targeted Protein Research." International Journal of Molecular Sciences 23, no. 18 (2022): 10328. http://dx.doi.org/10.3390/ijms231810328.

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Proteolysis-targeting chimera (PROTAC) is a heterobifunctional molecule. Typically, PROTAC consists of two terminals which are the ligand of the protein of interest (POI) and the specific ligand of E3 ubiquitin ligase, respectively, via a suitable linker. PROTAC degradation of the target protein is performed through the ubiquitin–proteasome system (UPS). The general process is that PROTAC binds to the target protein and E3 ligase to form a ternary complex and label the target protein with ubiquitination. The ubiquitinated protein is recognized and degraded by the proteasome in the cell. At pre

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Okada, Maiko, Fumiaki Ohtake, Hiroyuki Nishikawa та ін. "Liganded ERα Stimulates the E3 Ubiquitin Ligase Activity of UBE3C to Facilitate Cell Proliferation". Molecular Endocrinology 29, № 11 (2015): 1646–57. http://dx.doi.org/10.1210/me.2015-1125.

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Abstract Estrogen receptor (ER)α is a well-characterized ligand-dependent transcription factor. However, the global picture of its nongenomic functions remains to be illustrated. Here, we demonstrate a novel function of ERα during mitosis that facilitates estrogen-dependent cell proliferation. An E3 ubiquitin ligase, UBE3C, was identified in an ERα complex from estrogen-treated MCF-7 breast cancer cells arrested at mitosis. UBE3C interacts with ERα during mitosis in an estrogen-dependent manner. In vitro, estrogen dramatically stimulates the E3 activity of UBE3C in the presence of ERα. This ef

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Ilinca, Elena-Cristina, Ana-Marina Tomescu, and Sophie Dufossé Sournin. "The Olympic Games 2024 in French Online Media Discourse." XLinguae 18, no. 1 (2025): 144–52. https://doi.org/10.18355/xl.2025.18.01.11.

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This article aims to analyse the discursive construction around The 2024 Summer Olympics event in online media using an approach that brings together analysis elements used in linguistics, pragmatics, discourse analysis, argumentation, and rhetoric. First, we will attempt to clarify the meaning of a few key terms used in the study: media, mediatisation, media discourse, public space, media event construction. Then, we offer an analysis of some online texts dealing with the Olympic Torch Relay by highlighting the discursive mechanisms capable of establishing it at the media level as an event of

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Sandhya, P. V., P. K. Rejimon, and Kumar K. V. Satheesh. "Synthesis, molecular docking, antibacterial and antifungal studies of Fe (II) and Ni (II) complexes of N1, N2-bis((1,3-diphenyl-1H-pyrazol-4-yl) methylene) ethane-1,2-diamine." Research Journal of Chemistry and Environment 26, no. 2 (2022): 101–9. http://dx.doi.org/10.25303/2602rjce101109.

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1,3-Diphenyl pyrazole terminated ligand N1,N2- bis((1,3-diphenyl-1H-pyrazol-4-yl)methylene)ethane- 1,2-diamine and its iron and nickel complexes were synthesized. The structural environment of synthesis of ligand and its metal complexes was confirmed by elemental analysis, UV-Vis, FT-IR 1HNMR and 13NMR spectroscopic techniques. These compounds were further screened in vitro antimicrobial activities against some bacterial and some fungal strains and compared with the standard drugs. The result showed that the metal complexes are good candidates as antimicrobial agents than the ligands at the sa

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Wan, Yichao, Chunxing Yan, Han Gao, and Tingting Liu. "Small-molecule PROTACs: novel agents for cancer therapy." Future Medicinal Chemistry 12, no. 10 (2020): 915–38. http://dx.doi.org/10.4155/fmc-2019-0340.

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Proteolysis-targeting chimera (PROTAC) is a new technology to selectively degrade target proteins via ubiquitin-proteasome system. PROTAC molecules (PROTACs) are a class of heterobifunctional molecules, which contain a ligand targeting the protein of interest, a ligand recruiting an E3 ligase and a linker connecting these two ligands. They provide several advantages over traditional inhibitors in potency, selectivity and drug resistance. Thus, many promising PROTACs have been developed in the recent two decades, especially small-molecule PROTACs. In this review, we briefly introduce the mechan

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Williamson, Adele, Ulli Rothweiler, and Hanna-Kirsti Schrøder Leiros. "Enzyme–adenylate structure of a bacterial ATP-dependent DNA ligase with a minimized DNA-binding surface." Acta Crystallographica Section D Biological Crystallography 70, no. 11 (2014): 3043–56. http://dx.doi.org/10.1107/s1399004714021099.

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DNA ligases are a structurally diverse class of enzymes which share a common catalytic core and seal breaks in the phosphodiester backbone of double-stranded DNAviaan adenylated intermediate. Here, the structure and activity of a recombinantly produced ATP-dependent DNA ligase from the bacteriumPsychromonassp. strain SP041 is described. This minimal-type ligase, like its close homologues, is able to ligate singly nicked double-stranded DNA with high efficiency and to join cohesive-ended and blunt-ended substrates to a more limited extent. The 1.65 Å resolution crystal structure of the enzyme–a

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Gopinathan, Lakshmi, Daniel B. Hannon, Russell W. Smith, Jeffrey M. Peters, and John P. Vanden Heuvel. "Regulation of Peroxisome Proliferator-Activated Receptors by E6-Associated Protein." PPAR Research 2008 (2008): 1–8. http://dx.doi.org/10.1155/2008/746935.

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Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors (NRs) that regulate genes involved in lipid and glucose metabolism. PPAR activity is regulated by interactions with cofactors and of interest are cofactors with ubiquitin ligase activity. The E6-associated protein (E6-AP) is an E3 ubiquitin ligase that affects the activity of other NRs, although its effects on PPARs have not been examined. E6-AP inhibited the ligand-independent transcriptional activity of PPARαand PPARβ, with marginal effects on PPARγ, and decreased basal mRNA levels of PPARαtarget genes. Inhibition of P

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Koravović, Mladen, Gordana Tasić, Milena Rmandić, and Bojan Marković. "Photocontrollable PROTAC molecules: Structure and mechanism of action." Arhiv za farmaciju 71, no. 3 (2021): 161–76. http://dx.doi.org/10.5937/arhfarm71-30785.

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Traditional drug discovery strategies are usually focused on occupancy of binding sites that directly affect functions of proteins. Hence, proteins that lack such binding sites are generally considered pharmacologically intractable. Modulators of protein activity, especially inhibitors, must be applied in appropriate dosage regimens that often lead to high systemic drug exposures in order to maintain sufficient protein inhibition in vivo. Consequently, there is a risk of undesirable off-target drug binding and side effects. Recently, PROteolysis TArgeting Chimera (PROTAC) technology has emerge

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Kilroy, Gail, Heather Kirk-Ballard, Lauren E. Carter та Z. Elizabeth Floyd. "The Ubiquitin Ligase Siah2 Regulates PPARγ Activity in Adipocytes". Endocrinology 153, № 3 (2012): 1206–18. http://dx.doi.org/10.1210/en.2011-1725.

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Moderate reductions in peroxisome proliferator-activated receptor (PPAR)γ levels control insulin sensitivity as effectively as activation of PPARγ in adipocytes by the thiazolidinediones. That observation suggests that PPARγ activity can be regulated by modulating the amount of PPARγ protein in adipocytes. Activation of PPARγ in adipocytes is linked to changes in PPARγ protein levels via increased degradation of PPARγ proteins by the ubiquitin proteasome system. Identification of the ubiquitin ligase or ligases that recognize ligand bound PPARγ is an essential step in determining the physiolog

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Haddouche, Assia, Samy Slimani, Bilal Bengana, Imen Bencharif, and Abdelbaki Benmebarek. "What are the first-line treatments for rheumatoid arthritis ?" Batna Journal of Medical Sciences (BJMS) 1, no. 1 (2014): 27–33. http://dx.doi.org/10.48087/bjmstf.2014.1108.

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The management of rheumatoid arthritis has not stopped evolving after the advent of new effective therapies and the emergence of new concepts such as tight control, early and aggressive treatment with a target of remission, or at least low disease activity. Strategies to follow are now well codified by the new recommendations of the European League Against Rheumatism (EULAR) 2013, which clearly emphasized that conventional disease-modifying antirheumatic drugs (DMARDs) with methotrexate as a leader are the first-line therapies to use in the treatment of rheumatoid arthritis.

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Suresh Kumar, K. G. "SCFHOS ubiquitin ligase mediates the ligand-induced down-regulation of the interferon- receptor." EMBO Journal 22, no. 20 (2003): 5480–90. http://dx.doi.org/10.1093/emboj/cdg524.

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Sturgeon, Morgan, Dustin Davis, Amanda Albers, et al. "The Notch ligand E3 ligase, Mind Bomb1, regulates glutamate receptor localization in Drosophila." Molecular and Cellular Neuroscience 70 (January 2016): 11–21. http://dx.doi.org/10.1016/j.mcn.2015.11.004.

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Bertók, Béla, György Dormán, Zoltán Várkonyi, and Csaba Magyar. "Novel E3 Ligase Ligand Libraries for Degradation of Proteins Implicated in Malignant Diseases." Acta Pharmaceutica Hungarica 91, no. 3-4 (2021): 187–88. http://dx.doi.org/10.33892/aph.2021.91.187-188.

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Xia, Liwen, Wei Liu, Yinsen Song, Hailiang Zhu, and Yongtao Duan. "The Present and Future of Novel Protein Degradation Technology." Current Topics in Medicinal Chemistry 19, no. 20 (2019): 1784–88. http://dx.doi.org/10.2174/1568026619666191011162955.

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Proteolysis targeting chimeras (PROTACs), as a novel therapeutic modality, play a vital role in drug discovery. Each PROTAC contains three key parts; a protein-of-interest (POI) ligand, a E3 ligase ligand, and a linker. These bifunctional molecules could mediate the degradation of POIs by hijacking the activity of E3 ubiquitin ligases for POI ubiquitination and subsequent degradation via the ubiquitin proteasome system (UPS). With several advantages over other therapeutic strategies, PROTACs have set off a new upsurge of drug discovery in recent years. ENDTAC, as the development of PROTACs tec

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Pyda, Jakub. "„The last mark of a vanishing thought”. Zygmunt Krasiński’s Three thoughts of Ligenza as a Testament." Tekstualia 1, no. 56 (2019): 53–74. http://dx.doi.org/10.5604/01.3001.0013.3285.

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Can the testament be an artistic expression? Three thoughts of Ligenza (Trzy myśli Ligenzy), Zygmunt Krasiński’s work from 1840 is an intriguing case in point. It is not only the last will of the dying protagonist, but primarily a poetic and philosophic form that helps understanding the ultimate truth. On the structural level, the three eponymous thoughts are the consecutive parts of the poem. At the same time, in the fi ctional sense, they are refl ections of Henryk Ligenza, a mysterious romantic who has left his notes – „the last mark of a vanishing thought”. Ligenza’s essential role is to m

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Marijanovic, Zrinka, Josiane Ragimbeau, K. G. Suresh Kumar, Serge Y. Fuchs, and Sandra Pellegrini. "TYK2 activity promotes ligand-induced IFNAR1 proteolysis." Biochemical Journal 397, no. 1 (2006): 31–38. http://dx.doi.org/10.1042/bj20060272.

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The type I IFNR (interferon receptor) is a heterodimer composed of two transmembrane chains, IFNAR1 (interferon-α receptor 1 subunit) and IFNAR2, which are associated with the tyrosine kinases Tyk2 and Jak1 (Janus kinase 1) respectively. Ligand-induced down-regulation of the type I IFNR is a major mechanism of negative regulation of cellular signalling and involves the internalization and lysosomal degradation of IFNAR1. IFNα promotes the phosphorylation of IFNAR1 on Ser535, followed by recruitment of the E3 ubiquitin ligase, β-TrCP2 (β-transducin repeats-containing protein 2), ubiquitination

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Cao, Zhongwei, Xiuli Wu, Lily Yen, Colleen Sweeney, and Kermit L. Carraway. "Neuregulin-Induced ErbB3 Downregulation Is Mediated by a Protein Stability Cascade Involving the E3 Ubiquitin Ligase Nrdp1." Molecular and Cellular Biology 27, no. 6 (2007): 2180–88. http://dx.doi.org/10.1128/mcb.01245-06.

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ABSTRACT The molecular mechanisms underlying epidermal growth factor (EGF) receptor tyrosine kinase down-regulation in response to growth factor binding are coming into focus and involve cbl-mediated receptor ubiquitination followed by lysosomal degradation. However, mechanisms underlying the ligand-stimulated degradation of the related receptor tyrosine kinases of the ErbB family do not involve cbl and remain unexplored. Previous studies have demonstrated that the E3 ubiquitin ligase Nrdp1 contributes to the maintenance of steady-state ErbB3 levels by mediating its growth factor-independent d

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Peraldi, Jacques. "Ligne." Po&sie 159, no. 1 (2017): 66. http://dx.doi.org/10.3917/poesi.159.0066.

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Giardina, Sarah F., Elena Valdambrini, Michael Peel, et al. "Cure-PROs: Next-generation targeted protein degraders." Journal of Clinical Oncology 41, no. 16_suppl (2023): e15101-e15101. http://dx.doi.org/10.1200/jco.2023.41.16_suppl.e15101.

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e15101 Background: Many proteins, including transcription factors and scaffolding proteins, are not amenable to targeting by traditional small molecule inhibitors due to the lack of a well-defined binding pocket or active site. Proteolysis-Targeting Chimeras (PROTACs) are a new class of hetero-bifunctional molecules that bind both a target protein and an E3 ubiquitin ligase, bringing the two into proximity for appending ubiquitin, and subsequently marking the target protein for proteasomal degradation. Currently, thirteen PROTACs are in clinical trials for oncology indications. However, the cl

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Zhai, Yunpeng, Ming Tan, Defu Liu, Guoqian Wang, Jinying Ning, and Feng Hao. "Abstract 6181: Cell line panel with HIBIT tagged endogenous proteins to accelerate PROTAC drug discovery." Cancer Research 82, no. 12_Supplement (2022): 6181. http://dx.doi.org/10.1158/1538-7445.am2022-6181.

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Abstract Recent years have seen great advancement of targeted protein degradation technology, in particular, proteolysis targeting chimeras (PROTACs) are now widely used in developing therapeutics for treating cancer. A PROTAC is a heterobifunctional small molecule with three distinct moieties: a ligand to bind a targeted protein of interest (POI), a second ligand to recruit E3 ubiquitin ligase to form a ternary complex, and a linker for bridging the two ligands. Through the E3 ubiquitin ligase pathway, properly designed PROTACs can effectively degrade POIs with high specificity, which can be

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Kato, Koya, and George Chikenji. "2P272 A Ligand Based Virtual Screening method that takes into account of protein-ligand interactions(22A. Bioinformatics:Structural genomics,Poster)." Seibutsu Butsuri 54, supplement1-2 (2014): S240. http://dx.doi.org/10.2142/biophys.54.s240_2.

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S. Vasantha, S. Vasantha, D. Arputha Kiruba Nisha D. Arputha Kiruba Nisha, S. SivaKolunthu S. SivaKolunthu, and T. Angeline T. Angeline. "Synthesis, DNA Binding and Activity of Mixed Ligand Copper(II) Complexes with Sulfur Containing Ligand: 1-Hydroxy-2-Acetonaphthonetosylhydrazone." International Journal of Scientific Research 2, no. 12 (2012): 60–63. http://dx.doi.org/10.15373/22778179/dec2013/20.

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