Academic literature on the topic 'Small molecule modulators'

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Journal articles on the topic "Small molecule modulators"

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Li, Jie Jack. "Small molecule interleukin-8 modulators." Expert Opinion on Therapeutic Patents 11, no. 12 (2001): 1905–10. http://dx.doi.org/10.1517/13543776.11.12.1905.

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Arndt, Hans-Dieter. "Small Molecule Modulators of Transcription." Angewandte Chemie International Edition 45, no. 28 (2006): 4552–60. http://dx.doi.org/10.1002/anie.200600285.

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Lin, Cong, Hongshuang Wang, Miyuan Zhang, et al. "TLR4 biased small molecule modulators." Pharmacology & Therapeutics 228 (December 2021): 107918. http://dx.doi.org/10.1016/j.pharmthera.2021.107918.

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Sharma, Shiv K., Stuart Hazeldine, Michael L. Crowley, et al. "Polyamine-based small molecule epigenetic modulators." MedChemComm 3, no. 1 (2012): 14–21. http://dx.doi.org/10.1039/c1md00220a.

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Multiple series of HDAC and LSD1 inhibitors have been developed that increase histone lysine methylation and promote the re-expression of aberrantly silenced genes that are important in human cancer..
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Senderowicz, Adrian M. "Small-molecule cyclin-dependent kinase modulators." Oncogene 22, no. 42 (2003): 6609–20. http://dx.doi.org/10.1038/sj.onc.1206954.

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Pachaiyappan, Boobalan, and Patrick M. Woster. "Design of small molecule epigenetic modulators." Bioorganic & Medicinal Chemistry Letters 24, no. 1 (2014): 21–32. http://dx.doi.org/10.1016/j.bmcl.2013.11.001.

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Knapp, Stefan, and Hilmar Weinmann. "Small-Molecule Modulators for Epigenetics Targets." ChemMedChem 8, no. 11 (2013): 1885–91. http://dx.doi.org/10.1002/cmdc.201300344.

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He, Baokun, and Zheng Chen. "Molecular Targets for Small-Molecule Modulators of Circadian Clocks." Current Drug Metabolism 17, no. 5 (2016): 503–12. http://dx.doi.org/10.2174/1389200217666160111124439.

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Koehler, Carla. "Small molecule modulators for mitochondrial protein import." Mitochondrion 24 (September 2015): S5. http://dx.doi.org/10.1016/j.mito.2015.07.020.

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Wang, Yibo, Shuting Zhang, Hongyuan Li, et al. "Small-Molecule Modulators of Toll-like Receptors." Accounts of Chemical Research 53, no. 5 (2020): 1046–55. http://dx.doi.org/10.1021/acs.accounts.9b00631.

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Dissertations / Theses on the topic "Small molecule modulators"

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Luccarelli, James. "Small Molecule Modulators of Apoptosis." Thesis, Harvard University, 2017. http://nrs.harvard.edu/urn-3:HUL.InstRepos:32676118.

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Control of cell survival relies on a delicate balance between pro-apoptotic and anti-apoptotic signalling. In humans, the key regulatory proteins are those of the BCL-2 family, which include effector proteins such as BAX and BAK, anti-apoptotic proteins including BCL-2 and MCL-1, and pro-apoptotic proteins including BID and BIM. Dysregulation of apoptosis is among the Hallmarks of Cancer, and modulation of apoptosis holds promise as an effective therapeutic strategy for a range of malignancies. This thesis advances new strategies for modulating apoptosis using small molecules. The first secti
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Moustakim, Moses. "Discovery of small molecule epigenetic modulators." Thesis, University of Oxford, 2018. http://ora.ox.ac.uk/objects/uuid:0d4a42f1-8a47-4ad5-ac30-b4eaf0d36db3.

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Target validation is increasingly becoming a central tenet to successful execution of drug discovery campaigns. An emerging approach towards the development of novel therapies for previously untreated diseases is the development of small molecule chemical probes which can be used as early stage tools for pertinent biological questions to be explored about a molecular target within the context of disease. A number of proteins which regulate epigenetic mechanisms have been correlated with disease onset and progression. Despite disease links, there remains a paucity in the understanding by which
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Liu, Jia. "Mechanistic studies of small-molecule CFTR modulators." Thesis, University of Bristol, 2012. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.627986.

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The cystic fibrosis transmembrane conductance regulator (CFTR) is a CI channel found in the apical membrane of epithelial cells. CFTR activity is tightly controlled by complex regulation. However, CFTR overactivity or loss-of-function mutations in CFTR are both disease causing conditions. The aims of my research were to investigate the mechanisms Of action of small-molecule CFTR modulators that regulate CFTR function. Loop diuretics are inhibitors ofNa+-K+-2Cr-cotranspOlter isofOlm 1 (NKCC1) located in the basolateral membrane of epithelial cells. I demonstrated that loop diuretics also inhibi
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Rütschlin, Sina [Verfasser]. "Small Molecule Modulators of Bacterial Swarming Behavior / Sina Rütschlin." Konstanz : KOPS Universität Konstanz, 2019. http://d-nb.info/1189586592/34.

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Tampi, Girish. "Investigating small molecule modulators of bio-molecular interactions : an in-silico study." Thesis, University of Leeds, 2015. http://etheses.whiterose.ac.uk/12511/.

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Small molecule inhibitors are commonly used to target protein targets that assist in the spread of diseases such as AIDS, cancer and deadly forms of influenza. Despite drug companies spending millions on R&D, the number of drugs that pass clinical trials is limited due to difficulties in engineering optimal non-covalent interactions. As many protein targets have the ability to rapidly evolve resistance, there is an urgent need for methods that rapidly identify effective new compounds. The thermodynamic driving force behind most biochemical reactions is known as the Gibbs free energy and it con
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Yuan, Yuan. "Small-Molecule Modulators of Pancreatic Ductal Cells: Histone Methyltransferases and \(\beta\)-Cell Transdifferentiation." Thesis, Harvard University, 2012. http://dissertations.umi.com/gsas.harvard:10637.

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Small molecules are important not only for treating human diseases but also for studying disease-related biological processes. This dissertation focuses on the effects of small molecules on pancreatic ductal adenocarcinoma cells. Here, I describe the discovery of two small-molecule tool compounds and their applications for interrogating the biological processes related to two distinct diseases in the human pancreas. First, BRD4770 was identified as a histone methyltransferase inhibitor through a target-based biochemical approach, and was used as a probe to study the function of methyltransfera
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Paulk, Joshiawa Lanair James. "Modulators of Cellular and Biochemical PRC2 Activity." Thesis, Harvard University, 2014. http://nrs.harvard.edu/urn-3:HUL.InstRepos:13064968.

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EZH2 is a SET domain-containing methyltransferase and the catalytic component of the multimeric Polycomb- group (PcG) protein complex, PRC2. When in complex with other PRC2 members (EED, SUZ12, AEBP2, and RBBP4), EZH2 catalyzes methylation of H3K27, a histone modification associated with transcriptional repression and developmental regulation. As several PRC2 components are upregulated or mutated in a variety of human cancers, efforts to discover small-molecule modulators of PRC2 and understand its regulation may yield therapeutic insights. Identification of small-molecule probes with distinc
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Hamzah, Nurasyikin Binti. "Identification and optimisation of small molecule modulators of Orai3 and TRPC4 as potential therapeutics." Thesis, University of Leeds, 2018. http://etheses.whiterose.ac.uk/21990/.

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Ca2+ signalling pathways require different types of ion channels to help control the concentration of Ca2+ in the cell in order to carry out diverse physiological activities. Excessive Ca2+ leads to therapeutic diseases such as necrosis,[1] cancer,[2] and heart failure.[3] Unfortunately, many of the available calcium inhibitors suffer from weak potency and selectivity profiles (i.e TRP, sodium, potassium channels). Two Ca2+ ion proteins (Orai3 and TRPC4) were selected to target with novel chemical probes to better understand their biological function and potential utility as therapeutic target
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Mota, F. "The discovery of small molecule modulators of soluble guanylate cyclase aided by surface plasmon resonance." Thesis, University College London (University of London), 2014. http://discovery.ucl.ac.uk/1434127/.

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Soluble guanylate cyclase is a multidimeric enzyme that regulates cardiovascular homeostasis and is the receptor for nitric oxide in the brain. The enzyme is the known target for a new agonist drug used for the treatment of pulmonary hypertension. Whilst drug discovery has been successful for the finding of small molecules that activate the enzyme, the currently available inhibitors lack selectivity as they act through oxidation of a heme prosthetic group in the enzyme, which is conserved amongst other hemeproteins. Nonetheless, it has been suggested that inhibition of soluble guanylate cyclas
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Ang, Jit Hang Jackie. "Developing biophysical and structural methods for characterisation of small molecule modulators of K2P potassium channels." Thesis, University of Oxford, 2017. https://ora.ox.ac.uk/objects/uuid:850d137b-6270-48d9-9eaa-ce6fb65dcbc4.

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Biophysical techniques are widely used to determine the structure, function and ligand binding properties of a protein. However, their application to membrane proteins has been limited due to the difficulty of obtaining sufficient purified sample. In this work, I use such methods to examine the thermostability and ligand binding properties of TREKs, two members of the family of tandem pore domain K<sup>+</sup> channels important for the regulation of cellular excitability. Structures of TREK1 and TREK2 are available and thus when combined with such approaches may help guide the design of bette
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Books on the topic "Small molecule modulators"

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Thursfield, Rebecca, Chris Orchard, Rosanna Featherstone, and Jane C. Davies. Future treatments. Oxford University Press, 2015. http://dx.doi.org/10.1093/med/9780198702948.003.0013.

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There are only a relatively limited armoury of drugs, the majority of which are aimed at downstream symptoms of cystic fibrosis. Therapies targeting the basic defect in CF as well as continued availability of more conventional drugs are required. Progress in gene therapy has been limited by the significant barriers to gene transfer of the CF lung, but the UK is hosting a large repeated dose trial of nebulized non-viral gene therapy designed around clinically meaningful outcomes. The UK CF Gene Therapy Consortium is also seeking to develop a promising modified lentiviral approach, although this
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Book chapters on the topic "Small molecule modulators"

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Swaminathan, V., B. A. Ashok Reddy, Ruthrotha Selvi B, Sukanya M.S., and Tapas K. Kundu. "Small Molecule Modulators In Epigenetics." In Subcellular Biochemistry. Springer Netherlands, 2007. http://dx.doi.org/10.1007/1-4020-5466-1_18.

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Mazurov, Anatoly, and Daniel Yohannes. "Nicotinic Acetylcholine Receptor Modulators." In Small Molecule Therapeutics for Schizophrenia. Springer International Publishing, 2014. http://dx.doi.org/10.1007/7355_2014_56.

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Triola, Gemma. "Autophagy: Assays and Small-Molecule Modulators." In Concepts and Case Studies in Chemical Biology. Wiley-VCH Verlag GmbH & Co. KGaA, 2014. http://dx.doi.org/10.1002/9783527687503.ch5.

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Alcaín, Francisco J., Robin K. Minor, José M. Villalba, and Rafael de Cabo. "Small Molecule Modulators of Sirtuin Activity." In The Future of Aging. Springer Netherlands, 2010. http://dx.doi.org/10.1007/978-90-481-3999-6_10.

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Gurney, Mark E., Alex B. Burgin, Olafur T. Magnusson, and Lance J. Stewart. "Small Molecule Allosteric Modulators of Phosphodiesterase 4." In Phosphodiesterases as Drug Targets. Springer Berlin Heidelberg, 2011. http://dx.doi.org/10.1007/978-3-642-17969-3_7.

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Xiao, Zhangang, and Yangchao Chen. "Identification of Small Molecule Modulators of MicroRNA by Library Screening." In Methods in Molecular Biology. Springer New York, 2016. http://dx.doi.org/10.1007/978-1-4939-6563-2_12.

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Zhang, Lan, and Bo Liu. "Targeting Autophagy with Small-Molecule Modulators in Immune-Related Diseases." In Advances in Experimental Medicine and Biology. Springer Singapore, 2019. http://dx.doi.org/10.1007/978-981-15-0606-2_11.

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Talukdar, Arindam, Ayan Mukherjee, and Dipyaman Ganguly. "CHAPTER 13. Small Molecule Modulators of Endo-lysosomal Toll-like Receptors." In Protein–Protein Interaction Regulators. Royal Society of Chemistry, 2020. http://dx.doi.org/10.1039/9781788016544-00339.

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Berg, Thorsten. "Small-Molecule Modulators of c-Myc/Max and Max/Max Interactions." In Current Topics in Microbiology and Immunology. Springer Berlin Heidelberg, 2010. http://dx.doi.org/10.1007/82_2010_90.

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Zhang, Daniel, and Bin Zhang. "High Content Screening of Small Molecule Modulators Targeting Heat Shock Response Pathway." In Heat Shock Proteins and Stress. Springer International Publishing, 2018. http://dx.doi.org/10.1007/978-3-319-90725-3_8.

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Conference papers on the topic "Small molecule modulators"

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Chen, James K. "Abstract IA19: Small-molecule modulators of the Hedgehog signaling pathway." In Proceedings: AACR Special Conference on Chemical Systems Biology: Assembling and Interrogating Computational Models of the Cancer Cell by Chemical Perturbations--Jun 27-30, 2012; Boston, MA. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.csb12-ia19.

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Pal, Rajesh, Gauri Misra, and Puniti Mathur. "In silico screening of small molecule modulators of Zika virus proteins." In 2017 7th International Conference on Cloud Computing, Data Science & Engineering - Confluence (Confluence). IEEE, 2017. http://dx.doi.org/10.1109/confluence.2017.7943179.

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Lewis, Timothy A., Luc de Waal, Xiaoyun Wu, et al. "Abstract 5880: Small-molecule modulators of PDE3/SLFN12 to kill cancer cells." In Proceedings: AACR Annual Meeting 2018; April 14-18, 2018; Chicago, IL. American Association for Cancer Research, 2018. http://dx.doi.org/10.1158/1538-7445.am2018-5880.

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Azmi, Asfar S., William Senapedis, Yosef Landesman, et al. "Abstract 1771: Novel small molecule pak4 allosteric modulators with activity against pancreatic cancer." In Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA. American Association for Cancer Research, 2014. http://dx.doi.org/10.1158/1538-7445.am2014-1771.

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Grover, Prerna, Haibin Shi, Matthew Baumgartner, et al. "Abstract B132: Discovery of small molecule allosteric modulators of Abl kinase activity and function." In Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; November 5-9, 2015; Boston, MA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1535-7163.targ-15-b132.

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Wise, Scott C., Bryan D. Smith, Molly M. Hood, Michael D. Kaufman, Wei-Ping Lu, and Daniel L. Flynn. "Abstract LB-300: Small molecule modulators of MET kinase for treatment of human malignancies." In Proceedings: AACR 101st Annual Meeting 2010‐‐ Apr 17‐21, 2010; Washington, DC. American Association for Cancer Research, 2010. http://dx.doi.org/10.1158/1538-7445.am10-lb-300.

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Garapaty, Shivani Rao, Dhanalakshmi Sivanandhan, Guru Pavan Kumar Seerapu, et al. "Abstract 5578: Small molecule modulators to understand the role of IDO1 and TDO2 in cancer." In Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC. American Association for Cancer Research, 2017. http://dx.doi.org/10.1158/1538-7445.am2017-5578.

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Manabu, Kawada, Masayuki Arakawa, Isao Momose, Tetsuya Someno, and Daishiro Ikeda. "Abstract B153: Small molecule modulators of tumor‐stromal cell interactions, new natural compounds from fungi." In Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics--Nov 15-19, 2009; Boston, MA. American Association for Cancer Research, 2009. http://dx.doi.org/10.1158/1535-7163.targ-09-b153.

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Pathania, Divya, Mario Sechi, Michele Palomba, et al. "Abstract 4555: Design and discovery of novel small molecule redox modulators as therapies for pancreatic cancer." In Proceedings: AACR 104th Annual Meeting 2013; Apr 6-10, 2013; Washington, DC. American Association for Cancer Research, 2013. http://dx.doi.org/10.1158/1538-7445.am2013-4555.

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Pathania, Divya, Mario Sechi, Michele Palomba, et al. "Abstract 682: Design and discovery of novel small molecule modulators of reactive oxygen species-mediated cell signaling." In Proceedings: AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-682.

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