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1

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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2

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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3

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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4

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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5

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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6

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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7

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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8

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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9

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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10

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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11

Czarniecki, Michael. "Small Molecule Modulators of Toll-like Receptors." Journal of Medicinal Chemistry 51, no. 21 (2008): 6621–26. http://dx.doi.org/10.1021/jm800957k.

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12

Meijer, Femke A., Iris A. Leijten-van de Gevel, Rens M. J. M. de Vries, and Luc Brunsveld. "Allosteric small molecule modulators of nuclear receptors." Molecular and Cellular Endocrinology 485 (April 2019): 20–34. http://dx.doi.org/10.1016/j.mce.2019.01.022.

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13

Balasubramanyam, Karanam, V. Swaminathan, Anupama Ranganathan, and Tapas K. Kundu. "Small Molecule Modulators of Histone Acetyltransferase p300." Journal of Biological Chemistry 278, no. 21 (2003): 19134–40. http://dx.doi.org/10.1074/jbc.m301580200.

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14

Wu, Chengde. "Recent developments of small molecule endothelin modulators." Expert Opinion on Therapeutic Patents 16, no. 10 (2006): 1337–45. http://dx.doi.org/10.1517/13543776.16.10.1337.

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15

Hur, Wooyoung, and Nathanael S. Gray. "Small molecule modulators of antioxidant response pathway." Current Opinion in Chemical Biology 15, no. 1 (2011): 162–73. http://dx.doi.org/10.1016/j.cbpa.2010.12.009.

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16

Kundu, Tapas K. "Small molecule modulators of chromatin and coactivators." Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms 1799, no. 10-12 (2010): 669–70. http://dx.doi.org/10.1016/j.bbagrm.2010.10.003.

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17

Chai, Sergio C., Milu T. Cherian, Yue-Ming Wang, and Taosheng Chen. "Small-molecule modulators of PXR and CAR." Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms 1859, no. 9 (2016): 1141–54. http://dx.doi.org/10.1016/j.bbagrm.2016.02.013.

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18

Knapp, Stefan, and Hilmar Weinmann. "Corrigendum: Small-Molecule Modulators for Epigenetics Targets." ChemMedChem 8, no. 12 (2013): 1904. http://dx.doi.org/10.1002/cmdc.201300464.

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19

Tang, Zhichao, Sana Akhter, Ankita Ramprasad, et al. "Recognition of single-stranded nucleic acids by small-molecule splicing modulators." Nucleic Acids Research 49, no. 14 (2021): 7870–83. http://dx.doi.org/10.1093/nar/gkab602.

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Abstract Risdiplam is the first approved small-molecule splicing modulator for the treatment of spinal muscular atrophy (SMA). Previous studies demonstrated that risdiplam analogues have two separate binding sites in exon 7 of the SMN2 pre-mRNA: (i) the 5′-splice site and (ii) an upstream purine (GA)-rich binding site. Importantly, the sequence of this GA-rich binding site significantly enhanced the potency of risdiplam analogues. In this report, we unambiguously determined that a known risdiplam analogue, SMN-C2, binds to single-stranded GA-rich RNA in a sequence-specific manner. The minimum
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20

Bhagwanth, Swapna, Ram K. Mishra, and Rodney L. Johnson. "Development of peptidomimetic ligands of Pro-Leu-Gly-NH2 as allosteric modulators of the dopamine D2 receptor." Beilstein Journal of Organic Chemistry 9 (January 30, 2013): 204–14. http://dx.doi.org/10.3762/bjoc.9.24.

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A variety of stable, small-molecule peptidomimetic ligands have been developed to elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH2 (PLG) modulates dopaminergic neurotransmission. Photoaffinity labeling ligands based upon PLG peptidomimetics have been used to establish that PLG binds to the D2 dopamine receptor at a site that is different from the orthosteric site, thus making PLG and its peptidomimetics allosteric modulators of the dopamine receptor. Through the design, synthesis and pharmacological evaluation of conformationally constrained peptidomimetics containing lactam,
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21

Markossian, Sarine, Kenny K. Ang, Christopher G. Wilson, and Michelle R. Arkin. "Small-Molecule Screening for Genetic Diseases." Annual Review of Genomics and Human Genetics 19, no. 1 (2018): 263–88. http://dx.doi.org/10.1146/annurev-genom-083117-021452.

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The genetic determinants of many diseases, including monogenic diseases and cancers, have been identified; nevertheless, targeted therapy remains elusive for most. High-throughput screening (HTS) of small molecules, including high-content analysis (HCA), has been an important technology for the discovery of molecular tools and new therapeutics. HTS can be based on modulation of a known disease target (called reverse chemical genetics) or modulation of a disease-associated mechanism or phenotype (forward chemical genetics). Prominent target-based successes include modulators of transthyretin, u
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22

Luchowska-Stańska, Urszula, David Morgan, Stephen J. Yarwood, and Graeme Barker. "Selective small-molecule EPAC activators." Biochemical Society Transactions 47, no. 5 (2019): 1415–27. http://dx.doi.org/10.1042/bst20190254.

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Abstract The cellular signalling enzymes, EPAC1 and EPAC2, have emerged as key intracellular sensors of the secondary messenger cyclic 3′,5′-adenosine monophosphate (cyclic adenosine monophosphate) alongside protein kinase A. Interest has been galvanised in recent years thanks to the emergence of these species as potential targets for new cardiovascular disease therapies, including vascular inflammation and insulin resistance in vascular endothelial cells. We herein summarise the current state-of-the-art in small-molecule EPAC activity modulators, including cyclic nucleotides, sulphonylureas,
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23

Hayashi, Ken-ichiro. "Small molecule modulators on auxin biosynthesis and signaling." Japanese Journal of Pesticide Science 40, no. 1 (2015): 36–43. http://dx.doi.org/10.1584/jpestics.w14-29.

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24

Nguyen, Uyen T., Iwona B. Wenderska, Matthew A. Chong, Kalinka Koteva, Gerard D. Wright, and Lori L. Burrows. "Small-Molecule Modulators of Listeria monocytogenes Biofilm Development." Applied and Environmental Microbiology 78, no. 5 (2011): 1454–65. http://dx.doi.org/10.1128/aem.07227-11.

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ABSTRACTListeria monocytogenesis an important food-borne pathogen whose ability to form disinfectant-tolerant biofilms on a variety of surfaces presents a food safety challenge for manufacturers of ready-to-eat products. We developed here a high-throughput biofilm assay forL. monocytogenesand, as a proof of principle, used it to screen an 80-compound protein kinase inhibitor library to identify molecules that perturb biofilm development. The screen yielded molecules toxic to multiple strains ofListeriaat micromolar concentrations, as well as molecules that decreased (≤50% of vehicle control) o
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25

Hindo, Sarmad S., Allana M. Mancino, Joseph J. Braymer та ін. "Small Molecule Modulators of Copper-Induced Aβ Aggregation". Journal of the American Chemical Society 131, № 46 (2009): 16663–65. http://dx.doi.org/10.1021/ja907045h.

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26

Hirota, Tsuyoshi. "Small molecule modulators of the circadian clock function." Proceedings for Annual Meeting of The Japanese Pharmacological Society 93 (2020): 1—S12–3. http://dx.doi.org/10.1254/jpssuppl.93.0_1-s12-3.

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27

Cellitti, Jason, Ziming Zhang, Si Wang та ін. "Small Molecule DnaK Modulators Targeting the β-Domain". Chemical Biology & Drug Design 74, № 4 (2009): 349–57. http://dx.doi.org/10.1111/j.1747-0285.2009.00869.x.

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28

Cherian, Milu T., Sergio C. Chai, and Taosheng Chen. "Small-molecule modulators of the constitutive androstane receptor." Expert Opinion on Drug Metabolism & Toxicology 11, no. 7 (2015): 1099–114. http://dx.doi.org/10.1517/17425255.2015.1043887.

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29

Mook, Robert A., Minyong Chen, Jiuyi Lu, Larry S. Barak, H. Kim Lyerly та Wei Chen. "Small molecule modulators of Wnt/β-catenin signaling". Bioorganic & Medicinal Chemistry Letters 23, № 7 (2013): 2187–91. http://dx.doi.org/10.1016/j.bmcl.2013.01.101.

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30

Munshi, Soumyabrata, and Russell Dahl. "Cytoprotective small molecule modulators of endoplasmic reticulum stress." Bioorganic & Medicinal Chemistry 24, no. 11 (2016): 2382–88. http://dx.doi.org/10.1016/j.bmc.2016.03.045.

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31

Weinmann, Hilmar. "Cancer Immunotherapy: Selected Targets and Small-Molecule Modulators." ChemMedChem 11, no. 5 (2016): 450–66. http://dx.doi.org/10.1002/cmdc.201500566.

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32

Yuan, Zhao-Di, Wei-Ning Zhu, Ke-Zhi Liu, Zhan-Peng Huang, and Yan-Chuang Han. "Small Molecule Epigenetic Modulators in Pure Chemical Cell Fate Conversion." Stem Cells International 2020 (October 20, 2020): 1–12. http://dx.doi.org/10.1155/2020/8890917.

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Although innovative technologies for somatic cell reprogramming and transdifferentiation provide new strategies for the research of translational medicine, including disease modeling, drug screening, artificial organ development, and cell therapy, recipient safety remains a concern due to the use of exogenous transcription factors during induction. To resolve this problem, new induction approaches containing clinically applicable small molecules have been explored. Small molecule epigenetic modulators such as DNA methylation writer inhibitors, histone methylation writer inhibitors, histone acy
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33

Hino, Kyosuke, Hidetaka Nagata, Manabu Shimonishi, and Motoharu Ido. "High-Throughput Screening for Small-Molecule Adiponectin Secretion Modulators." Journal of Biomolecular Screening 16, no. 6 (2011): 628–36. http://dx.doi.org/10.1177/1087057111403474.

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Adiponectin is an adipokine secreted by adipocytes and plays a role in the suppression of metabolic disorders that can result in type 2 diabetes, obesity, and atherosclerosis. Several studies have shown that upregulation of adiponectin has a number of therapeutic benefits. Although peroxisome proliferator-activated receptor γ (PPARγ) agonists are known to increase adiponectin secretion both in cultured adipocytes and humans, they have several side effects, such as weight gain, congestive heart failure, and edema. Therefore, adiponectin secretion modulators that do not possess PPARγ agonistic a
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34

Chen, Kui, Klaus Michelsen, Robert J. M. Kurzeja, et al. "Discovery of Small-Molecule Glucokinase Regulatory Protein Modulators That Restore Glucokinase Activity." Journal of Biomolecular Screening 19, no. 7 (2014): 1014–23. http://dx.doi.org/10.1177/1087057114530468.

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In the nuclei of hepatocytes, glucokinase regulatory protein (GKRP) modulates the activity of glucokinase (GK), a key regulator of glucose homeostasis. Currently, direct activators of GK (GKAs) are in development for the treatment of type 2 diabetes. However, this approach is generally associated with a risk of hypoglycemia. To mitigate such risk, we target the GKRP regulation, which indirectly restores GK activity. Here we describe a screening strategy to look specifically for GKRP modulators, in addition to traditional GKAs. Two high-throughput screening campaigns were performed with our com
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35

Shalaly, Nancy Dekki, Eduardo Aneiros, Michael Blank, et al. "Positive Modulation of the Glycine Receptor by Means of Glycine Receptor–Binding Aptamers." Journal of Biomolecular Screening 20, no. 9 (2015): 1112–23. http://dx.doi.org/10.1177/1087057115590575.

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According to the gate control theory of pain, the glycine receptors (GlyRs) are putative targets for development of therapeutic analgesics. A possible approach for novel analgesics is to develop a positive modulator of the glycine-activated Cl− channels. Unfortunately, there has been limited success in developing drug-like small molecules to study the impact of agonists or positive modulators on GlyRs. Eight RNA aptamers with low nanomolar affinity to GlyRα1 were generated, and their pharmacological properties analyzed. Cytochemistry using fluorescein-labeled aptamers demonstrated GlyRα1-depen
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36

Henderson, Andrew R., Matthew J. Henley, Nicholas J. Foster, et al. "Conservation of coactivator engagement mechanism enables small-molecule allosteric modulators." Proceedings of the National Academy of Sciences 115, no. 36 (2018): 8960–65. http://dx.doi.org/10.1073/pnas.1806202115.

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Transcriptional coactivators are a molecular recognition marvel because a single domain within these proteins, the activator binding domain or ABD, interacts with multiple compositionally diverse transcriptional activators. Also remarkable is the structural diversity among ABDs, which range from conformationally dynamic helical motifs to those with a stable core such as a β-barrel. A significant objective is to define conserved properties of ABDs that allow them to interact with disparate activator sequences. The ABD of the coactivator Med25 (activator interaction domain or AcID) is unique in
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37

Cockburn, Ingrid L., Aileen Boshoff, Eva-Rachele Pesce, and Gregory L. Blatch. "Selective modulation of plasmodial Hsp70s by small molecules with antimalarial activity." Biological Chemistry 395, no. 11 (2014): 1353–62. http://dx.doi.org/10.1515/hsz-2014-0138.

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Abstract Plasmodial heat shock protein 70 (Hsp70) chaperones represent a promising new class of antimalarial drug targets because of the important roles they play in the survival and pathogenesis of the malaria parasite Plasmodium falciparum. This study assessed a set of small molecules (lapachol, bromo-β-lapachona and malonganenones A, B and C) as potential modulators of two biologically important plasmodial Hsp70s, the parasite-resident PfHsp70-1 and the exported PfHsp70-x. Compounds of interest were assessed for modulatory effects on the steady-state basal and heat shock protein 40 (Hsp40)-
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38

Bogum, Jana, Dörte Faust, Kerstin Zühlke, et al. "Small-Molecule Screening Identifies Modulators of Aquaporin-2 Trafficking." Journal of the American Society of Nephrology 24, no. 5 (2013): 744–58. http://dx.doi.org/10.1681/asn.2012030295.

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39

Simon, Roman P., Dina Robaa, Zayan Alhalabi, Wolfgang Sippl, and Manfred Jung. "KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases." Journal of Medicinal Chemistry 59, no. 4 (2016): 1249–70. http://dx.doi.org/10.1021/acs.jmedchem.5b01502.

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40

Kiselyov, Alex S., Sergey E. Tkachenko, Konstantin V. Balakin, and Alexandre V. Ivachtchenko. "Small-molecule modulators of Hh and Wnt signaling pathways." Expert Opinion on Therapeutic Targets 11, no. 8 (2007): 1087–101. http://dx.doi.org/10.1517/14728222.11.8.1087.

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41

Mehta, Ankita, Surabhi Sonam, Isha Gouri, Saurabh Loharch, Deepak K. Sharma, and Raman Parkesh. "SMMRNA: a database of small molecule modulators of RNA." Nucleic Acids Research 42, no. D1 (2013): D132—D141. http://dx.doi.org/10.1093/nar/gkt976.

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42

Stanton, Benjamin Z., and Lee F. Peng. "Small-molecule modulators of the Sonic Hedgehog signaling pathway." Mol. BioSyst. 6, no. 1 (2010): 44–54. http://dx.doi.org/10.1039/b910196a.

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43

Seyedsayamdost, Mohammad R., Gavin Carr, Roberto Kolter, and Jon Clardy. "Roseobacticides: Small Molecule Modulators of an Algal-Bacterial Symbiosis." Journal of the American Chemical Society 133, no. 45 (2011): 18343–49. http://dx.doi.org/10.1021/ja207172s.

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44

Liu, Jiawei, Qing Zhang, Kaotang Chen, et al. "Small-molecule STAT3 Signaling Pathway Modulators from Polygonum cuspidatum." Planta Medica 78, no. 14 (2012): 1568–70. http://dx.doi.org/10.1055/s-0032-1315121.

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45

Viernes, Dennis R., Lydia B. Choi, William G. Kerr, and John D. Chisholm. "Discovery and Development of Small Molecule SHIP Phosphatase Modulators." Medicinal Research Reviews 34, no. 4 (2013): 795–824. http://dx.doi.org/10.1002/med.21305.

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46

Qiao, Yuting, Tingkai Chen, Hongyu Yang, et al. "Small molecule modulators targeting protein kinase CK1 and CK2." European Journal of Medicinal Chemistry 181 (November 2019): 111581. http://dx.doi.org/10.1016/j.ejmech.2019.111581.

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47

Füllbeck, Melanie, Nina Gebhardt, Julia Hossbach, Peter T. Daniel, and Robert Preissner. "Computer-assisted identification of small-molecule Bcl-2 modulators." Computational Biology and Chemistry 33, no. 6 (2009): 451–56. http://dx.doi.org/10.1016/j.compbiolchem.2009.10.001.

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48

Belitsky, Jason M., Micah Z. Ellowitz, Diane Lye, and Alexander L. Kilbo. "Small molecule modulators of aggregation in synthetic melanin polymerizations." Bioorganic & Medicinal Chemistry Letters 22, no. 17 (2012): 5503–7. http://dx.doi.org/10.1016/j.bmcl.2012.07.027.

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49

Khan, Pasha M., Bahaa El-Dien M. El-Gendy, Naresh Kumar та ін. "Small molecule amides as potent ROR-γ selective modulators". Bioorganic & Medicinal Chemistry Letters 23, № 2 (2013): 532–36. http://dx.doi.org/10.1016/j.bmcl.2012.11.025.

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50

Huang, Fei, and Alexander V. Mazin. "Targeting the homologous recombination pathway by small molecule modulators." Bioorganic & Medicinal Chemistry Letters 24, no. 14 (2014): 3006–13. http://dx.doi.org/10.1016/j.bmcl.2014.04.088.

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