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Journal articles on the topic 'Gamma-secretase modulators'

Author: Grafiati

Published: 4 June 2021

Last updated: 6 February 2022

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1

Rotella, David P. "Gamma Secretase Modulators." ACS Medicinal Chemistry Letters 4, no. 9 (2013): 823. http://dx.doi.org/10.1021/ml4002826.

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2

Velter, Adriana I., François P. Bischoff, Didier Berthelot, et al. "Anilinotriazoles as potent gamma secretase modulators." Bioorganic & Medicinal Chemistry Letters 24, no. 24 (2014): 5805–13. http://dx.doi.org/10.1016/j.bmcl.2014.10.024.

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3

Kukar, Thomas L., Thomas B. Ladd, Maralyssa A. Bann, et al. "P2-338: Substrate-targeting gamma-secretase modulators." Alzheimer's & Dementia 4 (July 2008): T472. http://dx.doi.org/10.1016/j.jalz.2008.05.1415.

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4

Tate, Barbara, Timothy D. McKee, Robyn M. B. Loureiro, et al. "Modulation of Gamma-Secretase for the Treatment of Alzheimer's Disease." International Journal of Alzheimer's Disease 2012 (2012): 1–10. http://dx.doi.org/10.1155/2012/210756.

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The Amyloid Hypothesis states that the cascade of events associated with Alzheimer's disease (AD)—formation of amyloid plaques, neurofibrillary tangles, synaptic loss, neurodegeneration, and cognitive decline—are triggered by Aβpeptide dysregulation (Kakuda et al., 2006, Sato et al., 2003, Qi-Takahara et al., 2005). Sinceγ-secretase is critical for Aβproduction, many in the biopharmaceutical community focused onγ-secretase as a target for therapeutic approaches for Alzheimer's disease. However, pharmacological approaches to controlγ-secretase activity are challenging because the enzyme has mul

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5

Mekala, Shekar, Grady Nelson та Yue-Ming Li. "Recent developments of small molecule γ-secretase modulators for Alzheimer's disease". RSC Medicinal Chemistry 11, № 9 (2020): 1003–22. http://dx.doi.org/10.1039/d0md00196a.

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6

Shi, Jianliang, Dmitry Zuev, Li Xu, et al. "Design and optimization of tricyclic gamma-secretase modulators." Bioorganic & Medicinal Chemistry Letters 26, no. 5 (2016): 1498–502. http://dx.doi.org/10.1016/j.bmcl.2015.06.020.

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7

Bursavich, Matthew G., Bryce A. Harrison, and Jean-François Blain. "Gamma Secretase Modulators: New Alzheimer’s Drugs on the Horizon?" Journal of Medicinal Chemistry 59, no. 16 (2016): 7389–409. http://dx.doi.org/10.1021/acs.jmedchem.5b01960.

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8

Felsenstein, Kevin, Joo-In Jung, Thomas Ladd, et al. "S1-01-04: Cholesterol metabolites as endogenous gamma-secretase modulators." Alzheimer's & Dementia 9 (July 2013): P121—P122. http://dx.doi.org/10.1016/j.jalz.2013.04.035.

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9

Rynearson, Kevin D., Ronald N. Buckle, R. Jason Herr, et al. "Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators." Bioorganic & Medicinal Chemistry 28, no. 22 (2020): 115734. http://dx.doi.org/10.1016/j.bmc.2020.115734.

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10

Rynearson, Kevin D., Ronald N. Buckle, Keith D. Barnes, et al. "Design and synthesis of aminothiazole modulators of the gamma-secretase enzyme." Bioorganic & Medicinal Chemistry Letters 26, no. 16 (2016): 3928–37. http://dx.doi.org/10.1016/j.bmcl.2016.07.011.

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11

Hobson, Scott, Martin Lenter, and Cornelia Dorner-Ciossek. "P2-400: THE EFFECTS OF GAMMA SECRETASE MODULATORS ON ABETA OLIGOMERIZATION." Alzheimer's & Dementia 10 (July 2014): P625. http://dx.doi.org/10.1016/j.jalz.2014.05.1080.

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12

Findeis, Mark, Frank Schroeder, Steffen Creaser, Timothy McKee, and Weiming Xia. "Natural Product and Natural Product-Derived Gamma Secretase Modulators from Actaea Racemosa Extracts." Medicines 2, no. 3 (2015): 127–40. http://dx.doi.org/10.3390/medicines2030127.

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13

Tomita, Taisuke. "S2-03-02: Molecular mechanism of action of gamma-secretase inhibitors and modulators." Alzheimer's & Dementia 6 (July 2010): S93. http://dx.doi.org/10.1016/j.jalz.2010.05.286.

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14

Oborski, Christine E. J., Christine Parker, Martin Pettersson, Douglas S. Johnson, Rathna Iyer, and Kelly Bales. "P1-296: Gamma-secretase inhibitors and gamma-secretase modulators differentially regulate amyloid-beta 42 peptide generation in native brain membrane preparations from multiple species." Alzheimer's & Dementia 6 (July 2010): S259. http://dx.doi.org/10.1016/j.jalz.2010.05.848.

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15

Wuli, Wei, Sheng-Tzung Tsai, Tzyy-Wen Chiou, and Horng-Jyh Harn. "Human-Induced Pluripotent Stem Cells and Herbal Small-Molecule Drugs for Treatment of Alzheimer’s Disease." International Journal of Molecular Sciences 21, no. 4 (2020): 1327. http://dx.doi.org/10.3390/ijms21041327.

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Alzheimer’s disease (AD) is characterized by extracellular amyloid plaques composed of the β-amyloid peptides and intracellular neurofibrillary tangles and associates with progressive declines in memory and cognition. Several genes play important roles and regulate enzymes that produce a pathological accumulation of β-amyloid in the brain, such as gamma secretase (γ-secretase). Induced pluripotent stem cells from patients with Alzheimer’s disease with different underlying genetic mechanisms may help model different phenotypes of Alzheimer’s disease and facilitate personalized drug screening pl

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16

Li, Hongmei, Jun Qin, Pawan Dhondi, et al. "The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer’s disease." Bioorganic & Medicinal Chemistry Letters 23, no. 2 (2013): 466–71. http://dx.doi.org/10.1016/j.bmcl.2012.11.055.

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17

Harrison, David C., Julie Hawkins, Sharlin Ahmed, et al. "P2-329: Lowering of brain and plasma Abeta42 in rats using gamma-secretase modulators." Alzheimer's & Dementia 4 (July 2008): T469. http://dx.doi.org/10.1016/j.jalz.2008.05.1406.

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18

Nye, Jeffrey S. "S2-03-06 NSAID modulators of the gamma secretase: high throughput tools and mechanistic insights." Neurobiology of Aging 25 (July 2004): S29. http://dx.doi.org/10.1016/s0197-4580(04)80096-4.

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19

Austin, Wesley F., Jed L. Hubbs, Nathan O. Fuller, et al. "SAR investigations on a novel class of gamma-secretase modulators based on a unique scaffold." MedChemComm 4, no. 3 (2013): 569. http://dx.doi.org/10.1039/c3md20357c.

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20

Wood, Kathleen M., Cathleen Gonzales, Feng Pan, et al. "P4-315: Evaluating amyloid-beta processing using novel gamma-secretase modulators in preclinical animal models." Alzheimer's & Dementia 11, no. 7S_Part_19 (2015): P905. http://dx.doi.org/10.1016/j.jalz.2015.08.145.

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21

Han, Jonghee, Jiyeon Jang та Yong-Keun Jung. "P4-213: Novel gamma-secretase modulators (γSecAs) increase Aβ generation by enhancing its enzymatic activity". Alzheimer's & Dementia 4 (липень 2008): T734. http://dx.doi.org/10.1016/j.jalz.2008.05.2281.

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22

Lu, Yasong, Kathleen Wood, Stefanus Steyn, et al. "P1-252: Gamma-secretase modulators demonstrate similar exposure-response relationship in the rat and guinea pig." Alzheimer's & Dementia 8, no. 4S_Part_5 (2012): P194. http://dx.doi.org/10.1016/j.jalz.2012.05.533.

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23

Raven, Frank, Joseph F. Ward, Katarzyna M. Zoltowska та ін. "Soluble Gamma-secretase Modulators Attenuate Alzheimer's β-amyloid Pathology and Induce Conformational Changes in Presenilin 1". EBioMedicine 24 (жовтень 2017): 93–101. http://dx.doi.org/10.1016/j.ebiom.2017.08.028.

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24

Bronk, Brian, Barbara Tate, Robyn Loureiro, et al. "P1-028: Gamma-secretase modulators do not show a potency shift in high expressing model systems." Alzheimer's & Dementia 7 (July 2011): S119—S120. http://dx.doi.org/10.1016/j.jalz.2011.05.308.

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25

Rogers, Kathryn, Richard Chesworth, Kevin Felsenstein та ін. "P3-291: Putative gamma secretase modulators lower Aβ42 in multiple in vitro and in vivo models". Alzheimer's & Dementia 5, № 4S_Part_14 (2009): P428—P429. http://dx.doi.org/10.1016/j.jalz.2009.04.962.

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26

Gerlach, Kai, Scott Hobson, Christian Eickmeier, et al. "Discovery of tetrahydroindazoles as a novel class of potent and in vivo efficacious gamma secretase modulators." Bioorganic & Medicinal Chemistry 26, no. 12 (2018): 3227–41. http://dx.doi.org/10.1016/j.bmc.2018.04.053.

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27

Huang, Xianhai, Dmitri Pissarnitski, Hongmei Li, et al. "Efficient synthesis and reaction pathway studies of novel fused morpholine oxadiazolines for use as gamma secretase modulators." Tetrahedron Letters 53, no. 47 (2012): 6451–55. http://dx.doi.org/10.1016/j.tetlet.2012.09.070.

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28

Bursavich, Matthew G., Bryce A. Harrison, Raksha Acharya, et al. "Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer’s Disease." Journal of Medicinal Chemistry 60, no. 6 (2017): 2383–400. http://dx.doi.org/10.1021/acs.jmedchem.6b01620.

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29

Jumpertz, Thorsten, Andreas Rennhack, Julia Ness, et al. "O1-11-06: Presenilin is the molecular target of both acidic and non-acidic gamma-secretase modulators." Alzheimer's & Dementia 8, no. 4S_Part_3 (2012): P105—P106. http://dx.doi.org/10.1016/j.jalz.2012.05.268.

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30

Koo, Edward. "S1-02-05: Gamma-secretase modulators, nonsteroidal anti-inflammatory drugs, and Alzheimer's disease: A review and update." Alzheimer's & Dementia 4 (July 2008): T102. http://dx.doi.org/10.1016/j.jalz.2008.05.194.

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31

Findeis, Mark A., Frank Schroeder, Timothy D. McKee, et al. "Discovery of a Novel Pharmacological and Structural Class of Gamma Secretase Modulators Derived from the Extract of Actaea racemosa." ACS Chemical Neuroscience 3, no. 11 (2012): 941–51. http://dx.doi.org/10.1021/cn3000857.

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32

Luebbers, Thomas, Anja Limberg, Synese Jolidon, et al. "P1-246: N-heteroaryl-piperidinyl-4-amines as selective GAMMA secretase modulators for the potential treatment of Alzheimer's disease." Alzheimer's & Dementia 8, no. 4S_Part_5 (2012): P192. http://dx.doi.org/10.1016/j.jalz.2012.05.525.

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33

Hubbs, Jed L., Nathan O. Fuller, Wesley F. Austin, et al. "Minimization of drug–drug interaction risk and candidate selection in a natural product-based class of gamma-secretase modulators." Bioorganic & Medicinal Chemistry Letters 25, no. 7 (2015): 1621–26. http://dx.doi.org/10.1016/j.bmcl.2015.01.051.

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34

Schmidt, Boris, Stefanie Baumann, Nicole Hoettecke, et al. "IC-P3-212: Mapping the binding site of gamma-secretase modulators by small (and not so small) organic molecules." Alzheimer's & Dementia 4 (July 2008): T91. http://dx.doi.org/10.1016/j.jalz.2008.05.157.

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35

Ruzaeva, V. A., A. V. Morgun, E. D. Khilazheva, et al. "Development of blood-brain barrier under the modulation of HIF activity in astroglial and neuronal cells in vitro." Biomeditsinskaya Khimiya 62, no. 6 (2016): 664–69. http://dx.doi.org/10.18097/pbmc20166206664.

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Barriergenesis is the process of maturation of the primary vascular network of the brain responsible for the establishment of the blood-brain barrier. It represents a combination of factors that, on the one hand, contribute to the process of migration and tubulogenesis of endothelial cells (angiogenesis), on the other hand, contribute to the formation of new connections between endothelial cells and other elements of the neurovascular unit. Astrocytes play a key role in barriergenesis, however, mechanisms of their action are still poorly examined. We have studied the effects of HIF-1 modulator

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36

Loureiro, Robyn, Timothy McKee, Jo Ann Dumin, et al. "O1-11-01: Satori gamma-secretase modulators are efficacious in wild-type rodents following either acute or steady-state dosing." Alzheimer's & Dementia 8, no. 4S_Part_3 (2012): P104. http://dx.doi.org/10.1016/j.jalz.2012.05.263.

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37

Cusulin, Carlo, Isabelle Wells, Solveig Badillo, Gonzalo Christian Duran-Pacheco, Karlheinz Baumann та Christoph Patsch. "Gamma secretase modulators and BACE inhibitors reduce Aβ production without altering gene expression in Alzheimer's disease iPSC-derived neurons and mice". Molecular and Cellular Neuroscience 100 (жовтень 2019): 103392. http://dx.doi.org/10.1016/j.mcn.2019.103392.

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38

Portelius, Erik, Robert A. Dean, Bianca Van Broeck, et al. "O4-06-04: Acute effect on novel Abeta isoforms in cerebrospinal fluid as a response to treatment with gamma-secretase inhibitors and modulators in Alzheimer's disease." Alzheimer's & Dementia 6 (July 2010): S160. http://dx.doi.org/10.1016/j.jalz.2010.05.499.

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39

Mandal, Mihirbaran, Carolee Lavey, Alexei V. Buevich, Zhaoning Zhu, Andrew W. Stamford, and Xiaoxiang Liu. "On the power of super acid—iodination of aromatic ring in the presence of imidazole moiety of the potent gamma secretase modulators (GSM) en route to tritium labeling." Tetrahedron Letters 53, no. 14 (2012): 1725–27. http://dx.doi.org/10.1016/j.tetlet.2012.01.085.

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40

Figueroa, David J., Jill A. Morris, Lei Ma, et al. "Presenilin-Dependent Gamma-Secretase Activity Modulates Neurite Outgrowth." Neurobiology of Disease 9, no. 1 (2002): 49–60. http://dx.doi.org/10.1006/nbdi.2001.0447.

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41

Hashimoto, Toshihide, Akira Ishibashi, Hiroaki Hagiwara, Yoshiyuki Murata, Osamu Takenaka, and Takehiko Miyagawa. "P1-236: E2012: A novel gamma-secretase modulator-pharmacology part." Alzheimer's & Dementia 6 (July 2010): S242. http://dx.doi.org/10.1016/j.jalz.2010.05.787.

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42

Hou, Huayan, Demian Obregon, M. D. Shahaduzzaman, et al. "P2-287: sAPP-alpha modulates gamma-secretase processing of APP." Alzheimer's & Dementia 7 (July 2011): S402—S403. http://dx.doi.org/10.1016/j.jalz.2011.05.1165.

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43

Amino, Hiroyuki, Hiroaki Hagiwara, Yoshiyuki Murata, Hideki Watanabe, Takeo Sasaki, and Takehiko Miyagawa. "P3-307: E2012: A novel gamma-secretase modulator-mechanism of action." Alzheimer's & Dementia 6 (July 2010): S541—S542. http://dx.doi.org/10.1016/j.jalz.2010.05.1808.

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44

Irizarry, Michael C., Amy Deng, Alberto Lleo, et al. "Apolipoprotein E modulates gamma-secretase cleavage of the amyloid precursor protein." Journal of Neurochemistry 90, no. 5 (2004): 1132–43. http://dx.doi.org/10.1111/j.1471-4159.2004.02581.x.

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45

Alasmari, Fawaz, Musaad A. Alshammari, Abdullah F. Alasmari, Wael A. Alanazi, and Khalid Alhazzani. "Neuroinflammatory Cytokines Induce Amyloid Beta Neurotoxicity through Modulating Amyloid Precursor Protein Levels/Metabolism." BioMed Research International 2018 (October 25, 2018): 1–8. http://dx.doi.org/10.1155/2018/3087475.

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Neuroinflammation has been observed in association with neurodegenerative diseases including Alzheimer’s disease (AD). In particular, a positive correlation has been documented between neuroinflammatory cytokine release and the progression of the AD, which suggests these cytokines are involved in AD pathophysiology. A histological hallmark of the AD is the presence of beta-amyloid (Aβ) plaques and tau neurofibrillary tangles. Beta-amyloid is generated by the sequential cleavage of beta (β) and gamma (γ) sites in the amyloid precursor protein (APP) by β- and γ-secretase enzymes and its accumula

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46

Loureiro, Robyn M., Jo Dumin, Timothy D. McKee, et al. "Efficacy of SPI-1865, a novel gamma-secretase modulator, in multiple rodent models." Alzheimer's Research & Therapy 5, no. 2 (2013): 19. http://dx.doi.org/10.1186/alzrt173.

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47

D'Agostino, Carla, Mafalda Cacciottolo, Constantinos Sioutas, et al. "NOVEL GAMMA-SECRETASE MODULATOR REGULATES APP PROCESSING AND INFLAMMATORY RESPONSES IN NPM-EXPOSED MICE." Innovation in Aging 3, Supplement_1 (2019): S93. http://dx.doi.org/10.1093/geroni/igz038.353.

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Abstract Air pollution is associated with accelerated cognitive decline and increased risk of dementia in older populations (Cacciottolo et al 2017; Chen et al 2017). Rodent models of air pollution exposure also show Alzheimer-like changes including glial inflammatory responses and increased levels of endogenous amyloid beta (Aβ) peptides (Cacciottolo et al 2017 Levesque et al 2011). We hypothesized that pharmacological inhibition of Aβ production during nPM exposure would attenuate the amyloidogenic processing of APP and glial inflammatory responses. This hypothesis was tested using the γ-sec

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48

Felsenstein, Kevin M., Darcie Spaulding, Zhiyong Yang, et al. "P3-295: Pharmacokinetic and pharmacodynamic analysis of the gamma-secretase modulator (GSM) EVP-0015962." Alzheimer's & Dementia 6 (July 2010): S538. http://dx.doi.org/10.1016/j.jalz.2010.05.1795.

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49

Giovannini, Catia, Francesca Fornari, Fabio Piscaglia, and Laura Gramantieri. "Notch Signaling Regulation in HCC: From Hepatitis Virus to Non-Coding RNAs." Cells 10, no. 3 (2021): 521. http://dx.doi.org/10.3390/cells10030521.

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The Notch family includes evolutionary conserved genes that encode for single-pass transmembrane receptors involved in stem cell maintenance, development and cell fate determination of many cell lineages. Upon activation by different ligands, and depending on the cell type, Notch signaling plays pleomorphic roles in hepatocellular carcinoma (HCC) affecting neoplastic growth, invasion capability and stem like properties. A specific knowledge of the deregulated expression of each Notch receptor and ligand, coupled with resultant phenotypic changes, is still lacking in HCC. Therefore, while inter

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50

Nagy, Christa, Edgar Schuck, Akira Ishibashi, Yosuke Nakatani, Bhaskar Rege та Veronika Logovinsky. "P3-415: E2012, a novel gamma-secretase modulator, decreases plasma amyloid-beta (Aβ) levels in humans". Alzheimer's & Dementia 6 (липень 2010): S574. http://dx.doi.org/10.1016/j.jalz.2010.05.1958.

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