Results 181 to 190 of about 26,623 (217)

BACE1 interacts with lipid raft proteins

Journal of Neuroscience Research, 2006
AbstractA neuropathological hallmark of Alzheimer's disease is the presence of amyloid plaques in the brain. Amyloid‐β peptide (Aβ) is the major constituent of the plaques and is generated by proteolytic cleavages of amyloid precursor protein (APP) by β‐ and γ‐secretases. Growing evidence shows that lipid rafts are critically involved in regulating the
Chinatsu, Hattori, Masashi, Asai, Hayato, Onishi, Noboru, Sasagawa, Yasuhiro, Hashimoto, Takaomi C, Saido, Kei, Maruyama, Shigehiko, Mizutani, Shoichi, Ishiura   +8 more
openaire   +2 more sources

Carbazole-containing arylcarboxamides as BACE1 inhibitors

Bioorganic & Medicinal Chemistry Letters, 2011
β-Secretase (BACE1) is widely recognized as a prime drug target for the treatment of Alzheimer's disease (AD). In this Letter, we report the synthesis and the BACE1 inhibitory activity of novel, variously substituted N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-arylcarboxamides.
BERTINI, SIMONE, Asso V, Ghilardi E, GRANCHI, CARLOTTA, MANERA, CLEMENTINA, MINUTOLO, FILIPPO, SACCOMANNI, GIUSEPPE, Bortolato A, Mason J, Moro S, MACCHIA, MARCO   +10 more
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Discovery of potent iminoheterocycle BACE1 inhibitors

Bioorganic & Medicinal Chemistry Letters, 2014
The synthesis of a series of iminoheterocycles and their structure-activity relationships (SAR) as inhibitors of the aspartyl protease BACE1 will be detailed. An effort to access the S3 subsite directly from the S1 subsite initially yielded compounds with sub-micromolar potency.
John P, Caldwell, Robert D, Mazzola, James, Durkin, Joseph, Chen, Xia, Chen, Leonard, Favreau, Matthew, Kennedy, Reshma, Kuvelkar, Julie, Lee, Nansie, McHugh, Brian, McKittrick, Peter, Orth, Andrew, Stamford, Corey, Strickland, Johannes, Voigt, Liyang, Wang, Lili, Zhang, Qi, Zhang, Zhaoning, Zhu   +18 more
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Thiophene substituted acylguanidines as BACE1 inhibitors

Bioorganic & Medicinal Chemistry Letters, 2007
A series of thiophene-substituted acylguanidines were designed from a pyrrole substituted acylguanidine HTS lead. This template allowed a greater flexibility, through differential Suzuki couplings, to explore the binding site of BACE1 and to enhance the inhibitory potencies.
William F, Fobare, William R, Solvibile, Albert J, Robichaud, Michael S, Malamas, Eric, Manas, Jim, Turner, Yun, Hu, Erik, Wagner, Rajiv, Chopra, Rebecca, Cowling, Guixan, Jin, Jonathan, Bard   +11 more
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miR-29c regulates BACE1 protein expression

Brain Research, 2011
Recently, BACE1 expression was shown to be regulated by microRNAs, small endogenous RNA molecules that regulate protein expression through sequence-specific interaction with messenger RNA. Here, we showed that microRNA-29c (miR-29c), a miRNA that is enriched in the brain and highly expressed in the APPswe/PSΔE9 mouse lowers BACE1 protein in vitro and ...
Yuanyuan, Zong, Hailin, Wang, Wei, Dong, XiongZhi, Quan, Hua, Zhu, YanFeng, Xu, Lan, Huang, Chunmei, Ma, Chuan, Qin   +8 more
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Pyridinyl aminohydantoins as small molecule BACE1 inhibitors

Bioorganic & Medicinal Chemistry Letters, 2010
A novel class of pyridinyl aminohydantoins was designed and prepared as highly potent BACE1 inhibitors. Compound (S)-4g showed excellent potency with IC(50) of 20 nM for BACE1. X-ray crystallography indicated that the interaction between pyridine nitrogen and the tryptophan Trp76 was a key feature in the S2' region of the enzyme that contributed to ...
Ping, Zhou, Yanfang, Li, Yi, Fan, Zheng, Wang, Rajiv, Chopra, Andrea, Olland, Yun, Hu, Ronald L, Magolda, Menelas, Pangalos, Peter H, Reinhart, M James, Turner, Jonathan, Bard, Michael S, Malamas, Albert J, Robichaud   +13 more
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Cerebrovascular Endothelial Dysfunction: Role of BACE1

Arteriosclerosis, Thrombosis, and Vascular Biology
Dysfunctional endothelium is increasingly recognized as a mechanistic link between cardiovascular risk factors and dementia, including Alzheimer disease. BACE1 (β-site amyloid-β precursor protein-cleaving enzyme 1) is responsible for β-processing of APP (amyloid-β precursor protein), the first step in the production of Aβ (amyloid-β) peptides, major ...
Zvonimir S. Katusic, Livius V. d’Uscio, Tongrong He   +2 more
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Evaluation of transition-state mimics in a superior BACE1 cleavage sequence as peptide-mimetic BACE1 inhibitors

Bioorganic & Medicinal Chemistry, 2015
A superior substrate sequence for BACE1 containing transition-state mimics at the scissile site was evaluated as a protease inhibitor. Hydroxymethylcarbonyl (HMC) and hydroxyethylamine (HEA) isosteres were selected as the transition state mimics, and incorporated into the scissile site of the superior sequence covering the P4 to P1' sites (Glu-Ile-Thi ...
Yasunao Hattori, Kazuya Kobayashi, Ayaka Deguchi, Yukie Nohara, Tomomi Akiyama, Kenta Teruya, Akira Sanjoh, Atsushi Nakagawa, Eiki Yamashita, Kenichi Akaji   +9 more
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BACE1 Inhibitory Meroterpenoids from Aspergillus terreus

Journal of Natural Products, 2018
Sixteen 3,5-dimethylorsellinic acid-based (DMOA-based) meroterpenoids, including 10 new compounds, asperterpenes D-M (1-10), were obtained from Aspergillus terreus. The structures and absolute configurations of the new compounds were confirmed by extensive spectroscopy, single-crystal X-ray diffraction analysis, and experimental electronic circular ...
Changxing Qi, Mengting Liu, Qun Zhou, Weixi Gao, Chunmei Chen, Yongji Lai, Zhengxi Hu, Yongbo Xue, Jinwen Zhang, Dongyan Li, Xiao-Nian Li, Qing Zhang, Jianping Wang, Hucheng Zhu, Yonghui Zhang   +14 more
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BACE1 Dependent Neuregulin Proteolysis.

Current Alzheimer research
Neuregulin-1 (NRG1), which is also called acetylcholine receptor inducing activity (ARIA) or glial growth factor (GGF), signals as a ligand of ErbB receptors in a variety of important developmental processes but also later in life. NRG1 mediated signaling is crucial for cardiogenesis and the development of the breast.
D, Fleck, A N, Garratt, C, Haass, M, Willem   +3 more
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