Novel mTORC2/HSPB4 Interaction: Role and Regulation of HSPB4 T148 Phosphorylation

Autor: Zachary B. Sluzala, Yang Shan, Lynda Elghazi, Emilio L. Cárdenas, Angelina Hamati, Amanda L. Garner, Patrice E. Fort

Publikováno v: Cells, Vol 13, Iss 23, p 2000 (2024)

HSPB4 and HSPB5 (α-crystallins) have shown increasing promise as neuroprotective agents, demonstrating several anti-apoptotic and protective roles in disorders such as multiple sclerosis and diabetic retinopathy. HSPs are highly regulated by post-tr

Externí odkaz: https://doaj.org/article/2b6f5966d9104b4b8a0851e5050482a7

Highly stereoselective asymmetric aldol routes to tert-butyl-2-(3,5-difluorophenyl)-1-oxiran-2-yl)ethyl)carbamates: Building blocks for novel protease inhibitors

Autor: Arun K. Ghosh, Emilio L. Cárdenas, Margherita Brindisi

Publikováno v: Tetrahedron Letters. 58:4062-4065

Enantioselective syntheses of tert -butyl (( S )-2-(3,5-difluorophenyl)-1-(( S )-oxiran-2-yl)ethyl)carbamate and (( S )-2-(3,5-difluorophenyl)-1-(( R )-oxiran-2-yl)ethyl)carbamate are described. We utilized asymmetric syn- and anti- aldol reactions t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b0007fbea2fd6587ff2b71ba2ad712b
https://doi.org/10.1016/j.tetlet.2017.09.025

Highly Selective and Potent Human β-Secretase 2 (BACE2) Inhibitors against Type 2 Diabetes: Design, Synthesis, X-ray Structure and Structure-Activity Relationship Studies

Autor: Emma K. Lendy, Bhavanam Sekhara Reddy, Satish Kovela, Emilio L. Cárdenas, Andrew D. Mesecar, Yu-Chen Yen, Margherita Brindisi, Xiangping Huang, Jordan Tang, Arun K. Ghosh, Deborah Downs, Kalapala Venketeswara Rao

Publikováno v: ChemMedChem. 14(5)

Herein we present the design, synthesis, and biological evaluation of potent and highly selective β-secretase 2 (memapsin 1, beta-site amyloid precursor protein cleaving enzyme 2, or BACE 2) inhibitors. BACE2 has been recognized as an exciting new t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9fba27ca172570d648b5c71e66b4c56d
https://pubmed.ncbi.nlm.nih.gov/30637955

Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1 '-P2 ' ligands

Autor: Andrew D. Mesecar, Emilio L. Cárdenas, Jordan Tang, Yu-Chen Yen, Margherita Brindisi, Xiangping Huang, Nagaswamy Kumaragurubaran, Jean Rene Ella-Menye, Arun K. Ghosh

We report the design and synthesis of a series of BACE1 inhibitors incorporating mono- and bicyclic 6-substituted 2-oxopiperazines as novel P1′ and P2′ ligands and isophthalamide derivative as P2-P3 ligands. Among mono-substituted 2-oxopiperazine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ae81974b3994c5ead563c93b995ec91
http://hdl.handle.net/11588/771128

Design, synthesis and in vitro splicing inhibition of desmethyl and carba-derivatives of herboxidiene

Autor: Emilio L. Cárdenas, Nianchun Ma, Arun K. Ghosh, Melissa S. Jurica, Kerstin A. Effenberger, Kai Lv

Publikováno v: Organic & biomolecular chemistry, vol 14, iss 23
Ghosh, AK; Lv, K; Ma, N; Cardenas, EL; Effenberger, KA; & Jurica, MS. (2016). Design, synthesis and in vitro splicing inhibition of desmethyl and carba-derivatives of herboxidiene. ORGANIC & BIOMOLECULAR CHEMISTRY, 14(23), 5263-5271. doi: 10.1039/c6ob00725b. UC Santa Cruz: Retrieved from: http://www.escholarship.org/uc/item/5549r8bw

Herboxidiene is a potent inhibitor of spliceosomes. It exhibits excellent anticancer activity against multiple human cancer cell lines. Herein, we describe an enantioselective synthesis of a desmethyl derivative and the corresponding carba-derivative

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59a56230727890db00f04d940c46563e
https://escholarship.org/uc/item/5549r8bw