174884-11-8Relevant academic research and scientific papers
A Strategy to Prepare Peptide Heterodimers in the Solid Phase with an Acid-Labile Linker
Wang, Gang,Chen, Tingting,Peng, Tao,Zhang, Shouguo,Wang, Junyi,Wen, Xiaoxue,Yang, Xiaoming,Wang, Lin
, p. 7351 - 7355 (2019)
The currently synthetic methods of peptide heterodimer involve tedious synthesis and purification steps. An acid-labile traceless linker was prepared, which is highly compatible with the Fmoc strategy and could be used to prepare peptide heterodimer on re
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models
Nguyen, William,Jacobson, Jonathan,Jarman, Kate E.,Jousset Sabroux, Helene,Harty, Leigh,McMahon, James,Lewin, Sharon R.,Purcell, Damian F.,Sleebs, Brad E.
, p. 5148 - 5175 (2019/05/28)
The persistent reservoir of cells latently infected with human immunodeficiency virus (HIV)-integrated proviral DNA necessitates lifelong suppressive antiretroviral therapy (ART). Epigenetic targeted compounds have shown promise as potential latency-reversing agents; however, these drugs have undesirable toxicity and lack specificity for HIV. We utilized a novel HEK293-derived FlpIn dual-reporter cell line, which quantifies specific HIV provirus reactivation (LTR promoter) relative to nonspecific host cell gene expression (CMV promoter), to identify the 5-substituted 2-acylaminothiazole hit class. Here, we describe the optimization of the hit class, defining the functionality necessary for HIV gene activation and for improving in vitro metabolism and solubility. The optimized compounds displayed enhanced HIV gene expression in HEK293 and Jurkat 10.6 latency cellular models and increased unspliced HIV RNA in resting CD4+ T cells isolated from HIV-infected individuals on ART, demonstrating the potential of the 2-acylaminothiazole class as latency-reversing agents.
Chemoselective and site-selective peptide and native protein modification enabled by aldehyde auto-oxidation
Purushottam, Landa,Adusumalli, Srinivasa Rao,Chilamari, Maheshwerreddy,Rai, Vishal
, p. 959 - 962 (2017/01/17)
We report a chemoselective and site-selective formylation of ?-amine in native proteins. The aldehyde auto-oxidation re-routing, regulated generation of formate, and reversible N-terminus protection drive the transformation. It labels a single ?-amine in a pool of its copies, other nucleophilic residues, and α-amine. The extension of the methodology leads to site-selective acylation.
PYRAZOLE AMIDE DERIVATIVES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE
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Page/Page column 33, (2008/06/13)
Pyrazole amides are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
