analog synthesis
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2022 ◽  
Vol 2146 (1) ◽  
pp. 012042
Author(s):  
Yongfu Liu

Abstract In order to improve the integration of digital prints, this paper proposes a new method of printmaking analog synthesis, that is, using interactive technology.. Firstly, Harris corner algorithm is used to collect and preprocess the adjacent feature points of digital printmaking image, and the texture features of digital printmaking image are extracted, so as to construct the texture information transmission model of digital printmaking image; Secondly, with the help of segmentation technology to process the digital print image, the dynamic feature segmentation is carried out, the local binary fitting method is used to enhance and repair the digital print image information, and the information fusion method based on interactive technology is used to complete the analog synthesis of digital print image; Finally, the simulation results show that the method has good performance of simulation synthesis and strong information fusion ability.


2021 ◽  
Author(s):  
Danny Hung-Chieh Chou ◽  
Nai-Pin Lin ◽  
Yi Zhang ◽  
Nicolas Szabo-Fresnais

The B-chain C-terminal region of insulin has been mutated or modified to achieve improved therapeutic efficacies. For ex-ample, all FDA-approved insulin analogs have altered C-terminal segments, which leads to improved pharmacokinetic prop-erties and provide significant clinical benefits on blood sugar regulation. Nonetheless, there is still no efficient method to synthesize insulin analogs with the altered C-terminal region. Herein, we report a facile synthesis using omniligase-1 to li-gate an insulin core with a peptide segment in high conversion. We further apply this ligation to M13 phage surface modifi-cations and demonstrate that the phage displayed insulin molecules can bind to insulin receptor ectodomain in an insulin-dependent manner. These results pave the way for building phage display insulin library for therapeutic selections and demonstrate the feasibility of using omniligase-1 to display other disulfide-rich peptides and proteins on phage.


2021 ◽  
Author(s):  
zongqiang wang ◽  
Amanda Kasper ◽  
Rabia Mehmood ◽  
Melinda Ternei ◽  
Shaogang Li ◽  
...  

Author(s):  
zongqiang wang ◽  
Amanda Kasper ◽  
Rabia Mehmood ◽  
Melinda Ternei ◽  
Shaogang Li ◽  
...  

2021 ◽  
pp. 153250
Author(s):  
Shinji Tanaka ◽  
Sho Yoshinaka ◽  
Kiyoshi Kawamura ◽  
Mikio Morita ◽  
Masato Kitamura

2020 ◽  
Vol 63 (4) ◽  
pp. 308-313
Author(s):  
V. V. Romashov ◽  
K. A. Yakimenko ◽  
A. N. Doktorov ◽  
L. V. Romashova

Chemosphere ◽  
2020 ◽  
Vol 250 ◽  
pp. 126606 ◽  
Author(s):  
Shuaishuai Zhang ◽  
Jingpeng Song ◽  
Qing Du ◽  
Kui Cheng ◽  
Fan Yang

2020 ◽  
Vol 84 (8) ◽  
pp. 1560-1569
Author(s):  
Yamato Miyazawa ◽  
Kenji Kawaguchi ◽  
Ryo Katsuta ◽  
Tomoo Nukada ◽  
Ken Ishigami
Keyword(s):  

Viruses ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 452 ◽  
Author(s):  
Sanjeev Kumar V. Vernekar ◽  
Rajkumar Lalji Sahani ◽  
Mary C. Casey ◽  
Jayakanth Kankanala ◽  
Lei Wang ◽  
...  

HIV-1 capsid protein (CA) plays an important role in many steps of viral replication and represents an appealing antiviral target. Several CA-targeting small molecules of various chemotypes have been studied, but the peptidomimetic PF74 has drawn particular interest due to its potent antiviral activity, well-characterized binding mode, and unique mechanism of action. Importantly, PF74 competes against important host factors for binding, conferring highly desirable antiviral phenotypes. However, further development of PF74 is hindered by its prohibitively poor metabolic stability, which necessitates the search for structurally novel and metabolically stable chemotypes. We have conducted a pharmacophore-based shape similarity search for compounds mimicking PF74. We report herein the analog synthesis and structure-activity relationship (SAR) of two hits from the search, and a third hit designed via molecular hybridization. All analogs were characterized for their effect on CA hexamer stability, antiviral activity, and cytotoxicity. These assays identified three active compounds that moderately stabilize CA hexamer and inhibit HIV-1. The most potent analog (10) inhibited HIV-1 comparably to PF74 but demonstrated drastically improved metabolic stability in liver microsomes (31 min vs. 0.7 min t1/2). Collectively, the current studies identified a structurally novel and metabolically stable PF74-like chemotype for targeting HIV-1 CA.


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