Biopharmaceutical drug discovery using novel protein scaffolds

2006 ◽  
Vol 17 (6) ◽  
pp. 653-658 ◽  
Author(s):  
Davinder S Gill ◽  
Nitin K Damle
Keyword(s):  
Drug Discovery ◽  
Protein Scaffolds ◽  
Novel Protein

Mimicry and antagonism in biotechnology drug discovery: Recognition peptides in protein scaffolds

Proteins ◽  
1991 ◽  
pp. 277-282
Author(s):  
Irwin M. Chaiken ◽  
Tom J. Graddis ◽  
Feng Xian Lu ◽  
Michael Brigham-Burke ◽  
Sergio Rosé ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Protein Scaffolds

In-silico Structure-Based Drug Discovery of Candidate Drugs against Novel Protein Receptor Complex Nsp10-Nsp16 of SARS-CoV-2 using Drug Repurposing Approach

Coronaviruses ◽  
2020 ◽  
Vol 01 ◽  
Author(s):  
Abhishek Sengupta ◽  
Pooja Vijayaraghavan ◽  
Priyansh Srivastava ◽  
Lovely Gupta ◽  
Chaitanya Chandwani ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Drug Repurposing ◽  
Antiviral Drugs ◽  
Receptor Complex ◽  
Tanimoto Similarity ◽  
Protein Receptor ◽  
Complex Protein ◽  
Positive Results ◽  
Novel Protein

Background: Several therapeutic possibilities have been explored against Severe Acute Respiratory Syndrome-2 (SARS-CoV-2), such as convalescent plasma (CP), intravenous immunoglobulin (IVIG) and monoclonal antibodies. Compounds such as hydroxychloroquine have also been found to have fatal drawbacks. Repurposing of existing antiviral drugs can be an effective strategy, which could fasten up the process of drug discovery. Objective: The present study is designed to predict the computational efficacy of pre-existing antiviral drugs as inhibitors for the Nsp10-Nsp16 complex protein of SARS-CoV-2. Method: Twenty-six known antiviral drugs along with their similar structures based on Tanimoto similarity were screened towards Nsp10-Nsp16 complex’s active site. Result: Our study reports competitive binding of 1-[3-[2-(2-Ethoxyphenoxy) ethylamino]-2-hydroxypropyl] -9H-carbazol-4- ol against AdoMet binding site in Nsp10-Nsp16 complex. Formation of the stable ligand-receptor complex with 1-[3-[2-(2- Ethoxyphenoxy) ethylamino]-2-hydroxypropyl] -9H-carbazol-4-ol could functionally inhibit the Nsp10-Nsp16 complex, thereby making the SARS-CoV-2 vulnerable to host immuno-surveillance mechanisms. Conclusion: We conclude that these computational hits can display positive results in in-vitro trials against SARS-CoV-2.

The Present and Future of Novel Protein Degradation Technology

2019 ◽  
Vol 19 (20) ◽  
pp. 1784-1788 ◽  
Author(s):  
Liwen Xia ◽  
Wei Liu ◽  
Yinsen Song ◽  
Hailiang Zhu ◽  
Yongtao Duan
Keyword(s):  
Drug Discovery ◽  
Protein Degradation ◽  
Ubiquitin Proteasome System ◽  
Vital Role ◽  
Therapeutic Modality ◽  
Bifunctional Molecules ◽  
Subsequent Degradation ◽  
Ubiquitin Proteasome ◽  
Future Direction ◽  
Novel Protein

Proteolysis targeting chimeras (PROTACs), as a novel therapeutic modality, play a vital role in drug discovery. Each PROTAC contains three key parts; a protein-of-interest (POI) ligand, a E3 ligase ligand, and a linker. These bifunctional molecules could mediate the degradation of POIs by hijacking the activity of E3 ubiquitin ligases for POI ubiquitination and subsequent degradation via the ubiquitin proteasome system (UPS). With several advantages over other therapeutic strategies, PROTACs have set off a new upsurge of drug discovery in recent years. ENDTAC, as the development of PROTACs technology, is now receiving more attention. In this review, we aim to summarize the rapid progress from 2018 to 2019 in protein degradation and analyze the challenges and future direction that need to be addressed in order to efficiently develop potent protein degradation technology.

Recent advances in the development of novel protein scaffolds based therapeutics

2017 ◽  
Vol 102 ◽  
pp. 630-641 ◽  
Author(s):  
Asim Azhar ◽  
Ejaj Ahmad ◽  
Qamar Zia ◽  
Mohd. Ahmar Rauf ◽  
Mohammad Owais ◽  
...  
Keyword(s):  
Protein Scaffolds ◽  
Recent Advances ◽  
Novel Protein

Practical application of 3-substituted-2,6-difluoropyridines in drug discovery: Facile synthesis of novel protein kinase C theta inhibitors

2017 ◽  
Vol 27 (11) ◽  
pp. 2497-2501 ◽  
Author(s):  
Taisuke Katoh ◽  
Yoshihide Tomata ◽  
Masaki Setoh ◽  
Satoshi Sasaki ◽  
Takafumi Takai ◽  
...  
Keyword(s):  
Protein Kinase C ◽  
Drug Discovery ◽  
Protein Kinase ◽  
Practical Application ◽  
Facile Synthesis ◽  
Kinase C ◽  
Novel Protein
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