Results 21 to 30 of about 19,199 (236)

Peptidomimetics and Their Applications for Opioid Peptide Drug Discovery

Biomolecules, 2022
Despite various advantages, opioid peptides have been limited in their therapeutic uses due to the main drawbacks in metabolic stability, blood-brain barrier permeability, and bioavailability.
Yeon Sun Lee
doaj   +1 more source

Binding Modes of Peptidomimetics Designed to Inhibit STAT3 [PDF]

, 2012
STAT3 is a transcription factor that has been found to be constitutively activated in a number of human cancers. Dimerization of STAT3 via its SH2 domain and the subsequent translocation of the dimer to the nucleus leads to transcription of anti ...
A Kamb, AC Anderson, AC Pierce, AN Jain, Ankur Dhanik, B Kuhn, B Raveh, BK Shoichet, C Hetényi, CN Cavasotto, CN Cavasotto, D Bhasin, D Plewczynski, D Plewczynski, DB Kitchen, DE Levy, DR Coleman, E Kellenberger, EF Pettersen, G Jones, G Schneider, GC Terstappen, GL Warren, GM Morris, GM Morris, HJC Berendsen, HM Berman, I Kuntz, I Massova, I Park, IG Khalil, IW Kuntz, J Darnell, J Schust, J Wang, JA DiMasi, JA Erickson, JA Hartigan, JB Cross, JC Owicki, Jie Zheng, JM Reichert, John S. McMurray, JP Rogers, JS Isaccs, JS McMurray, JW Shay, K Onodera, L Xing, Lydia E. Kavraki, M Karplus, M Mangoni, M Rarey, M Stahl, MM Moasser, MW Chang, MW Chang, N Li, N Okimoto, O Trott, P Weber, PA Kollman, PK Mandal, PK Mandal, PK Mandal, R Abagyan, R Buettner, R García-Nieto, R Wang, RA Friesner, RC Wade, S Becker, S Kaushik, S Morgan, SJ Projan, SK Panigrahi, T Bowman, T Darden, X Li, X Mao, X Xu, Y Cheng, Y Hua   +82 more
core   +7 more sources

Peptidomimetic inhibitors of N-myristoyltransferase from human malaria and leishmaniasis parasites [PDF]

, 2014
N-Myristoyltransferase (NMT) has been shown to be essential in Leishmania and subsequently validated as a drug target in Plasmodium. Herein, we discuss the use of antifungal NMT inhibitors as a basis for inhibitor development resulting in the first sub ...
Brannigan, JA, Leatherbarrow, RJ, Olaleye, TO, Roberts, SM, Tate, EW, Wilkinson, AJ   +5 more
core   +4 more sources

In vitro and in vivo screening for novel essential cell-envelope proteins in Pseudomonas aeruginosa [PDF]

, 2015
The Gram-negative bacterium Pseudomonas aeruginosa represents a prototype of multi-drug resistant opportunistic pathogens for which novel therapeutic options are urgently required.
Bragonzi, Alessandra, Fernandez Pinar, Regina, Imperi, Francesco, LO SCIUTO, Alessandra, Ranucci, Serena, Rossi, Alice   +5 more
core   +1 more source

Repurposing cancer drugs, batimastat and marimastat, to inhibit the activity of a group I metalloprotease from the venom of the Western Diamondback rattlesnake, Crotalus atrox [PDF]

, 2020
Snakebite envenomation causes over 140,000 deaths every year predominantly in developing countries. As a result, it is one of the most lethal neglected tropical diseases.
Bicknell, Andrew B., Lakshminarayanan, Karthik, Layfield, Harry J., Mehmi, Amita, Patel, Ketan, Ravishankar, Divyashree, Salim, Anika, Sonavane, Medha, Trim, Steven A., Vaiyapuri, Rajendran, Vaiyapuri, Sakthivel, Vallance, Thomas M., Williams, Harry F.   +12 more
core   +1 more source

Targeting STAT3 in Cancer with Nucleotide Therapeutics. [PDF]

, 2019
Signal transducer and activator of transcription 3 (STAT3) plays a critical role in promoting the proliferation and survival of tumor cells. As a ubiquitously-expressed transcription factor, STAT3 has commonly been considered an "undruggable" target for ...
Grandis, Jennifer R, Johnson, Daniel E, Lau, Yue-Ting K, Ramaiyer, Malini   +3 more
core   +2 more sources

Repurposing Azithromycin and Rifampicin Against Gram-Negative Pathogens by Combination With Peptidomimetics

Frontiers in Cellular and Infection Microbiology, 2019
Synthetic peptidomimetics may be designed to mimic functions of antimicrobial peptides, including potentiation of antibiotics, yet possessing improved pharmacological properties.
Kristin R. Baker, Kristin R. Baker, Bimal Jana, Bimal Jana, Anna Mette Hansen, Hanne Mørck Nielsen, Henrik Franzyk, Luca Guardabassi, Luca Guardabassi   +8 more
doaj   +1 more source

Cationic Peptidomimetic Amphiphiles Having a N-Aryl- or N-Naphthyl-1,2,3-Triazole Core Structure Targeting Clostridioides (Clostridium) difficile: Synthesis, Antibacterial Evaluation, and an In Vivo C. difficile Infection Model

Antibiotics, 2021
Clostridioides (also known as Clostridium) difficile is a Gram-positive anaerobic, spore producing bacterial pathogen that causes severe gastrointestinal infection in humans.
Muni Kumar Mahadari, Sreenu Jennepalli, Andrew J. Tague, Papanin Putsathit, Melanie L. Hutton, Katherine A. Hammer, Daniel R. Knight, Thomas V. Riley, Dena Lyras, Paul A. Keller, Stephen G. Pyne   +10 more
doaj   +1 more source

Designing Peptidomimetics [PDF]

Current Topics in Medicinal Chemistry, 2018
The concept of a peptidomimetic was coined about forty years ago. Since then, enormous effort and interest have been devoted to mimic the properties of peptides with small molecules or pseudopeptides. The present report aims to review different approaches described in the past to succeed in this goal.
openaire   +4 more sources

Quinazolinone-Peptido-Nitrophenyl-Derivatives as Potential Inhibitors of SARS-CoV-2 Main Protease

Viruses, 2023
The severe acute respiratory syndrome coronavirus 2 main protease (SARS-CoV-2-Mpro) plays an essential role in viral replication, transcription, maturation, and entry into host cells.
Huynh-Nguyet-Huong Giang, Feng-Pai Chou, Ching-Yun Chen, Shen-Chieh Chou, Sheng-Cih Huang, Tuoh Wu, Bui-Thi-Buu Hue, Hong-Cheu Lin, Tung-Kung Wu   +8 more
doaj   +1 more source