Results 11 to 20 of about 26,717 (273)

A peptidomimetic modulator of the CaV2.2 N-type calcium channel for chronic pain

Proceedings of the National Academy of Sciences of the United States of America, 2023
Significance Transmembrane Cav2.2 voltage-gated calcium channels play a central role in pain through providing the Ca2+ for sustained neuronal firing and neurotransmitter release.
Kimberly Gomez, Ulises Santiago, Tyler S. Nelson, Heather N. Allen, Aida Calderon-Rivera, S. Hestehave, Erick J. Rodríguez Palma, Yuan Zhou, Paz Duran, Santiago Loya-López, Elaine Zhu, Upasana Kumar, Rory Shields, E. Koseli, Bryan D McKiver, Denise Giuvelis, Wanhong Zuo, Kufreobong E. Inyang, Angie Dorame, Aude Chefdeville, Dongzhi Ran, S. Perez-Miller, Yi Lu, Xia Liu, Handoko, P. Arora, M. Patek, Aubin Moutal, M. Khanna, Huijuan Hu, G. Laumet, Tamara D. King, Jing Wang, M. Damaj, Olga A. Korczeniewska, C. Camacho, R. Khanna   +36 more
semanticscholar   +1 more source

Investigation of the Compatibility between Warheads and Peptidomimetic Sequences of Protease Inhibitors—A Comprehensive Reactivity and Selectivity Study

International Journal of Molecular Sciences, 2023
Covalent peptidomimetic protease inhibitors have gained a lot of attention in drug development in recent years. They are designed to covalently bind the catalytically active amino acids through electrophilic groups called warheads.
P. Müller, Mergim Meta, J. L. Meidner, M. Schwickert, Jessica Meyr, K. Schwickert, C. Kersten, Collin Zimmer, S. Hammerschmidt, Ariane Frey, Albin Lahu, Sergio de la Hoz-Rodríguez, Laura Agost-Beltrán, S. Rodríguez, Kira Diemer, Wilhelm Neumann, F. González, B. Engels, T. Schirmeister   +18 more
semanticscholar   +1 more source

Design, Synthesis, and Biological Evaluation of Peptidomimetic Aldehydes as Broad-Spectrum Inhibitors against Enterovirus and SARS-CoV-2

Journal of Medicinal Chemistry, 2021
A novel series of peptidomimetic aldehydes was designed and synthesized to target 3C protease (3Cpro) of enterovirus 71 (EV71). Most of the compounds exhibited high antiviral activity, and among them, compound 18p demonstrated potent enzyme inhibitory ...
Wenhao Dai, D. Jochmans, Hang Xie, Hang Yang, Jian Li, H. Su, Di Chang, Jiang Wang, Jingjing Peng, Lili Zhu, Yong Nian, R. Hilgenfeld, Hualiang Jiang, Kaixian Chen, Lei-ke Zhang, Yechun Xu, J. Neyts, Hong Liu   +17 more
semanticscholar   +1 more source

Human defensin-inspired discovery of peptidomimetic antibiotics

Proceedings of the National Academy of Sciences of the United States of America, 2022
Significance We report the development of peptidomimetic antibiotics derived from a natural antimicrobial peptide, human α-defensin 5. By engaging multiple bacterial targets, the lead compound is efficacious in vitro and in vivo against bacteria with ...
Gan Luo, Jue Zhang, Hanbin Wang, Yaqi Sun, B. Cheng, Zhipeng Xu, Yan Zhang, Hui Li, Wuyuan Lu, E. Nemeth, T. Ganz, X. Fang   +11 more
semanticscholar   +1 more source

Peptidomimetic inhibitors of TMPRSS2 block SARS-CoV-2 infection in cell culture

Communications Biology, 2022
The transmembrane serine protease 2 (TMPRSS2) primes the SARS-CoV-2 Spike (S) protein for host cell entry and represents a promising target for COVID-19 therapy.
Lukas Wettstein, P. Knaff, C. Kersten, P. Müller, Tatjana Weil, Carina Conzelmann, Janis A. Müller, Maximilian Brückner, M. Hoffmann, S. Pöhlmann, T. Schirmeister, K. Landfester, J. Münch, V. Mailänder   +13 more
semanticscholar   +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

Allosteric Modulator Leads Hiding in Plain Site: Developing Peptide and Peptidomimetics as GPCR Allosteric Modulators

Frontiers in Chemistry, 2021
Allosteric modulators (AMs) of G-protein coupled receptors (GPCRs) are desirable drug targets because they can produce fewer on-target side effects, improved selectivity, and better biological specificity (e.g., biased signaling or probe dependence) than
Keith M. Olson, John R. Traynor, John R. Traynor, Andrew Alt, Andrew Alt   +4 more
doaj   +1 more source

Antibiotic Potentiation in Multidrug-Resistant Gram-Negative Pathogenic Bacteria by a Synthetic Peptidomimetic.

ACS Infectious Diseases, 2021
The peptidomimetic H-[NLys-tBuAla]6-NH2 (CEP-136), which exhibits low inherent antimicrobial activity against Gram-negative bacteria (MIC = 16-64 μM), was shown to significantly potentiate the antibacterial activity of several clinically important ...
Elnaz Harifi Mood, Lise Goltermann, Camilla Brolin, L. Cavaco, A. J. Nejad, Niloofar Yavari, Nicki Frederiksen, H. Franzyk, P. Nielsen   +8 more
semanticscholar   +1 more source

Improvement on Permeability of Cyclic Peptide/Peptidomimetic: Backbone N-Methylation as A Useful Tool

Marine Drugs, 2021
Peptides have a three-dimensional configuration that can adopt particular conformations for binding to proteins, which are well suited to interact with larger contact surface areas on target proteins.
Yang Li, Wang Li, Zhengshuang Xu
semanticscholar   +1 more source

Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors.

RSC Medicinal Chemistry, 2021
Tragically, the death toll from the COVID-19 pandemic continues to rise, and with variants being observed around the globe new therapeutics, particularly direct-acting antivirals that are easily administered, are desperately needed. Studies targeting the
Bing Bai, E. Arutyunova, Muhammad Bashir Khan, Jimmy Lu, Michael A. Joyce, H. Saffran, Justin A Shields, Appan Srinivas Kandadai, Alexandr Belovodskiy, Mostofa A Hena, Wayne Vuong, Tess Lamer, H. Young, J. Vederas, D. Tyrrell, M. J. Lemieux, J. Nieman   +16 more
semanticscholar   +1 more source