Results 61 to 70 of about 17,763 (235)

Peptidomimetics in cancer targeting

Molecular Medicine, 2022
AbstractThe low efficiency of treatment strategies is one of the main obstacles to developing cancer inhibitors. Up to now, various classes of therapeutics have been developed to inhibit cancer progression. Peptides due to their small size and easy production compared to proteins are highly regarded in designing cancer vaccines and oncogenic pathway ...
Mohammad Mahmoudi Gomari, Shadi Abkhiz, Taha Ghantab Pour, Ehsan Lotfi, Neda Rostami, Fatemeh Nafe Monfared, Babak Ghobari, Mona Mosavi, Behruz Alipour, Nikolay V. Dokholyan   +9 more
openaire   +3 more sources

Targeting Lipopolysaccharide Transport Induces Membrane Lipid Remodeling and Sensitizes Acinetobacter baumannii to Colistin Treatment

Advanced Science, EarlyView.
This study identifies C4 as a lead inhibitor of the Lpt system. Notably, C4 potentiates colistin activity by disrupting LPS transport and remodeling phospholipid homeostasis, revealing a functional interplay between the Lpt and Mla systems. These findings establish a mechanistic link between Lpt inhibition and membrane lipid remodeling, positioning Lpt–
Jianya Luo, Hetianzi Zhang, Jinju Cai, Shuang Zhou, Haijie Zhang, Zhiqiang Wang, Yuan Liu   +6 more
wiley   +1 more source

Targeted Degradation of Picornaviral 3C Protease via PROTACs Confers High Barrier to Viral Resistance and Broad‐Spectrum Antiviral Activity

Advanced Science, EarlyView.
This study reports D34 as the first PROTAC degrader that targets the 3C protease of picornaviruses. D34 effectively degrades EV71 3C protease via the ubiquitin‐proteasome pathway. More importantly, D34 exhibits a high resistance barrier and shows broad‐spectrum antiviral activity against multiple picornaviruses, highlighting its potential as a novel ...
Weilong Deng, Junyu Chen, Yingyue Pang, Yuanyuan Zhang, Siqian Chen, Guoliang You, Xiaoman Tian, Zhongxin Xu, Jing Wang, Luqing Shang   +9 more
wiley   +1 more source

TRIM28‐Derived Peptide Exerts Anti‐Tumor Roles by Stabilizing Tumor Suppressive BRD7 Protein in Multiple Cancers

Advanced Science, EarlyView.
An α‐helical peptide, TAB12, designed to mimic the TRIM28 binding interface, competitively disrupts the TRIM28‐BRD7 interaction, thereby blocking ubiquitin‐mediated degradation of the tumor suppressor BRD7. This stabilization unleashes potent anti‐tumor effects across multiple tumor types with a favorable safety profile, offering a feasible strategy ...
Qingqing Wei, Changning Xue, Mengna Li, Jianxia Wei, Lemei Zheng, Shipeng Chen, Yijie Wang, Yumei Duan, Yanwei Luo, Wei Xiong, Ming Zhou   +10 more
wiley   +1 more source

Adding diverse noncanonical backbones to rosetta: enabling peptidomimetic design. [PDF]

PLoS ONE, 2013
Peptidomimetics are classes of molecules that mimic structural and functional attributes of polypeptides. Peptidomimetic oligomers can frequently be synthesized using efficient solid phase synthesis procedures similar to peptide synthesis ...
Kevin Drew, P Douglas Renfrew, Timothy W Craven, Glenn L Butterfoss, Fang-Chieh Chou, Sergey Lyskov, Brooke N Bullock, Andrew Watkins, Jason W Labonte, Michael Pacella, Krishna Praneeth Kilambi, Andrew Leaver-Fay, Brian Kuhlman, Jeffrey J Gray, Philip Bradley, Kent Kirshenbaum, Paramjit S Arora, Rhiju Das, Richard Bonneau   +18 more
doaj   +1 more source

Identification of highly selective type II kinase inhibitors with chiral peptidomimetic tails

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Identification of highly selective type II kinase inhibitors is described. Two different chiral peptidomimetic scaffolds were introduced on the tail region of non-selective type II kinase inhibitor GNF-7 to enhance the selectivity.
Seo-Jung Han, Jae Eun Jung, Do Hee Oh, Minsup Kim, Jae-Min Kim, Kyung-Sook Chung, Hee-Soo Han, Jeong-Hun Lee, Kyung-Tae Lee, Hee Jin Jeong, In Ho Park, Eunkyeong Jeon, Jeon-Soo Shin, Dongkeun Hwang, Art E. Cho, Duck-Hyung Lee, Taebo Sim   +16 more
doaj   +1 more source

Peptides and Peptidomimetics as Immunomodulators [PDF]

Immunotherapy, 2014
Peptides and peptidomimetics can function as immunomodulating agents by either blocking the immune response or stimulating the immune response to generate tolerance. Knowledge of B- or T-cell epitopes along with conformational constraints is important in the design of peptide-based immunomodulating agents. Work on the conformational aspects of peptides,
Ameya S, Gokhale, Seetharama, Satyanarayanajois   +1 more
openaire   +2 more sources

Antiviral Activity of Anthranilamide Peptidomimetics against Herpes Simplex Virus 1 and a Coronavirus

Antibiotics, 2023
The development of potent antiviral agents is of utmost importance to combat the global burden of viral infections. Traditional antiviral drug development involves targeting specific viral proteins, which may lead to the emergence of resistant strains ...
Umme Laila Urmi, Samuel Attard, Ajay Kumar Vijay, Mark D. P. Willcox, Naresh Kumar, Salequl Islam, Rajesh Kuppusamy   +6 more
doaj   +1 more source

A cyclic carbo-isosteric penta-depsipeptide: cyclo(Phe1–d-Ala2–Gly3–Phe4–APO5)

Acta Crystallographica Section E: Crystallographic Communications, 2015
The title compound, cyclo(Phe1–d-Ala2–Gly3–Phe4–APO5), C26H32N4O5, is the minor diastereoisomer of a cyclic penta-peptidomimetic analogue containing a novel 2-aminopropyl lactone (APO) motif, which displays the same number of atoms as the native amino ...
Stéphanie M. Guéret, Trixie Wagner
doaj   +1 more source

Peptidomimetic therapeutics: scientific approaches and opportunities

Drug Discovery Today, 2016
Natural endogenously occurring peptides exhibit desirable medicinal properties, but are often limited in application by rapid proteolysis and inadequate membrane permeability.
Nir Qvit, Samuel J. S. Rubin, Travis J. Urban, D. Mochly‐Rosen, E. Gross   +4 more
semanticscholar   +1 more source