Results 101 to 110 of about 16,142 (230)
Solid-phase synthesis of oxetane modified peptides [PDF]
, 2017 Solid-phase peptide synthesis (SPPS) is used to create peptidomimetics in which one of the backbone amide C=O bonds is replaced by a four-membered oxetane ring.
Beadle, Jonathan D. +5 more
core +2 more sources
Cancer pain: current practice and emerging targets
British Journal of Pharmacology, EarlyView.Cancer pain (CP) arises from a complex interplay between the tumour and its microenvironment. Many patients experience a mixed pain phenotype that encompasses nociceptive, neuropathic and neuroinflammatory mechanisms, and vary across tumour type and disease stage. Despite decades of intensive research, the mainstay of cancer pain treatment is still non‐
Yi Ye +5 more
wiley +1 more source
Synthesis of oxetane- and azetidine-containing spirocycles related to the 2,5-diketopiperazine framework [PDF]
, 2015 A simple two-step sequence is used to efficiently make novel spirocyclic analogues of the diketopiperazine nucleus. Conjugate addition of chiral α-amino esters to nitroalkenes, generated from oxetan-3-one or N-Boc-azetidin-3-one, followed by nitro group ...
Beadle, Jonathan D. +4 more
core +1 more source
British Journal of Pharmacology, EarlyView.Abstract Background and Purpose Kinases phosphorylate ion channels, but their noncatalytic roles via protein–protein interactions (PPI) are less understood. Here, we identified the peptidomimetic ZL141 to characterize the PPI between GSK3β and Nav1.6, revealing a noncatalytic role for GSK3β in regulating Nav1.6 currents and neuronal excitability ...
Aditya K. Singh +19 more
wiley +1 more source
Statine-based peptidomimetic compounds as inhibitors for SARS-CoV-2 main protease (SARS-CoV‑2 Mpro)
Scientific ReportsCOVID-19 is a multisystemic disease caused by the SARS-CoV-2 airborne virus, a member of the Coronaviridae family. It has a positive sense single-stranded RNA genome and encodes two non-structural proteins through viral cysteine-proteases processing ...
Pedro Henrique R. de A. Azevedo +18 more
doaj +1 more source
Bio-mimetic strategies to re-activate apoptotic cell death for cancer treatments [PDF]
Exploration of Drug ScienceApoptosis is a crucial process to maintain the correct balance between healthy cells and committed-to-death cells in every tissue. The internal (or mitochondrial) and external (or death receptor) pathways are responsible for driving a series of molecular
Andrea Venerando +2 more
doaj +1 more source
A new potential radiosensitizer: ammonium persulfate modified WCNTs [PDF]
, 2007 Radiotherapy plays a very important role in cancer treatment. Radiosensitizers have been widely used to enhance the radiosensitivity of cancer cells at given radiations.
Bo-Zhang Yu, Jian-She Yang, Wen-Xin Li
core +1 more source
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 +5 more
core +1 more source
Cancer Science, EarlyView.Graphical representation of formation of self‐assembled PEGylated Chitosan Nanoparticles and their mechanism in tumor localization. ABSTRACT Polymer‐based nanocarriers have emerged as transformative platforms in cancer nanomedicine, enabling controlled and site‐specific delivery of therapeutic agents.
Prashant Kesharwani +5 more
wiley +1 more source
Phenylalanine-derived β-lactam TRPM8 antagonists: revisiting configuration and new benzoyl derivatives [PDF]
Exploration of Drug ScienceAim: To expand the understanding of the structure-activity relationship within a family of amino acid-derived β-lactam TRPM8 (transient receptor potential melastatin channel, subtype 8) antagonists, this work investigated both the configuration ...
Cristina Martín-Escura +6 more
doaj +1 more source