Results 91 to 100 of about 12,487 (241)
Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries
British Journal of Pharmacology, EarlyView.Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley +1 more source
Immunomodulation by opioid peptidomimetic compound
, 2001 Objective: As a follow-up to our earlier studies on immunomodulation with opioid peptides, we synthesized and evaluated immunomodulatory activity of four peptidomimetic compounds, i.e. Tyr-NH-C(Me)2-CH2-O-Phe-NH2(1), Tyr-NH-C6H5-(o)-CH2-CH2-O-Phe-NH2 (2),
Dhar, Manojit M. +6 more
core +1 more source
, 2016 We have developed a novel protecting-group-free strategy for the synthesis of peptidomimetic conjugates. The high degrees of stereocontrol and chemoselectivity achieved in this chemistry hinge upon unusual preferences of the amphoteric amino aldehydes ...
Andrei K. Yudin (1470634) +1 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
, 2016 Conjugation of cytotoxic agents to targeting carriers (e.g. antibodies or small molecules) capable of selectively binding to tumor-specific antigens, is emerging as a successful strategy to overcome the drawbacks of traditional chemotherapy.[1] Being ...
D. Arosio +6 more
core
, 2018 The prevailing hypothesis stipulates that the preamyloid oligomers of Aβ are the main culprits associated with the onset and progression of Alzheimer’s disease (AD), which has prompted efforts to search for therapeutic agents with the ability to inhibit ...
Sunil Kumar (102321) +3 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
Synthesis and biological evaluation of RGD peptidomimetic-paclitaxel conjugates for tumor targeting
, 2016 Integrins are a large family of heterodimeric transmembrane glycoprotein receptors, composed by two non-covalently-associated subunits (α and β). Integrins αVβ3 and αVβ5 are overexpressed on blood vessels in human tumors but not on vessels in normal ...
D. Arosio +13 more
core
Computational design of novel peptidomimetic inhibitors of cadherin homophilic interactions [PDF]
, 2015 We report a first set of peptidomimetic ligands mimicking the adhesive interface identified by recent crystallographic structures of E- and N-cadherin.
Arosio, Daniela +27 more
core +1 more source
A guide to the types, structures, and multifaceted functions of matrix metalloproteinases in cancer
The FEBS Journal, EarlyView.Matrix metalloproteinases (MMPs) orchestrate cancer progression and metastasis through proteolytic and non‐proteolytic actions. By remodeling the tumor microenvironment, enhancing growth factor availability, and modulating cell behavior, MMPs promote proliferation, migration or invasion, and epithelial‐to‐mesenchymal transition. Alongside extracellular
Zoi Piperigkou +4 more
wiley +1 more source