Results 141 to 150 of about 346,955 (321)

Advances in Diclofenac Derivatives: Exploring Carborane‐Substituted N‐Methyl and Nitrile Analogs for Anticancer Therapy

open access: yesChemMedChem, EarlyView.
By N‐methylation, the intramolecular lactam formation in carborane‐substituted diclofenac analogs is prevented, yielding a series of open‐chain derivatives alongside with their phenyl analogs exhibiting anticancer activity and thus offering a promising avenue for future drug development. This study explores the anticancer potential of N‐methylated open‐
Christoph Selg   +12 more
wiley   +1 more source

Visual quantification of prostaglandin E2 discharge from a single cell. [PDF]

open access: yesCell Struct Funct, 2023
Watabe T   +3 more
europepmc   +1 more source

Carborane‐based Analogues of Celecoxib and Flurbiprofen, their COX Inhibition Potential and COX Selectivity Index

open access: yesChemMedChem, Accepted Article.
The cylcooxygenase isoforms COX‐1 and COX‐2 are involved in the production of prostaglandins in physiological and pathological processes. The overexpression of COX‐2 under inflammatory conditions as well as its role in cancer and neurodegenerative diseases necessitates the need to develop and improve non‐steroidal anti‐inflammatory drugs.
Lea Ueberham   +8 more
wiley   +1 more source

KEAP1‐NRF2 protein–protein interaction inhibitors: Design, pharmacological properties and therapeutic potential

open access: yesMedicinal Research Reviews, Volume 43, Issue 1, Page 237-287, January 2023., 2023
Abstract The transcription factor nuclear factor erythroid 2‐related factor 2 (NRF2) is considered the master regulator of the phase II antioxidant response. It controls a plethora of cytoprotective genes related to oxidative stress, inflammation, and protein homeostasis, among other processes.
Enrique Crisman   +6 more
wiley   +1 more source

Extensive Molecular Dynamics Simulations Disclosed the Stability of mPGES‐1 Enzyme and the Structural Role of Glutathione (GSH) Cofactor

open access: yesMolecular Informatics, Volume 41, Issue 12, December 2022., 2022
Abstract A deep in silico investigation of various microsomal prostaglandin E2 synthase‐1 (mPGES‐1) protein systems is here reported using molecular dynamics (MD) simulations. Firstly, eight different proteins models (Models A−H) were built, starting from the active enzyme trimer system (Model A), namely that bound to three glutathione (GSH) cofactor ...
Simone Di Micco   +2 more
wiley   +1 more source

THE EFFECTS OF PROSTAGLANDIN E1, BRADYKININ AND HISTAMINE ON CANINE SYNOVIAL VASCULAR PERMEABILITY [PDF]

open access: bronze, 1977
D M Grennan   +3 more
openalex   +1 more source

A Phase 1C, Open Label, Single Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of DM199 Administered Intravenously with a Polyvinyl Chloride Bag in Adult Healthy Subjects and Adults Recently Taking Angiotensin‐Converting Enzyme Inhibitors

open access: yesClinical Pharmacology in Drug Development, EarlyView.
Abstract This small phase 1C, open‐label, single ascending dose study evaluated the safety, tolerability, and pharmacokinetics (PKs) of DM199, a recombinant form of human tissue kallikrein‐1 (KLK1). A small sample size of both healthy subjects and hypertensive adults recently taking angiotensin‐converting enzyme inhibitors was studied. KLK1 has a known
Michael Giuffre   +3 more
wiley   +1 more source

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