Identification of highly potent and selective PI3Kδ inhibitors.

Bioorg Med Chem Lett

Research & Development, Bristol-Myers Squibb Company, Route 206 & Province Line Road, Princeton, NJ 08543, United States.

Published: July 2017

Selective PI3Kδ inhibitors have recently been hypothesized to be appropriate immunosuppressive agents for the treatment of immunological disorders such as rheumatoid arthritis. However, few reports have highlighted molecules that are highly selective for PI3Kδ over the other PI3K isoforms. In this letter, isoform and kinome selective PI3Kδ inhibitors are presented. The Structural Activity Relationship leading to such molecules is outlined.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2017.01.077DOI Listing

Publication Analysis

Top Keywords

selective pi3kδ
16
pi3kδ inhibitors
12
identification highly
4
highly potent
4
selective
4
potent selective
4
pi3kδ
4
inhibitors selective
4
inhibitors hypothesized
4
hypothesized appropriate
4

Similar Publications

The association between multilingual experience factors and cognitive functioning in older adults: A Lifelines study.

J Gerontol B Psychol Sci Soc Sci

January 2025

Linguistics and English as a Second Language, Faculty of Arts, University of Groningen, Groningen, the Netherlands.

Objectives: The complex life experience of speaking two or more languages has been suggested to preserve cognition in older adulthood. This study aimed to investigate this further by examining the relationship between multilingual experience variables and cognitive functioning in a large cohort of older adults in the diversely multilingual north of the Netherlands.

Method: 11,332 older individuals participating in the Lifelines Cohort Study completed a language experience questionnaire.

View Article and Find Full Text PDF

Objective: Segmentation of individual thigh muscles in MRI images is essential for monitoring neuromuscular diseases and quantifying relevant biomarkers such as fat fraction (FF). Deep learning approaches such as U-Net have demonstrated effectiveness in this field. However, the impact of reducing neural network complexity remains unexplored in the FF quantification in individual muscles.

View Article and Find Full Text PDF

Recent studies have suggested that the interaction between diet and an individual's genetic predisposition can determine the likelihood of obesity and various metabolic disorders. The current study aimed to examine the association of dietary branched-chain amino acids(BCAAs) and aromatic amino acids(AAAs) with the expression of the leptin and FTO genes in the visceral and subcutaneous adipose tissues of individuals undergoing surgery. This cross-sectional study was conducted on 136 Iranian adults, both men and women, aged ≥18 years.

View Article and Find Full Text PDF

This systematic review and meta-analysis aimed to assess the accuracy and success rate of ultrasound in determining fetal sex. A search was conducted on Medline, Cochrane Library, and EMBASE databases, and the reference lists of selected studies were also reviewed. Meta-analyses were performed using Revman 5.

View Article and Find Full Text PDF

Purpose: Locally advanced colorectal tumors frequently invade adjacent organs, particularly the urinary bladder in the sigmoid colon and upper rectum, complicating multivisceral resections. This study compared postoperative outcomes of partial cystectomy (PC) and total cystectomy (TC) in patients with locally advanced colorectal cancer.

Methods: A systematic review was conducted in PubMed, Scopus, Central Register of Clinical Trials, and Web of Science for studies published up to November 2024.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!