Several isoquinoline-based templates were identified from the studies of the conformational effects of the diketopiperazine structures for PAI-1 inhibition. Moderate to good activity was retained with the elimination of unattractive characteristics in the diketopiperazine template.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0960-894x(02)00389-x | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
NXP800 activates the unfolded protein response, altering AR and E2F function to impact castration-resistant prostate cancer growth.
Clin Cancer Res
January 2025
Institute of Cancer Research, Sutton, Surrey, United Kingdom.
Purpose: Advanced prostate cancer (PCa) is invariably fatal with the androgen receptor (AR) being a major therapeutic target. AR signaling inhibitors have improved overall survival for men with advanced PCa, but treatment resistance is inevitable and includes reactivation of AR signaling. Novel therapeutic approaches targeting these mechanisms to block tumor growth is an urgent unmet clinical need.
View Article and Find Full Text PDFGenome-Wide A → G and C → T Mutations Induced by Functional TadA Variants in .
ACS Synth Biol
January 2025
Laboratory of Synthetic Microbiology, School of Chemical Engineering & Technology, Tianjin University, Tianjin 300072, P. R. China.
The fusion expression of deoxyribonucleic acid (DNA) replication-related proteins with nucleotide deaminase enzymes promotes random mutations in bacterial genomes, thereby increasing genetic diversity among the population. Most previous studies have focused on cytosine deaminase, which produces only C → T mutations, significantly limiting the variety of mutation types. In this study, we developed a fusion expression system by combining DnaG (RNA primase) with adenine deaminase TadA-8e (DnaG-TadA) in , which is capable of rapidly introducing A → G mutations into the genome, resulting in a 664-fold increase in terms of mutation rate.
View Article and Find Full Text PDFInclisiran, Reasons for a Novel Agent in a Crowded Therapeutic Field.
Curr Atheroscler Rep
January 2025
Unitat de Medicina Vascular I Metabolismo, Hospital Universitario Sant Joan, Universitat Rovira I Virgili, IISPV, CIBERDEM, Reus, Spain.
Purpose Of The Review: A significant number of patients fail to achieve target LDL cholesterol (LDL-C) levels. This review aims to explore why inclisiran, a novel class of LLT, should be considered a valuable addition to the current treatment options.
Recent Findings: Inclisiran is a small interfering RNA (siRNA) that targets PCSK9 synthesis specifically in the hepatocytes.
Integrating machine learning and structural dynamics to explore B-cell lymphoma-2 inhibitors for chronic lymphocytic leukemia therapy.
Mol Divers
January 2025
Department of Biotechnology, Deen Dayal, Upadhyay Gorakhpur University, Gorakhpur, India.
Chronic lymphocytic leukemia (CLL) is a malignancy caused by the overexpression of the anti-apoptotic protein B-cell lymphoma-2 (BCL-2), making it a critical therapeutic target. This study integrates computational screening, molecular docking, and molecular dynamics to identify and validate novel BCL-2 inhibitors from the ChEMBL database. Starting with 836 BCL-2 inhibitors, we performed ADME and Lipinski's Rule of Five (RO5) filtering, clustering, maximum common substructure (MCS) analysis, and machine learning models (Random Forest, SVM, and ANN), yielding a refined set of 124 compounds.
View Article and Find Full Text PDFNovel anti-HER2 ADCs vs dual anti-HER2 antibody for HER2-positive metastatic breast cancer failed to tyrosine kinase inhibitor.
Oncologist
December 2024
Department of Breast Oncology, The Fifth Medical Center of Chinese PLA General Hospital, Beijing 100071, People's Republic of China.
Background: Both novel anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugates (ADCs) and pertuzumab and trastuzumab (HP) combined with chemotherapy(C) regimens are the choice of treatment for HER2 positive metastatic breast cancer (MBC) after tyrosine kinase inhibitors (TKIs). Our team's previous research has shown significant therapeutic effects of novel anti-HER2 ADCs in patients with TKIs treatment failure. Unfortunately, there is currently no data available to compare novel anti-HER2 ADCs with HP combined with chemotherapy regimens.
View Article and Find Full Text PDFWant 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!