![conference banner](/images/conference-banner.jpeg)
Abstract
The PI3K signaling cascade is the key moderator of cell proliferation, survival, motility, and apoptosis. Class I PI3K proteins are well characterized and linked to thrombosis (PI3Kβ), rheumatoid arthritis (PI3Kδ), and cancer (PI3Kα). In this review, we explore the latest progress in the design and development of selective Class I PI3K inhibitors from the perspective of drug design and structure activity relationships.
Keywords: Class I PI3Ks, p100α, Anticancer, Drug design, Mutation, LY294002, GDC-0941, NVP-BEZ235, PI3Kγ, KRAS, BRAF, EGFR, MEK, PI3K/AKT, GSK2118436, Selectivity, and mTOR.
Current Topics in Medicinal Chemistry
Title:Advances in the Development of Class I Phosphoinositide 3-Kinase (PI3K) Inhibitors
Volume: 16 Issue: 13
Author(s): Dima A. Sabbah, Jian Hu and Haizhen A. Zhong
Affiliation:
Keywords: Class I PI3Ks, p100α, Anticancer, Drug design, Mutation, LY294002, GDC-0941, NVP-BEZ235, PI3Kγ, KRAS, BRAF, EGFR, MEK, PI3K/AKT, GSK2118436, Selectivity, and mTOR.
Abstract: The PI3K signaling cascade is the key moderator of cell proliferation, survival, motility, and apoptosis. Class I PI3K proteins are well characterized and linked to thrombosis (PI3Kβ), rheumatoid arthritis (PI3Kδ), and cancer (PI3Kα). In this review, we explore the latest progress in the design and development of selective Class I PI3K inhibitors from the perspective of drug design and structure activity relationships.
Export Options
About this article
Cite this article as:
Sabbah A. Dima, Hu Jian and Zhong A. Haizhen, Advances in the Development of Class I Phosphoinositide 3-Kinase (PI3K) Inhibitors , Current Topics in Medicinal Chemistry 2016; 16 (13) . https://dx.doi.org/10.2174/1568026615666150915115823
DOI https://dx.doi.org/10.2174/1568026615666150915115823 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Adaptogens—History and Future Perspectives
Adaptogens are pharmacologically active compounds or plant extracts that are associated with the ability to enhance the body’s stability against stress. The intake of adaptogens is associated not only with a better ability to adapt to stress and maintain or normalise metabolic functions but also with better mental and physical ...read more
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
![Wayfinder Image](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Transcriptional Regulation by Promoter Targeted RNAs
Current Topics in Medicinal Chemistry Virus, Oncolytic Virus and Human Prostate Cancer
Current Cancer Drug Targets Applications of Aptamers in Targeted Imaging: State of the Art
Current Topics in Medicinal Chemistry Sphere Formation Assay is not an Effective Method for Cancer Stem Cell Derivation and Characterization from the Caco-2 Colorectal Cell Line
Current Stem Cell Research & Therapy Mammalian Antimicrobial Peptides: Promising Therapeutic Targets Against Infection and Chronic Inflammation
Current Topics in Medicinal Chemistry Cry1A Proteins are Cytotoxic to HeLa but not to SiHa Cervical Cancer Cells
Current Pharmaceutical Biotechnology HPV Cervical Infection and Immunodysregulation: Synergistic Risks for Neoplasia-Review
Current Women`s Health Reviews Neural Plasticity After Spinal Cord Injury
Current Pharmaceutical Design Signal Transducer and Activator of Transcription Protein 3 (STAT3): An Update on its Direct Inhibitors as Promising Anticancer Agents
Current Medicinal Chemistry The Protective Effects of Silymarin on the Reproductive Toxicity: A Comprehensive Review
Current Medicinal Chemistry Patent Selections:
Current Biomarkers (Discontinued) Research Progress in Tumor Diagnosis Based on Raman Spectroscopy
Current Medical Imaging Intravoxel Incoherent Motion Diffusion-weighted Magnetic Resonance Imaging combined with Texture Analysis in Predicting the Histological Grades of Rectal Adenocarcinoma
Current Medical Imaging Exploiting Cancer Metal Metabolism using Anti-Cancer Metal- Binding Agents
Current Medicinal Chemistry The Origin and Identification of Mesenchymal Stem Cells in Teeth: from Odontogenic to Non-odontogenic
Current Stem Cell Research & Therapy Involvement of Cannabinoids in Cellular Proliferation
Mini-Reviews in Medicinal Chemistry Lymphatic Drainage in Patients with Primary Cutaneous Melanoma - the Role of Lymphoscintigraphy in Sentinel Lymph Node Biopsy
Current Medical Imaging Carbonic Anhydrase Inhibitors and the Management of Cancer
Current Topics in Medicinal Chemistry Recent Advance in the Research of Flavonoids as Anticancer Agents
Mini-Reviews in Medicinal Chemistry Arginyl Aminopeptidase-Like 1 (RNPEPL1) Is an Alternatively Processed Aminopeptidase with Specificity for Methionine, Glutamine, and Citrulline Residues
Protein & Peptide Letters