Incidence of Cutaneous Adverse Events With Phosphoinositide 3-Kinase Inhibitors as Adjuvant Therapy in Patients With Cancer: A Systematic Review and Meta-analysis.
Sign Up to like & getrecommendations! Published in 2022 at "JAMA oncology"
DOI: 10.1001/jamaoncol.2022.4327
Abstract: Importance The phosphoinositide 3-kinase (PI3K) pathway is among the most frequently activated pathways in human cancers. As the use of PI3K inhibitors for cancer treatment grows, there is increasing need for understanding the cutaneous effects… read more here.
Keywords: incidence cutaneous; incidence; pi3k inhibitors; analysis ... See more keywords
PI3K Inhibitors in Breast Cancer Therapy
Sign Up to like & getrecommendations! Published in 2019 at "Current Oncology Reports"
DOI: 10.1007/s11912-019-0846-7
Abstract: The phosphatidylinositol 3-kinase (PI3K) pathway is the most common aberrantly activated pathway in breast cancer, making it an attractive therapeutic target. In this review, we will discuss the rationale for targeting PI3K/AKT signaling and the… read more here.
Keywords: cancer; inhibitors breast; pi3k inhibitors; breast cancer ... See more keywords
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111718
Abstract: Phosphatidylinositol-3 kinase (PI3K) pathway is one of the most frequently activated pathogenic signaling cascades in human malignancies. PI3K is genetically mutated or overexpressed in a wide variety of cancers including ovarian, breast, prostate, gastric, colorectal,… read more here.
Keywords: pi3k; kinase pi3k; selective pi3k; phosphatidylinositol kinase ... See more keywords
Development of PI3K inhibitors: advances in clinical trials and new strategies (Review).
Sign Up to like & getrecommendations! Published in 2021 at "Pharmacological research"
DOI: 10.1016/j.phrs.2021.105900
Abstract: Phosphatidylinositol 3-kinases (PI3Ks) are the family of vital lipid kinases widely distributed in mammalian cells. The overexpression of PI3Ks leads to hyperactivation of the PI3K/AKT/mTOR pathway, which is considered a pivotal pathway in the occurrence… read more here.
Keywords: pi3k; development pi3k; inhibitors advances; clinical trials ... See more keywords
Discovery of Potent and Selective PI3Kγ Inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01203
Abstract: The selective inhibition of the lipid signaling enzyme PI3Kγ constitutes an opportunity to mediate immunosuppression and inflammation within the tumor microenvironment but is difficult to achieve due to the high sequence homology across the class… read more here.
Keywords: pi3k; potent selective; discovery potent; selective pi3k ... See more keywords
Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01520
Abstract: PI3Kδ inhibitors have been developed for treatment of B-cell malignancies and inflammatory and autoimmune diseases. However, their therapeutic role in solid tumors like hepatocellular carcinoma (HCC) is rarely reported. Thus, the development of potent and… read more here.
Keywords: pi3k; hepatocellular carcinoma; pi3k inhibitors; selective pi3k ... See more keywords
Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a key off-target activity.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01585
Abstract: Optimisation of a lead series of PI3Kδ inhibitors based on a dihydroisobenzofuran core led to the identification of potent, orally bioavailable compound 19. Selectivity profiling of compound 19 showed similar potency for the class III… read more here.
Keywords: orally bioavailable; pi3k; optimization orally; compound ... See more keywords
Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.
Sign Up to like & getrecommendations! Published in 2017 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.7b00222
Abstract: The phosphoinositide 3-kinase (PI3K) inhibitors potently inhibit the signaling pathway of PI3K/AKT/mTOR, which provides a promising new approach for the molecularly targeted cancer therapy. In this work, a novel series of 7-azaindole scaffold derivatives was… read more here.
Keywords: series azaindole; novel series; azaindole scaffold; activity ... See more keywords
Emerging roles of class I PI3K inhibitors in modulating tumor microenvironment and immunity.
Sign Up to like & getrecommendations! Published in 2020 at "Acta pharmacologica Sinica"
DOI: 10.1038/s41401-020-00500-8
Abstract: Immune system-mediated tumor killing has revolutionized anti-tumor therapies, providing long-term and durable responses in some patients. The phosphoinositide 3-kinase (PI3K) pathway controls multiple biological processes and is frequently dysregulated in malignancies. Enormous efforts have been… read more here.
Keywords: microenvironment; pi3k; pi3k inhibitors; class pi3k ... See more keywords
Structural basis for tailor-made selective PI3K α/β inhibitors: a computational perspective
Sign Up to like & getrecommendations! Published in 2021 at "New Journal of Chemistry"
DOI: 10.1039/d0nj04216a
Abstract: PI3K α and β are Class IA PI3K isoforms that share a highly homologous ATP binding site, differing only in a few residues around the binding site. They are ubiquitously expressed in various organs and… read more here.
Keywords: structural basis; pi3k; selective pi3k; basis tailor ... See more keywords
PI3K inhibitors: review and new strategies
Sign Up to like & getrecommendations! Published in 2020 at "Chemical Science"
DOI: 10.1039/d0sc01676d
Abstract: The search is on for effective specific inhibitors for PI3Kα mutants. read more here.
Keywords: new strategies; review new; pi3k inhibitors; inhibitors review ... See more keywords