Results 271 to 280 of about 112,243 (300)

Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase γ

Journal of Medicinal Chemistry, 2015
A series of high affinity second-generation thiazolopiperidine inhibitors of PI3Kγ were designed based on some general observations around lipid kinase structure. Optimization of the alkylimidazole group led to inhibitors with higher levels of PI3Kγ selectivity.
Philip N, Collier, David, Messersmith, Arnaud, Le Tiran, Upul K, Bandarage, Christina, Boucher, Jon, Come, Kevin M, Cottrell, Veronique, Damagnez, John D, Doran, James P, Griffith, Suvarna, Khare-Pandit, Elaine B, Krueger, Mark W, Ledeboer, Brian, Ledford, Yusheng, Liao, Sudipta, Mahajan, Cameron S, Moody, Setu, Roday, Tiansheng, Wang, Jinwang, Xu, Alex M, Aronov   +20 more
openaire   +2 more sources

Phosphoinositide-3-kinase (PI3K) inhibitors: Identification of new scaffolds using virtual screening

Bioorganic & Medicinal Chemistry Letters, 2009
In the present work, we used virtual screening (VS) of the ZINC database of 2.5 million compounds to seek new PI3K inhibitory scaffolds. The VS flowchart implemented various filters, including a 3D-database screen, and extensive docking studies, to derive 89 derivatives that were experimentally assayed against the four PI3K isoforms.
Raphaël, Frédérick, Claire, Mawson, Jackie D, Kendall, Claire, Chaussade, Gordon W, Rewcastle, Peter R, Shepherd, William A, Denny   +6 more
openaire   +2 more sources

Rationalizing Predictions of Isoform-Selective Phosphoinositide 3-Kinase Inhibitors Using MolAnchor Analysis

Journal of Chemical Information and Modeling
Explaining the predictions of machine learning models is of critical importance for integrating predictive modeling in drug discovery projects. We have generated a test system for predicting isoform selectivity of phosphoinositide 3-kinase (PI3K) inhibitors and systematically analyzed correct predictions of selective inhibitors using a new methodology ...
Alec Lamens, Jürgen Bajorath
openaire   +2 more sources

The Design and Identification of Brain Penetrant Inhibitors of Phosphoinositide 3-Kinase α

Journal of Medicinal Chemistry, 2012
Inhibition of phosphoinositide 3-kinase (PI3K) signaling through PI3Kα has received significant attention for its potential in cancer therapy. While the PI3K pathway is a well-established and widely pursued target for the treatment of many cancer types due to the high frequency of abnormal PI3K signaling, glioblastoma multiforme (GBM) is particularly ...
Timothy P, Heffron, Laurent, Salphati, Bruno, Alicke, Jonathan, Cheong, Jennafer, Dotson, Kyle, Edgar, Richard, Goldsmith, Stephen E, Gould, Leslie B, Lee, John D, Lesnick, Cristina, Lewis, Chudi, Ndubaku, Jim, Nonomiya, Alan G, Olivero, Jodie, Pang, Emile G, Plise, Steve, Sideris, Sean, Trapp, Jeffrey, Wallin, Lan, Wang, Xiaolin, Zhang   +20 more
openaire   +2 more sources

Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability

Bioorganic & Medicinal Chemistry, 2015
Phosphoinositide 3-kinase (PI3K) is activated in various human cancer cells and well known as a cancer therapy target. We previously reported a dihydropyrrolopyrimidine derivative as a highly potent PI3K inhibitor that has strong tumor growth inhibition in a xenograft model.
Hatsuo, Kawada, Hirosato, Ebiike, Masao, Tsukazaki, Shun, Yamamoto, Kohei, Koyama, Mitsuaki, Nakamura, Kenji, Morikami, Kiyoshi, Yoshinari, Miyuki, Yoshida, Kotaro, Ogawa, Nobuo, Shinma, Takuo, Tsukuda, Jun, Ohwada   +12 more
openaire   +2 more sources

Preventive and Therapeutic Effects of Phosphoinositide 3-Kinase Inhibitors on Acute Lung Injury

Chest, 2011
Phosphoinositide 3-kinases (PI3Ks) are involved in a number of biologic responses. Recent preclinical studies demonstrated that the PI3K-dominant signal pathway could play an important role in the development of acute lung injury, although the mechanism remains unclear.CD-1 mice were administered different PI3K inhibitors either intranasally or ...
Chengshui, Chen, Xiaocong, Fang, Yaoli, Wang, Yuping, Li, Diane, Wang, Xia, Zhao, Chunxue, Bai, Xiangdong, Wang   +7 more
openaire   +2 more sources

Integrative oncology: Addressing the global challenges of cancer prevention and treatment

Ca-A Cancer Journal for Clinicians, 2022
Jun J Mao,, Msce, Lorenzo Cohen, Karen M Mustian   +2 more
exaly  

Small molecule inhibitors of phosphoinositide 3-kinase (PI3K) delta and gamma.

Current topics in medicinal chemistry, 2009
In recent years, pharmaceutical companies have increasingly focused on phosphoinositide 3-kinases delta (PI3Kdelta) and gamma (PI3Kgamma) as therapeutic targets for the treatment of inflammatory and autoimmune diseases. All class 1 PI3-kinases (alpha/beta/gamma/delta) generate phospholipid second messengers that help govern cellular processes such as ...
Michael K, Ameriks, Jennifer D, Venable
openaire   +1 more source

AEs of phosphoinositide 3 kinase Inhibitors in patients with lymphoma

Reactions Weekly, 2022
openaire   +1 more source

Obesity and adverse breast cancer risk and outcome: Mechanistic insights and strategies for intervention

Ca-A Cancer Journal for Clinicians, 2017
Cynthia Morata-Tarifa, Joyce M Slingerland   +1 more
exaly