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PI3K

NVP-BKM120 inhibits colon cancer growth via FoxO3a-dependent PUMA induction

13 views | Oct 12 2019

Yang S et al. demonstrated a key role of PUMA in mediating the anticancer effects of NVP-BKM120 and suggest that PUMA could be used as an indicator of NVP-BKM120 sensitivity, and also have important implications for it clinical applications. [Read the Full Post]

Phase II study of copanlisib, a PI3K inhibitor, in relapsed or refractory, indolent or aggressive lymphoma

14 views | Sep 21 2019

Dreyling M et al. demonstrated promising efficacy and manageable toxicity in heavily pretreated patients with various subtypes of indolent and aggressive malignant lymphoma. Subtype-specific studies of copanlisib in patients with follicular, peripheral T-cell, and mantle cell lymphomas are ongoing. [Read the Full Post]

Copanlisib: An Intravenous Phosphatidylinositol 3-Kinase (PI3K) Inhibitor for the Treatment of Relapsed Follicular Lymphoma

0 views | Sep 19 2019

Eltantawy A et al. provided an alternative option for patients with relapsed FL. It is safe and effective and has an acceptable toxicity profile. [Read the Full Post]

Copanlisib: First Global Approval

0 views | Sep 18 2019

Markham A summarizes the milestones in the development of copanlisib leading to this first approval for relapsed follicular lymphoma. [Read the Full Post]

GS-1101: a delta-specific PI3K inhibitor in chronic lymphocytic leukemia

13 views | Sep 16 2019

Macias-Perez IM et al. indicated this article will review new insights into the pathophysiology of CLL, the preclinical rationale of a PI3Kδ inhibitor in CLL, and the clinical evidence supporting this first-in-class therapeutic target for CLL patients. [Read the Full Post]

The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia

13 views | Sep 16 2019

Hoellenriegel J et al. provided an explanation for the clinical activity of CAL-101, and a roadmap for future therapeutic development. [Read the Full Post]

Synthesis and screening of 3-MA derivatives for autophagy inhibitors

21 views | Sep 11 2019

Wu Y et al. demonstrated that chemical modification of an existing autophagy inhibitor is an effective method to generate improved autophagy inhibitors. [Read the Full Post]

Autophagy inhibitor 3-methyladenine protects against endothelial cell barrier dysfunction in acute lung injury

16 views | Sep 11 2019

Slavin SA et al. indicated these data imply a role of autophagy in lung vascular injury and reveal the protective and therapeutic utility of 3-MA against ALI. [Read the Full Post]

BYL719, a new α-specific PI3K inhibitor: single administration and in combination with conventional chemotherapy for the treatment of osteosarcoma

67 views | Sep 07 2019

Gobin B et al. indicated the present work shows that BYL719 is a promising drug in either a single or multidrug approach to curing bone sarcoma. [Read the Full Post]

Doxorubicin as a fluorescent reporter identifies novel MRP1 (ABCC1) inhibitors missed by calcein-based high content screening of anticancer agents

35 views | Aug 13 2019

Sampson A et al. indicated mifepristone and doramapimod as pan inhibitors of these three drug transporters while celecoxib exhibited selective MRP1 inhibition. Together, our findings signify the importance of MRP1 in drug discovery and demonstrate the effectiveness and value of doxorubicin-based high content screening approach. Anti-cancer agents that exhibit MRP1 inhibition may be used to reverse multidrug resistance or to improve the efficacy and reduce the toxicity of various cancer chemotherapies. On the other hand, anti-cancer drugs that did not interact with MRP1 carry a low risk for developing MRP1-mediated resistance. [Read the Full Post]