An enzyme-responsive peptide drug conjugate was developed for TGX-D1, a promising
PI3K inhibitor for prostate cancer therapy. LNCaP-specific KYL peptide was used as the …

TGX-221 is a highly potent phosphoinositide 3-kinase β (PI3Kβ) inhibitor that holds great
promise as a novel chemotherapeutic agent to treat prostate cancer. However, poor …

Abstract PI3K/Akt/mTOR pathway is crucial for carcinogenesis and its inhibitors have made a
great progress in cancer treatment. However, there is still a great developing space for PI3K …

TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β
catalytic subunit. Recent studies showed that TGX-221 has antiproliferative activity against …

The serine/threonine kinase Polo-like kinase 1 (Plk1) plays a pivotal role in cell proliferation
and has been validated as a promising anticancer drug target. However, very limited …

Alterations in PIK3CA, the gene encoding the p110α subunit of phosphatidylinositol 3-
kinase (PI3Kα), are frequent in head and neck squamous cell carcinomas. Inhibitors of …

Alternative treatments are urgently needed for prostate cancer, especially to address the
aggressive metastatic castration-resistant disease. Proteolytic enzymes are involved in …

Abstract The phosphoinositide-3-kinases (PI3Ks) are a conserved family of lipid kinases that
phosphorylate the 3-hydroxyl group of phosphatidylinositols in response to extracellular …

Four novel water-soluble peptide-paclitaxel conjugates were designed and synthesized as
prostate-specific antigen (PSA)-activated prodrugs for prostate cancer therapy. These …

One of the major weaknesses of therapeutic peptides is their sensitivity to degradation by
proteolytic enzymes in vivo. Gold nanoparticles (GNPs) are a good carrier for therapeutic …