Robert Milne
YOU?
Author Swipe
View article: The Ottawa Mobile Screening Program—Concept and First 18 Months of Experience with a Community-Based Outreach Cardiovascular Prevention Program
The Ottawa Mobile Screening Program—Concept and First 18 Months of Experience with a Community-Based Outreach Cardiovascular Prevention Program Open
In this innovative prevention initiative, we demonstrate the feasibility of an outreach mobile screening program, revealing relatively high rates of VHD, nonvalvular abnormalities, and uncontrolled risk factors. These findings highlight th…
View article: A brain-penetrant CDK4/6 inhibitor - AU3-14 shows robust anti-tumor efficacy against glioblastoma
A brain-penetrant CDK4/6 inhibitor - AU3-14 shows robust anti-tumor efficacy against glioblastoma Open
The cyclin D-CDK4/6-INK4-Rb pathway is frequently dysregulated in glioblastoma (GBM), the most aggressive and poorly prognosed brain malignancy. Despite extensive research, advances in GBM treatment have seen limited progress, with current…
View article: An Orally Bioavailable and Highly Efficacious Inhibitor of CDK9/FLT3 for the Treatment of Acute Myeloid Leukemia
An Orally Bioavailable and Highly Efficacious Inhibitor of CDK9/FLT3 for the Treatment of Acute Myeloid Leukemia Open
Mutations in FMS-like tyrosine kinase 3 (FLT3) occur in approximately one-third of AML patients and are associated with a particularly poor prognosis. The most common mutation, FLT3-ITD, is a self-activating internal tandem duplication (IT…
View article: Liposomal 5-Fluorouracil Polymer Complexes Facilitate Tumor-Specific Delivery: Pharmaco-Distribution Kinetics Using Microdialysis
Liposomal 5-Fluorouracil Polymer Complexes Facilitate Tumor-Specific Delivery: Pharmaco-Distribution Kinetics Using Microdialysis Open
Liposomes are widely used as carriers for anticancer drugs due to their ability to prolong the retention of encapsulated drugs in blood plasma while directing their distribution increasingly into tumor tissue. We report on the development …
View article: CDK9: A Comprehensive Review of Its Biology, and Its Role as a Potential Target for Anti-Cancer Agents
CDK9: A Comprehensive Review of Its Biology, and Its Role as a Potential Target for Anti-Cancer Agents Open
Cyclin-dependent kinases (CDKs) are proteins pivotal to a wide range of cellular functions, most importantly cell division and transcription, and their dysregulations have been implicated as prominent drivers of tumorigenesis. Besides the …
View article: Targeting CDK9 for treatment of colorectal cancer
Targeting CDK9 for treatment of colorectal cancer Open
Colorectal cancer (CRC) remains one of the most lethal human malignancies, and pursuit of new therapeutic targets for treatment has been a major research focus. Cyclin‐dependent kinase 9 (CDK9), which plays a crucial role in transcription,…
View article: Discovery of CDK5 Inhibitors through Structure-Guided Approach
Discovery of CDK5 Inhibitors through Structure-Guided Approach Open
Specific abrogation of cyclin-dependent kinase 5 (CDK5) activity has been validated as a viable approach for the development of anticancer agents. However, no selective CDK5 inhibitor has been reported to date. Herein, a structure-based in…
View article: Enantioselectivity in the tissue distribution of perhexiline contributes to different effects on hepatic histology and peripheral neural function in rats
Enantioselectivity in the tissue distribution of perhexiline contributes to different effects on hepatic histology and peripheral neural function in rats Open
Perhexiline, a chiral drug, is a potent antiischemic agent whose clinical utility is limited by hepatic and neural toxicities. It inhibits mitochondrial carnitine palmitoyltransferase‐1, however, excessive inhibition predisposes toward tis…
View article: Discovery and pharmacological characterization of a novel series of highly selective inhibitors of cyclin‐dependent kinases 4 and 6 as anticancer agents
Discovery and pharmacological characterization of a novel series of highly selective inhibitors of cyclin‐dependent kinases 4 and 6 as anticancer agents Open
Background and Purpose Cyclin D‐dependent kinases 4 and 6 (CDK4/6) are crucial regulators of the G1 to S phase transition of the cell cycle and are actively pursued as therapeutic targets in cancer. We sought to discover a novel series of …
View article: Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-<i>N</i>-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation
Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-<i>N</i>-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation Open
Cyclin D dependent kinases (CDK4 and CDK6) regulate entry into S phase of the cell cycle and are validated targets for anticancer drug discovery. Herein we detail the discovery of a novel series of 4-thiazol-N-(pyridin-2-yl)pyrimidin-2-ami…
View article: Targeting CDK9: a promising therapeutic opportunity in prostate cancer
Targeting CDK9: a promising therapeutic opportunity in prostate cancer Open
Cyclin-dependent kinase 9 (CDK9) is a key transcriptional regulator and a lucrative target for cancer treatment. Targeting CDK9 can effectively confine the hyperactivity of androgen receptor and the constitutive expression of anti-apoptoti…
View article: Inhibition of Mnk enhances apoptotic activity of cytarabine in acute myeloid leukemia cells
Inhibition of Mnk enhances apoptotic activity of cytarabine in acute myeloid leukemia cells Open
Cytarabine (Ara-C) is a first line clinical therapeutic agent for treatment of acute myeloid leukemia (AML). However, this therapy is limited due to high rate of resistance and relapse. Recent research has revealed that the poor prognosis …