Brain exposure of two selective dual CDK4 and CDK6 inhibitors and the antitumor activity of CDK4 and CDK6 inhibition in combination with temozolomide in an …

…, BA Staton, RT Ajamie, GA Sawada… - Drug Metabolism and …, 2015 - ASPET
Effective treatments for primary brain tumors and brain metastases represent a major unmet
medical need. Targeting the CDK4/CDK6-cyclin D1-Rb-p16/ink4a pathway using a potent …

Permeability of bovine brain microvessel endothelial cells in vitro: barrier tightening by a factor released from astroglioma cells

TJ Raub, SL Kuentzel, GA Sawada - Experimental cell research, 1992 - Elsevier
It has been shown both in vivo and in culture that astrocytes communicate with brain microvessel
endothelial cells (BMECs) to induce many of the blood—brain barrier characteristics …

Pioglitazone preserves pancreatic islet structure and insulin secretory function in three murine models of type 2 diabetes

AR Diani, G Sawada, B Wyse… - American Journal of …, 2004 - journals.physiology.org
Thiazolidinediones may slow the progression of type 2 diabetes by preserving pancreatic β-cells.
The effects of pioglitazone (PIO) on structure and function of β-cells in KKA(y), C57BL/…

Integration of in silico and in vitro tools for scaffold optimization during drug discovery: predicting P-glycoprotein efflux

PV Desai, GA Sawada, IA Watson… - Molecular …, 2013 - ACS Publications
In silico tools are regularly utilized for designing and prioritizing compounds to address
challenges related to drug metabolism and pharmacokinetics (DMPK) during the process of drug …

Stereochemistry balances cell permeability and solubility in the naturally derived phepropeptin cyclic peptides

…, JA Barrett, G Sawada… - ACS Medicinal …, 2016 - ACS Publications
Cyclic peptide (CP) natural products provide useful model systems for mapping “beyond-Rule-of-5”
(bRo5) space. We identified the phepropeptins as natural product CPs with potential …

Selenorhodamine photosensitizers for photodynamic therapy of P-glycoprotein-expressing cancer cells

JE Hill, MK Linder, KS Davies, GA Sawada… - Journal of Medicinal …, 2014 - ACS Publications
We examined a series of selenorhodamines with amide and thioamide functionality at the 5-position
of a 9-(2-thienyl) substituent on the selenorhodamine core for their potential as …

Breast cancer resistance protein interacts with various compounds in vitro, but plays a minor role in substrate efflux at the blood-brain barrier

R Zhao, TJ Raub, GA Sawada, SC Kasper… - Drug Metabolism and …, 2009 - ASPET
Expression of breast cancer resistance protein (Bcrp) at the blood-brain barrier (BBB) has
been revealed recently. To investigate comprehensively the potential role of Bcrp at the …

Rhodamine inhibitors of P-glycoprotein: an amide/thioamide “switch” for ATPase activity

…, MC Bartlett, DM Clarke, GA Sawada… - Journal of medicinal …, 2009 - ACS Publications
We have examined 46 tetramethylrosamine/rhodamine derivatives with structural diversity in
the heteroatom of the xanthylium core, the amino substituents of the 3- and 6-positions, and …

[HTML][HTML] Advances in blood–brain barrier modeling in microphysiological systems highlight critical differences in opioid transport due to cortisol exposure

…, SL Faley, Y Shi, KM Hillgren, GA Sawada… - Fluids and Barriers of …, 2020 - Springer
Background The United States faces a national crisis involving opioid medications, where
currently more than 130 people die every day. To combat this epidemic, a better …

Increased lipophilicity and subsequent cell partitioning decrease passive transcellular diffusion of novel, highly lipophilic antioxidants

GA Sawada, CL Barsuhn, BS Lutzke… - … of Pharmacology and …, 1999 - ASPET
Oxidative stress is considered a cause or propagator of acute and chronic disorders of the
central nervous system. Novel 2,4-diamino-pyrrolo[2,3-d]pyrimidines are potent inhibitors of …