Recent advances in ligand-based drug design: relevance and utility of the conformationally sampled pharmacophore approach

C Acharya, A Coop, JE Polli… - Current computer-aided …, 2011 - ingentaconnect.com
In the absence of three-dimensional (3D) structures of potential drug targets, ligand-based
drug design is one of the popular approaches for drug discovery and lead optimization. 3D …

Kappa opioid antagonists: past successes and future prospects

MD Metcalf, A Coop - Drug Addiction: From Basic Research to Therapy, 2008 - Springer
Antagonists of the kappa opioid receptor were initially investigated as pharmacological tools
that would reverse the effects of kappa opioid receptor agonists. In the years following the …

Letrozole is more effective neoadjuvant endocrine therapy than tamoxifen for ErbB-1–and/or ErbB-2–positive, estrogen receptor–positive primary breast cancer …

MJ Ellis, A Coop, B Singh, L Mauriac… - Journal of Clinical …, 2001 - ascopubs.org
PURPOSE: Expression of ErbB-1 and ErbB-2 (epidermal growth factor receptor and HER2/neu)
in breast cancer may cause tamoxifen resistance, but not all studies concur. Additionally, …

Opioid analgesics and P-glycoprotein efflux transporters: a potential systems-level contribution to analgesic tolerance

SL Mercer, A Coop - Current topics in medicinal chemistry, 2011 - ingentaconnect.com
Chronic clinical pain remains poorly treated. Despite attempts to develop novel analgesic
agents, opioids remain the standard analgesics of choice in the clinical management of …

Letrozole inhibits tumor proliferation more effectively than tamoxifen independent of HER1/2 expression status

MJ Ellis, A Coop, B Singh, Y Tao, A Llombart-Cussac… - Cancer research, 2003 - AACR
Background: The biological basis for the superior efficacy of neoadjuvant letrozole versus
tamoxifen for postmenopausal women with estrogen receptor (ER)-positive locally advanced …

[PDF][PDF] A small-molecule inhibitor of BCL6 kills DLBCL cells in vitro and in vivo

…, C Fares, CH Arrowsmith, SN Yang, M Garcia, A Coop… - Cancer cell, 2010 - cell.com
The BCL6 transcriptional repressor is the most frequently involved oncogene in diffuse
large B cell lymphoma (DLBCL). We combined computer-aided drug design with functional …

[HTML][HTML] Identification of a new class of molecules, the arachidonyl amino acids, and characterization of one member that inhibits pain

…, RE Zipkin, R Sivakumar, A Coop… - Journal of Biological …, 2001 - ASBMB
In mammals, specific lipids and amino acids serve as crucial signaling molecules. In bacteria,
conjugates of lipids and amino acids (referred to as lipoamino acids) have been identified …

Oxycodone induces overexpression of P‐glycoprotein (ABCB1) and affects paclitaxel's tissue distribution in Sprague Dawley rats

HE Hassan, AL Myers, IJ Lee, A Coop… - Journal of …, 2007 - Elsevier
Previous studies suggest that P‐glycoprotein (P‐gp) modulates the PK/PD of many compounds
including opioid agonists and chemotherapeutic agents. The objective of this study was …

Hallucinogen-like actions of 5-methoxy-N, N-diisopropyltryptamine in mice and rats

…, JR Eckler, RA Rabin, JC Winter, A Coop… - Pharmacology …, 2006 - Elsevier
Few studies have examined the effects of 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT)
in vivo. In these studies, 5-MeO-DIPT was tested in a drug-elicited head twitch assay in …

Differential involvement of P-glycoprotein (ABCB1) in permeability, tissue distribution, and antinociceptive activity of methadone, buprenorphine, and diprenorphine: in …

HE Hassan, AL Myers, A Coop… - Journal of pharmaceutical …, 2009 - Elsevier
Conclusions based on either in vitro or in vivo approach to evaluate the P-gp affinity status
of opioids may be misleading. For example, in vitro studies indicated that fentanyl is a P-gp …