Recent advances in ligand-based drug design: relevance and utility of the conformationally sampled pharmacophore approach
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 …
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 …
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, …
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 …
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 …
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 …
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 …
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
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 …
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 …
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 …
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 …
of opioids may be misleading. For example, in vitro studies indicated that fentanyl is a P-gp …