Chemokine receptor antagonists: overcoming developmental hurdles
R Horuk - Nature reviews Drug discovery, 2009 - nature.com
Chemokine receptors have a key role in the pathogenesis of autoimmune diseases,
inflammation and viral infection. However, with the exception of selective CCR5 antagonists …
inflammation and viral infection. However, with the exception of selective CCR5 antagonists …
Chemokine receptor antagonists: Part 1
Background: Chemokines were originally defined as host defense proteins, however, their
biological role goes well beyond this simple description of their function as immune cell …
biological role goes well beyond this simple description of their function as immune cell …
Role of eotaxin-1 signaling in ovarian cancer
V Levina, BM Nolen, AM Marrangoni, P Cheng… - Clinical Cancer …, 2009 - AACR
Purpose: Tumor cell growth and migration can be directly regulated by chemokines. In the
present study, the association of CCL11 with ovarian cancer has been investigated …
present study, the association of CCL11 with ovarian cancer has been investigated …
Chemokine receptor antagonists: part 2
Background: The first part of this two-part review discussed approaches to generating
antagonists for some of the CC chemokine receptors, including CCR1, CCR2, CCR3, and …
antagonists for some of the CC chemokine receptors, including CCR1, CCR2, CCR3, and …
SB265610 is an allosteric, inverse agonist at the human CXCR2 receptor
ME Bradley, ME Bond, J Manini… - British journal of …, 2009 - Wiley Online Library
Background and purpose: In several previous studies, the C‐X‐C chemokine receptor
(CXCR) 2 antagonist 1‐(2‐bromo‐phenyl)‐3‐(7‐cyano‐3H‐benzotriazol‐4‐yl)‐urea …
(CXCR) 2 antagonist 1‐(2‐bromo‐phenyl)‐3‐(7‐cyano‐3H‐benzotriazol‐4‐yl)‐urea …
Quantifying biological activity in chemical terms: a pharmacology primer to describe drug effect
T Kenakin - 2009 - ACS Publications
Drugs can initiate, inhibit, modulate, or potentiate basal activity in cells to produce
physiological effects. The interplay between the fundamental affinity and efficacy of drugs …
physiological effects. The interplay between the fundamental affinity and efficacy of drugs …
Chemokines as possible targets in modulation of the secondary damage after acute spinal cord injury: a review
P Gál, P Kravčuková, M Mokrý, D Kluchová - Cellular and molecular …, 2009 - Springer
In spite of many promising experimental studies, an effective treatment dramatically
eliminating the secondary damage after spinal cord injury (SCI) is still missing. Since clinical …
eliminating the secondary damage after spinal cord injury (SCI) is still missing. Since clinical …
Promiscuous drugs as therapeutics for chemokine receptors
R Horuk - Expert reviews in molecular medicine, 2009 - cambridge.org
Chemokine receptor antagonists that held much promise for the treatment of autoimmune
and inflammatory diseases have recently performed poorly in clinical trials, resulting in …
and inflammatory diseases have recently performed poorly in clinical trials, resulting in …
CCR3 antagonists: a survey of the patent literature
L Gong, RS Wilhelm - Expert opinion on therapeutic patents, 2009 - Taylor & Francis
Background: Since the mid-1990s, there has been significant effort invested in the discovery
and clinical development of CC chemokine receptor-3 (CCR3) antagonists as potential …
and clinical development of CC chemokine receptor-3 (CCR3) antagonists as potential …
Enzymatic activities in chemokine-mediated inflammation
RD Berahovich, Z Miao, B Premack… - US Patent 7,572,600, 2009 - Google Patents
Truncated chemokines lacking an N-terminal region that acti vate CCR1 and/or FPRL1 and
compositions containing the truncated chemokines are provided. Methods of identifying …
compositions containing the truncated chemokines are provided. Methods of identifying …