Inhibitory effect of
CXC chemokine receptor 4 antagonist AMD3100 on bleomycin induced murine pulmonary fibrosis.
Azevedo - Pereira JM, Santos - Costa Q.
[Chemokine receptors and its importance in the replication cycle of human immunodeficiency virus: clinical and therapeutic implications].
C - X-C
chemokine receptor type 4 (CXCR4), also known as fusin or cluster of differentiation 184 (CD184), is a seven transmembrane (TM) G - protein coupled receptor (GPCR) belonging to Class I GPCR or rhodopsin - like GPCR family [1, 2].
Synthesis and structure - activity relationships of azamacrocyclic C -
X-C chemokine receptor 4 antagonists: analogues containing a single azamacrocyclic ring are potent inhibitors of T - cell tropic (X4) HIV - 1 replication.
As a postdoc I cloned the
CCR6 chemokine receptor and now as a group leader I head a team looking at chemokine biology in atherosclerosis, the disease process that underlies the development of myocardial infarction and strokes.
The implication, he says, is that compounds that
block chemokine receptors might someday be used in people to protect wounded arteries.
While we have demonstrated that CXCR4 is not essential for CD4 + T cell viability and function in vitro and in humanized mice in vivo, the redundancy of
lymphocyte chemokine receptors and their ligands makes predicting the in vivo consequences of cxcr4 disruption in a normal host on CD4 + T cell function and trafficking difficult.
Structure - activity relationships of cyclic peptide -
based chemokine receptor CXCR4 antagonists: disclosing the importance of side - chain and backbone functionalities.
Akashi T, Koizumi K, Tsuneyama K, Saiki I, Takano Y, Fuse
H. Chemokine receptor CXCR4 expression and prognosis in patients with metastatic prostate cancer.
CXCR4
Chemokine Receptor Overview: Biology, Pathology and Applications in Imaging and Therapy Orit Jacobson, Ido Dov Weiss Theranostics 2013; 3 (1): 1 - 2.
Combining computational methods with site directed mutagenesis we have studied antagonist binding for
several chemokine receptors such as CCR1, CCR2, CCR3, CCR5, CXCR1, CXCR2, CXCR3, and CXCR4.
They have made key contributions in understanding the immunological basis of asthma, including identifying CCR4 as a
key chemokine receptor that regulates recruitment of T cells to the human asthmatic airways.
McGuire HM, Vogelzang A, Ma CS, Hughes WE, Silveira PA, Tangye SG, Christ D, Fulcher D, Falcone M, King C. Subset of interleukin - 21 (+)
chemokine receptor CCR9 (+) T helper cells target accessory organs of the digestive system in autoimmunity.
Chemokines and
chemokine receptors in chronic lymphocytic leukemia (CLL): from understanding the basics towards therapeutic targeting.
A duodenally absorbable
CXC chemokine receptor 4 antagonist, KRH - 1636, exhibits a potent and selective anti-HIV-1 activity.
The ECL2 was chosen because this region is less well conserved amongst the CXC family
of chemokine receptors, which should reduce the frequency with which other CXC receptors might be targeted, and because ECL2 is important in supporting interactions with the HIV - 1 Env protein [37], [38].
To do so, the team looked to the mechanisms that control the movement of cells into the bone marrow in the first place — CXCR4,
a chemokine receptor, and its ligand, CXCL12.
Both markers, CX3CR1 (green) and CCR2 (red), are
chemokine receptors.
The chemokine receptor CXCR4 is required for outgrowth of colon carcinoma micrometastases.
HIV - 1 entry into CD4 + cells is mediated by
the chemokine receptor CC - CKR - 5.
Li RJ, Zhao LJ, Zhan ZL, Lu X, Gong LL, Wang P. [Significance of expression of
chemokine receptor and matrix metalloproteinase in small cell lung cancer].
The human chemokine system is comprised of 50 chemokines and 20
chemokine receptors [6].
Agonists for
the Chemokine Receptor CXCR4.
The chemokine receptor CXCR - 4 is expressed on CD34 + hematopoietic progenitors and leukemic cells and mediates transendothelial migration induced by stromal cell - derived factor - 1.
CXC
chemokine receptor 4 expressed in T cells plays an important role in the development of collagen - induced arthritis.
Pharmacology of AMD3465: a small molecule antagonist of
the chemokine receptor CXCR4.
Chronic lymphocytic leukemia B cells express functional CXCR4
chemokine receptors that mediate spontaneous migration beneath bone marrow stromal cells.
Small peptide inhibitors of the CXCR4
chemokine receptor (CD184) antagonize the activation, migration, and antiapoptotic responses of CXCL12 in chronic lymphocytic leukemia B cells.
Pharmacokinetics and safety of AMD - 3100, a novel antagonist of the CXCR - 4
chemokine receptor, in human volunteers.
Mohle R, Failenschmid C, Bautz F, Kanz L. Overexpression of
the chemokine receptor CXCR4 in B cell chronic lymphocytic leukemia is associated with increased functional response to stromal cell - derived factor - 1 (SDF - 1).
Mutations in
the chemokine receptor gene CXCR4 are associated with WHIM syndrome, a combined immunodeficiency disease.
Targeting
Chemokine receptors for pancreatic cancer: We are particularly interested in understanding the structural basis of antagonist binding to chemokine receptors.
Cxcl12 evolution - subfunctionalization of a ligand through altered interaction with
the chemokine receptor.
Persistent induction of
the chemokine receptor CXCR4 by TGF - beta 1 on synovial T cells contributes to their accumulation within the rheumatoid synovium.
The histone deacetylase inhibitor suberoylanilide hydroxamic acid induces apoptosis, down - regulates the CXCR4
chemokine receptor and impairs migration of chronic lymphocytic leukemia cells