AMD3100/CXCR4 Inhibitor
نویسنده
چکیده
The original bicyclam, JM1657 (JM standing for Johnson Matthey) was discovered as a contaminant in a commercial preparation of monocyclams when evaluated for their anti-HIV activity. The original compound, in which the cyclam rings were tethered by a C–C linkage could not be re-synthesized but launched the synthesis of new bicyclams in which the cyclam moieties were linked through an aliphatic bridge: one of these derivatives, i.e., JM2763, exhibited an anti-HIV activity similar to that of JM1657 (1). The compound was postulated to
منابع مشابه
V3-Independent Competitive Resistance of a Dual-X4 HIV-1 to the CXCR4 Inhibitor AMD3100
A CXCR4 inhibitor-resistant HIV-1 was isolated from a dual-X4 HIV-1 in vitro. The resistant variant displayed competitive resistance to the CXCR4 inhibitor AMD3100, indicating that the resistant variant had a higher affinity for CXCR4 than that of the wild-type HIV-1. Amino acid sequence analyses revealed that the resistant variant harbored amino acid substitutions in the V2, C2, and C4 regions...
متن کاملT134, a small-molecule CXCR4 inhibitor, has no cross-drug resistance with AMD3100, a CXCR4 antagonist with a different structure.
T22, an analog of polyphemusin II (18 amino acid residues), was found to block T-tropic human immunodeficiency virus type 1 (HIV-1) entry into target cells as a CXCR4 inhibitor. We synthesized T134, a small analog (14 amino acid residues) of T22 with reduced positive charges. T134 exhibited highly potent activity and significantly less cytotoxicity in comparison to that of T22. T134 prevents th...
متن کاملEffect of CXCR4 inhibitor AMD3100 on alkaline phosphatase activity and mineralization in osteoblastic MC3T3-E1 cells.
The aim of the study was to investigate the effect of C-X-C chemokine receptor type 4 (CXCR4) inhibitor AMD3100 on the osteogenic differentiation of pre-osteoblastic cell line MC3T3-E1. In this study we found that blocking SDF-1/CXCR4 signaling with AMD3100 strongly suppressed osteogenic differentiation in MC3T3-E1 cells, as evidenced by an early decrease in the activity of alkaline phosphatase...
متن کاملEffect of a nitric oxide synthase inhibitor and a CXC chemokine receptor-4 antagonist on tumor growth and metastasis in a xenotransplanted mouse model of adenoid cystic carcinoma of the oral floor.
Nitric oxide (NO) is related to angiogenesis and tumor progression and chemokine receptor-4 (CXCR4) plays a central role in cell migration in metastasis and dissemination of cancer. The present study evaluated the effectiveness of a NOS inhibitor and a CXCR4 antagonist, given as single agents or in combination, in a xenotransplanted mouse model of adenoid cystic carcinoma (ACC) of the oral floo...
متن کاملMicroRNA-146a and AMD3100, two ways to control CXCR4 expression in acute myeloid leukemias
CXCR4 is a negative prognostic marker in acute myeloid leukemias (AMLs). Therefore, it is necessary to develop novel ways to inhibit CXCR4 expression in leukemia. AMD3100 is an inhibitor of CXCR4 currently used to mobilize cancer cells. CXCR4 is a target of microRNA (miR)-146a that may represent a new tool to inhibit CXCR4 expression. We then investigated CXCR4 regulation by miR-146a in primary...
متن کاملPreparation and preliminary biological evaluation of [153Sm] samarium AMD3100; towards a possible therapeutic chemokine receptor CXCR4 targeting complex
Introduction: In continuation of recent development of possible C-X-C chemokine receptor type 4 (CXCR4) imaging agents, we report the development of a possible CXCR4 targeted therapy agent. Methods: [153Sm]labeled 1,1′-[1,4-phenylenebis(methylene)] bis-1,4,8,11-tetraazacyclo -tetradecane ([153Sm]-AMD3100) was prepared using [153Sm]SmCl3 and AMD-3100 ...
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