Fifty years in search of selective antiviral drugs: miniperspective

E De Clercq - Journal of medicinal chemistry, 2019 - ACS Publications
Fifty years of research (1968–2018) toward the identification of selective antiviral drugs have
been primarily focused on antiviral compounds active against DNA viruses (HSV, VZV, CMV …

Potential clinical applications of the CXCR4 antagonist bicyclam AMD3100

E De Clercq - Mini reviews in medicinal chemistry, 2005 - ingentaconnect.com
The bicyclam AMD3100 (originally called JM3100), in which the two cyclam rings are
tethered by an aromatic bridge, emanated from JM2763, where the two cyclam moieties are …

AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor

S Hatse, K Princen, E De Clercq, MM Rosenkilde… - Biochemical …, 2005 - Elsevier
The chemokine receptors CCR5 and CXCR4 function as coreceptors for human
immunodeficiency virus (HIV) and are attractive targets for the development of anti-HIV …

Small molecules anti-HIV therapeutics targeting CXCR4

F Grande, A Garofalo, N Neamati - Current pharmaceutical …, 2008 - ingentaconnect.com
HIV cellular entry is a multistep process that requires the interaction of a viral envelope
glycoprotein (gp120) and a host receptor (CD4) followed by binding to a co-receptor. The …

AMD3100/CXCR4 inhibitor

E De Clercq - Frontiers in immunology, 2015 - frontiersin.org
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 …

A cutting‐edge view on the current state of antiviral drug development

E De Clercq - Medicinal research reviews, 2013 - Wiley Online Library
Prominent in the current stage of antiviral drug development are:(i) for human
immunodeficiency virus (HIV), the use of fixed‐dose combinations (FDCs), the most recent …

Development of novel CXCR4-based therapeutics

A Peled, O Wald, J Burger - Expert opinion on investigational drugs, 2012 - Taylor & Francis
Introduction: During embryogenesis, CXCR4, a chemokine receptor, and its ligand, stromal
cell-derived factor-1 (SDF-1/CXCL12), are critically involved in the development of the …

Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes

H Tamamura, A Omagari, S Oishi, T Kanamoto… - Bioorganic & medicinal …, 2000 - Elsevier
A polyphemusin peptide analogue, T22 ([Tyr5, 12, Lys7]-polyphemusin II), and its shortened
potent analogues, T134 (des-[Cys8, 13, Tyr9, 12]-[d-Lys10, Pro11, l-citrulline16]-T22 without …

Targeting CXCR4 in HIV cell-entry inhibition.

A Steen, TW Schwartz… - Mini reviews in medicinal …, 2009 - ingentaconnect.com
CXCR4 and CCR5 constitute the two major coreceptors for HIV-1 entry into host cells. In the
course of an HIV-infection, a coreceptor switch takes place in approximately half of the …

Function-oriented development of CXCR4 antagonists as selective human immunodeficiency virus (HIV)-1 entry inhibitors

CH Wu, CJ Wang, CP Chang, YC Cheng… - Journal of medicinal …, 2015 - ACS Publications
Motivated by the pivotal role of CXCR4 as an HIV entry co-receptor, we herein report a de
novo hit-to-lead effort on the identification of subnanomolar purine-based CXCR4 …