Abstract: The present application discloses compounds of e.g. formulae (2), (1A), (1B) or (1C) as selective atypical chemokine receptor 3 (ACKR3) modulators for the treatment of e.g. cancer, atherosclerotic vascular disease, cardiovascular diseases, fibrosis (e.g. cardiac fibrosis), inflammatory or autoimmune diseases and conditions, conditions of excessive or abnormal vascularization (e.g. wound healing), stem cell differentiation and mobilization disorders, brain and neuronal dysfunctions (e.g. Alzheimer's disease, multiple sclerosis and demyelinating diseases), kidney dysfunction, renal dysfunction, preeclampsia, human immunodeficiency virus (HIV) infection and obesity. Further provided are said compounds for use in methods for in vitro or ex vivo diagnosis, prediction, prognosis and/or monitoring of a disease or condition characterized by an aberrant level of ACKR3 polypeptide, as well as for use in in vitro methods for identifying an agent useful as a therapeutic. An exemplary compound is e.g. WW-1.

Abstract: The application discloses selective ACKR3 modulating peptides comprising amino acid sequence FGGX1MRRX2 (SEQ ID NO: 1), wherein X1 is F or W; X2 is K, V or F; and wherein the peptides have a length of at most 15 amino acids; fusion proteins comprising the peptides as taught herein; nucleic acids encoding the peptides as taught herein; nucleic acid expression cassettes and vectors comprising the nucleic acid as taught herein; and pharmaceutical compositions comprising the peptide as taught herein or the nucleic acid as taught herein. Further provided are the peptide as taught herein for use as a medicament; methods for in vitro or ex vivo diagnosis, prediction, prognosis and/or monitoring of a disease or condition characterized by an aberrant level of ACKR3 polypeptide using the peptide as taught herein; and in vitro methods for identifying an agent useful as a therapeutic using the peptide as taught herein.