title: Immunomodulation using agonists and antagonists: potential clinical applications.
abstract: BACKGROUND
  Extensive studies have gone into understanding the differential role of the innate and adaptive arms of the immune system in the context of various diseases. Receptor-ligand interactions are responsible for mediating cross-talk between the innate and adaptive arms of the immune system, so as to effectively counter the pathogenic challenge. While TLRs remain the best studied innate immune receptor, many other receptor families are now coming to the fore for their role in various pathologies. Research has focused on the discovery of novel agonists and antagonists for these receptors as potential therapeutics.
  
  
  METHODS
  In this review, we present an overview of the recent advances in the discovery of drugs targeting important receptors such as G-protein coupled receptors, TRAIL-R, IL-1β receptor, PPARs, etc. All these receptors play a critical role in the modulation of the immune response. We focus on the recent paradigms applied for the generation of specific and effective therapeutics for these receptors and their status in clinical trials.
  
  
  CONCLUSIONS
  Non-specific activation by antagonist/agonist is a difficult problem to dodge. This demands innovation in ligand designing with the use of strategies such as allosterism and dual-specific ligands. Rigorous preclinical and clinical studies are required in transforming a compound to a therapeutic.
authors.affiliation: Indian Institute of Science, Centre for Infectious Disease Research and Biosafety Laboratories, Department of Microbiology and Cell Biology, Bangalore 560012, India.
authors.forename: Namrata
authors.initials: N
authors.lastname: Iyer
authors.forename: Sandhya A
authors.initials: SA
authors.lastname: Marathe
authors.forename: Debalina
authors.initials: D
authors.lastname: Chaudhuri
authors.forename: Preeti
authors.initials: P
authors.lastname: Garai
authors.forename: Dipshikha
authors.initials: D
authors.lastname: Chakravortty
mesh_terms: D000818:Animals; D002986:Clinical Trials as Topic; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007107:Immune System / Q000187:drug effects* / Q000378:metabolism; D007155:Immunologic Factors / Q000494:pharmacology*; D011956:Receptors, Cell Surface / Q000819:agonists / Q000037:antagonists & inhibitors; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists / Q000037:antagonists & inhibitors; D011971:Receptors, Immunologic / Q000819:agonists / Q000037:antagonists & inhibitors
chemical_list: D007155:Immunologic Factors; D011956:Receptors, Cell Surface; D018160:Receptors, Cytoplasmic and Nuclear; D011971:Receptors, Immunologic