title: FK506-binding protein 12 ligands: a patent review.
abstract: BACKGROUND
  FK506-binding protein 12 (FKBP12) is an endogenous protein with peptidyl-prolyl isomerase (PPIase) activity. Natural compounds FK506, rapamycin and ascomycin, are FKBP12 ligands used for treating organ transplant rejection and other diseases. Small ligands that also interact with FKBP12 are designed and synthetized based on the natural ligands. This suggests that targeting FKBP12 has potential in the treatment of multiple diseases.
  
  
  METHODS
  This article describes the features of FKBP12 and the therapeutic actions of agents targeting FKBP12 reported in the published articles and patents.
  
  
  CONCLUSIONS
  The multiple functions of FKBP12 cause side effects during therapy with FKBP12 ligands. The interaction between FKBP12 and other receptors should be explored to guide their use as drugs in the clinical setting. In addition, the neuroprotective mechanism of small-molecule FKBP12 ligands needs further study in order to develop them as novel drugs for treating neurological disorders.
authors: Nanjing Medical University, The First Affiliated Hospital, Research Division of Clinical Pharmacology , 300 Guangzhou Road, Nanjing, Jiangsu Province, 210029 , China.
authors: Fei
authors: F
authors: Liu
authors: Yong-Qing
authors: YQ
authors: Wang
authors: Ling
authors: L
authors: Meng
authors: Min
authors: M
authors: Gu
authors: Ruo-Yun
authors: RY
authors: Tan
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D003872:Dermatitis / Q000188:drug therapy; D006801:Humans; D007166:Immunosuppressive Agents / Q000494:pharmacology / Q000627:therapeutic use; D008024:Ligands; D018696:Neuroprotective Agents / Q000494:pharmacology / Q000627:therapeutic use; D010330:Patents as Topic; D020123:Sirolimus / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D054852:Small Molecule Libraries; D016559:Tacrolimus / Q000494:pharmacology / Q000627:therapeutic use; D022061:Tacrolimus Binding Protein 1A / Q000187:drug effects*; D014786:Vision Disorders / Q000188:drug therapy
chemical_list: D000970:Antineoplastic Agents; D007166:Immunosuppressive Agents; D008024:Ligands; D018696:Neuroprotective Agents; D054852:Small Molecule Libraries; D022061:Tacrolimus Binding Protein 1A; D020123:Sirolimus; D016559:Tacrolimus