FK506 binding
Definition
Target type: molecularfunction
Binding to a 23-membered macrolide lactone FK506. [GOC:jl]
FK506 binding protein (FKBP) is a molecular chaperone that plays a crucial role in protein folding and signaling pathways. It derives its name from its ability to bind the immunosuppressant drug FK506. FKBP exhibits diverse functions, including:'
'1. **Peptidyl-prolyl cis-trans isomerase (PPIase) activity:** FKBP catalyzes the isomerization of proline residues within proteins, facilitating the transition between cis and trans conformations. This activity is essential for proper protein folding and the formation of functional protein structures.'
'2. **Chaperone activity:** FKBP interacts with unfolded or misfolded proteins, preventing their aggregation and promoting their correct folding. This chaperone function is crucial for maintaining cellular homeostasis and preventing protein misfolding-related diseases.'
'3. **Signaling pathway regulation:** FKBP participates in various signaling pathways, including the calcineurin pathway. FK506 binding to FKBP inhibits calcineurin activity, a phosphatase that plays a role in immune responses and cellular growth. This inhibition is the basis for the immunosuppressive effects of FK506 in transplantation.'
'4. **Protein-protein interactions:** FKBP interacts with a variety of proteins, including the glucocorticoid receptor, the heat shock protein 90 (Hsp90), and other chaperones. These interactions contribute to diverse cellular processes, such as hormone signaling, protein stability, and cellular stress response.'
'5. **Regulation of gene expression:** FKBP can influence gene expression by interacting with transcription factors and other regulatory proteins. This activity contributes to the modulation of cellular processes and the response to environmental cues.'
'The molecular function of FKBP is thus multifaceted and essential for maintaining cellular integrity, regulating signaling pathways, and facilitating proper protein folding.'
"
Proteins (6)
| Protein | Definition | Taxonomy |
|---|---|---|
| Peptidyl-prolyl cis-trans isomerase FKBP1A | [no definition available] | Bos taurus (cattle) |
| Peptidyl-prolyl cis-trans isomerase FKBP5 | A peptidyl-prolyl cis-trans isomerase FKBP5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13451] | Homo sapiens (human) |
| Peptidyl-prolyl cis-trans isomerase FKBP4 | A peptidyl-prolyl cis-trans isomerase FKBP4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q02790] | Homo sapiens (human) |
| Peptidyl-prolyl cis-trans isomerase FKBP3 | A peptidyl-prolyl cis-trans isomerase FKBP3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q00688] | Homo sapiens (human) |
| Peptidyl-prolyl cis-trans isomerase FKBP1B | A peptidyl-prolyl cis-trans isomerase FKBP1B that is encoded in the genome of human. [PRO:DNx, UniProtKB:P68106] | Homo sapiens (human) |
| Peptidyl-prolyl cis-trans isomerase FKBP1A | A peptidyl-prolyl cis-trans isomerase FKBP1A that is encoded in the genome of human. [PRO:DNx, UniProtKB:P62942] | Homo sapiens (human) |
Compounds (16)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| imidazole | 1H-imidazole : An imidazole tautomer which has the migrating hydrogen at position 1. imidazole: RN given refers to parent cpd | imidazole | |
| thiabendazole | Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate | 1,3-thiazoles; benzimidazole fungicide; benzimidazoles | antifungal agrochemical; antinematodal drug |
| cycloheximide | cycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus. Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis. | antibiotic fungicide; cyclic ketone; dicarboximide; piperidine antibiotic; piperidones; secondary alcohol | anticoronaviral agent; bacterial metabolite; ferroptosis inhibitor; neuroprotective agent; protein synthesis inhibitor |
| 2-hydroxypyridine | hydroxypyridine : Any member of the class of pyridines with at least one hydroxy substituent. pyridin-2-ol : A monohydroxypyridine that is pyridine substituted by a hydroxy group at position 2. | monohydroxypyridine | plant metabolite |
| 2-piperidone | 2-piperidone: structure given in first source piperidin-2-one : A delta-lactam that is piperidine which is substituted by an oxo group at position 2. | delta-lactam; piperidones | EC 1.2.1.88 (L-glutamate gamma-semialdehyde dehydrogenase) inhibitor |
| 4-methylimidazole | 4-methylimidazole : Imidazole substituted at position 4 by a methyl group. 4-methylimidazole: RN given refers to parent cpd | imidazoles | carcinogenic agent; reaction intermediate |
| 3-(3-pyridyl)-1-propyl-(2s)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate | |||
| tacrolimus | tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro. | macrolide lactam | bacterial metabolite; immunosuppressive agent |
| N-(2-fluorophenyl)-2-[2-(4-thiazolyl)-1-benzimidazolyl]acetamide | benzimidazoles | ||
| biricodar | biricodar: a non-macrocyclic ligand for FKBP12; structure in first source | alpha-amino acid ester | |
| pd 407824 | |||
| l 683590 | immunomycin: from Streptomyces hygroscopicus; structure given in first source | ether; lactol; macrolide; secondary alcohol | antifungal agent; bacterial metabolite; immunosuppressive agent |
| cyclosporine | ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF | homodetic cyclic peptide | anti-asthmatic drug; anticoronaviral agent; antifungal agent; antirheumatic drug; carcinogenic agent; dermatologic drug; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; geroprotector; immunosuppressive agent; metabolite |
| sirolimus | sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent. Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties. | antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol | antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor |
| bastadin 5 | |||
| timcodar | timcodar: a mutlidrug resistance inhibitor; structure in first source |