Target type: molecularfunction
Binding to a transforming growth factor beta receptor. [GOC:ai]
Transforming growth factor beta (TGF-β) receptor binding is a crucial molecular process involved in cell signaling, ultimately leading to diverse cellular responses. TGF-β, a pleiotropic cytokine, exerts its effects by binding to its specific receptors, initiating a cascade of intracellular events. The TGF-β receptors are transmembrane proteins with serine/threonine kinase activity. They are classified into three types: TGF-β receptor type I (TGF-βRI), TGF-β receptor type II (TGF-βRII), and TGF-β receptor type III (TGF-βRIII).
TGF-βRII, a constitutively active kinase, serves as the primary receptor for TGF-β. Upon TGF-β binding to TGF-βRII, the complex recruits TGF-βRI, forming a heteromeric complex. TGF-βRII then phosphorylates TGF-βRI, activating its kinase activity. The activated TGF-βRI, in turn, phosphorylates intracellular signaling molecules, including Smad proteins. The phosphorylation of Smad proteins triggers their translocation to the nucleus, where they regulate gene expression, contributing to the biological effects of TGF-β.
The molecular function of TGF-β receptor binding encompasses the following key steps:
1. **Ligand binding:** TGF-β binds to the extracellular domain of TGF-βRII with high affinity, initiating the signaling cascade.
2. **Receptor complex formation:** TGF-βRII recruits TGF-βRI to form a heteromeric complex.
3. **Phosphorylation and activation:** TGF-βRII phosphorylates TGF-βRI, activating its kinase activity.
4. **Downstream signaling:** Activated TGF-βRI phosphorylates Smad proteins, triggering their translocation to the nucleus.
5. **Gene regulation:** Smad proteins in the nucleus regulate gene expression, influencing various cellular processes.
The molecular function of TGF-β receptor binding is critical for a wide range of cellular processes, including cell growth, proliferation, differentiation, apoptosis, migration, and extracellular matrix production. Dysregulation of TGF-β signaling has been implicated in various diseases, including cancer, fibrosis, and immune disorders.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Ubiquitin carboxyl-terminal hydrolase 15 | A ubiquitin carboxyl-terminal hydrolase 15 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y4E8] | 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) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| 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 |
| celastrol | monocarboxylic acid; pentacyclic triterpenoid | anti-inflammatory drug; antineoplastic agent; antioxidant; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; Hsp90 inhibitor; metabolite | |
| 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 | |
| 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 |
| acetyl isogambogic acid | acetyl isogambogic acid: structure in first source | ||
| bastadin 5 | |||
| timcodar | timcodar: a mutlidrug resistance inhibitor; structure in first source |