Target type: molecularfunction
Binding to an activin receptor. [GOC:BHF, GOC:vk]
Activin receptors are transmembrane proteins that belong to the transforming growth factor-beta (TGF-β) superfamily. They play crucial roles in a wide range of biological processes, including cell growth, differentiation, and development. Activin receptors bind to activin ligands, which are dimeric proteins composed of two related subunits, known as activin A, B, or AB. Upon ligand binding, activin receptors undergo a series of conformational changes that ultimately lead to the activation of intracellular signaling pathways. The molecular function of activin receptor binding can be described as follows:
1. **Ligand Recognition and Binding:** Activin receptors possess extracellular domains that specifically recognize and bind to activin ligands. The interaction between the receptor and the ligand is mediated by non-covalent bonds, including hydrogen bonds and van der Waals forces. The binding affinity of activin receptors for different activin ligands varies, contributing to the specificity of signaling.
2. **Receptor Dimerization:** Upon ligand binding, activin receptors undergo dimerization, forming a complex of two receptor molecules. This dimerization is essential for signal transduction, as it brings the intracellular domains of the receptors into close proximity, facilitating the activation of downstream signaling pathways.
3. **Phosphorylation Cascade:** The intracellular domains of activin receptors contain serine/threonine kinase domains. Upon ligand binding and dimerization, these kinase domains become activated, leading to the phosphorylation of downstream signaling proteins. This phosphorylation cascade amplifies the signal and initiates the activation of specific transcription factors.
4. **Transcriptional Regulation:** The activated signaling pathways ultimately regulate the expression of target genes. Activin receptors can activate various transcription factors, including Smad proteins, which bind to specific DNA sequences in the promoters of target genes, thereby regulating their transcription. The transcription of target genes, in turn, leads to changes in cellular processes, such as cell proliferation, differentiation, and apoptosis.
5. **Cellular Function Modulation:** The activation of activin receptors and downstream signaling pathways ultimately modulates a wide range of cellular functions. These functions include:
- **Cell Growth and Proliferation:** Activin receptors play a role in regulating cell growth and proliferation by controlling the expression of genes involved in cell cycle progression.
- **Cell Differentiation:** Activin receptors are involved in directing cells towards specific lineages, such as muscle cells, bone cells, or blood cells.
- **Development:** Activin signaling plays a crucial role in embryonic development, regulating organogenesis and tissue formation.
- **Apoptosis:** Activin receptors can trigger programmed cell death, known as apoptosis, which is a crucial process for maintaining tissue homeostasis.
6. **Feedback Regulation:** Activin signaling is subject to a complex network of feedback regulation. The activation of activin receptors can trigger the production of inhibitory proteins, such as follistatin and inhibin, which can bind to activin ligands and block their interaction with receptors. This feedback mechanism helps to maintain appropriate levels of activin signaling and prevent uncontrolled activation.'
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Protein | Definition | Taxonomy |
---|---|---|
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 |
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 |
bastadin 5 | |||
timcodar | timcodar: a mutlidrug resistance inhibitor; structure in first source |