Page last updated: 2024-12-05

activins

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Activins: Activins are produced in the pituitary, gonads, and other tissues. By acting locally, they stimulate pituitary FSH secretion and have diverse effects on cell differentiation and embryonic development. Activins are glycoproteins that are hetero- or homodimers of INHIBIN-BETA SUBUNITS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4435
CHEMBL ID1357160
MeSH IDM0150466

Synonyms (25)

Synonym
nandroloni phenylpropionas
AC-12171
estr-4-en-3-one, 17-(1-oxo-3-phenylpropoxy)-, (17.beta.)-
activin
104625-48-1
3-oxoestr-4-en-17-yl 3-phenylpropanoate
durabol
(13-methyl-3-oxo-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-17-yl) 3-phenylpropanoate
activins
AKOS015960714
STL372833
BBL028862
CHEMBL1357160
estr-4-ene-3-one, 17-.beta.-hydroxy-, 3-phenylpropionate
4-androstene-17-beta-ol-3-one, 19-nor-delta-, phenylpropionate
17-.beta.-hydroxy-estra-4-en-3-one, 17-phenylpropionate
estr-4-en-3-one, 17.beta.-hydroxy-, hydrocinnamate
UBWXUGDQUBIEIZ-UHFFFAOYSA-N
17-.beta.-phenylpropionyloxy-4-estren-3-one
3-oxoestr-4-en-17-yl 3-phenylpropanoate, (17.beta.)- #
AC-32555
VS-08999
11a-methyl-7-oxo-1h,2h,3h,3ah,3bh,4h,5h,7h,8h,9h,9ah,9bh,10h,11h,11ah-cyclopenta[a]phenanthren-1-yl 3-phenylpropanoate
BCP09258
DTXSID60859051

Research Excerpts

Overview

Activins are dimeric in nature and consisting of two inhibin beta subunits linked via a disulfide bridge. Activins are a closely related subgroup within the TGFbeta superfamily of growth and differentiation factors.

ExcerptReferenceRelevance
"Activins are a subgroup of the TGFβ superfamily of growth and differentiation factors, dimeric in nature and consisting of two inhibin beta subunits linked via a disulfide bridge. "( Gastrointestinal pharmacology activins in liver health and disease.
Dai, G; Hamang, M; Yaden, B, 2023
)
2.64
"Activins are a closely related subgroup within the TGFbeta superfamily of growth and differentiation factors. "( The activin axis in liver biology and disease.
Berger, W; Bursch, W; Erlach, N; Grusch, M; Losert, A; Rodgarkia-Dara, C; Schulte-Hermann, R; Vejda, S,
)
1.57

Effects

Activins are implicated as important regulating factors for many reproductive processes. Activins have been shown to mediate their signals through type I and type II serine/threonine kinase receptors.

ExcerptReferenceRelevance
"Activins have been implicated as important regulating factors for many reproductive processes. "( Activin promotes oocyte development in ovine preantral follicles in vitro.
Armstrong, DG; Telfer, EE; Thomas, FH, 2003
)
1.76
"Activins have been shown to mediate their signals through type I and type II serine/threonine kinase receptors."( Transgenic models to study the roles of inhibins and activins in reproduction, oncogenesis, and development.
Behringer, RR; Coerver, KA; Finegold, MJ; Kumar, TR; Lau, AL; Matzuk, MM; Shou, W, 1996
)
1.26

Actions

Activins can cause stimulation of FSH release from pituitary cells. They are involved in embryogenesis, erythropoiesis, and reproductive function. Activins may tonically inhibit hepatocyte growth in the intact liver.

ExcerptReferenceRelevance
"As activins inhibit prolactin gene expression through the inhibition of Pit-1 involving the p38MAPK pathway, in the present work, we studied the local activin system as an alternative inhibitory system for lactotroph hyperplasia treatment."( Activin-inhibitory action on lactotrophs is decreased in lactotroph hyperplasia.
Abeledo Machado, AI; Camilletti, MA; Díaz-Torga, G; Faraoni, EY; Gutiérrez, S; Marcial López, CA; Peña-Zanoni, M; Pérez, PA; Rulli, SB, 2020
)
1.07
"Activins can cause stimulation of FSH release from pituitary cells both in vitro and in vivo, and in addition are involved in embryogenesis, erythropoiesis, and reproductive function."( Follistatins and alpha 2-macroglobulin are soluble binding proteins for inhibin and activin.
Mather, JP, 1996
)
1.02
"Activins may tonically inhibit hepatocyte growth in the intact liver."( The role of activin and transforming growth factor-beta in the regulation of organ mass in the rat liver.
Kogure, K; Kojima, I; Kuwano, H; Maeshima, A; Suzuki, K; Zhang, YQ, 2000
)
1.03

Pharmacokinetics

ExcerptReferenceRelevance
" In contrast, radiolabeled activin A-alpha 2M* complexes were rapidly cleared from plasma with a half-life of approximately 5 min and were specifically targeted to alpha 2M receptors in vivo."( Alpha 2-macroglobulin conformation determines binding affinity for activin A and plasma clearance of activin A/alpha 2-macroglobulin complex.
Gonias, SL; LaMarre, J; Niemuller, CA; Randall, KJ; Webb, DJ, 1995
)
0.29
" All these results show that we have generated enterocyte-like cells that have pharmacokinetic functions, and we have identified small-molecule compounds that are effective for promoting intestinal differentiation and the gain of pharmacokinetic functions."( Generation of enterocyte-like cells with pharmacokinetic functions from human induced pluripotent stem cells using small-molecule compounds.
Horikawa, T; Iwao, T; Kabeya, T; Kodama, N; Kondo, Y; Kurose, K; Matsunaga, T; Nakamura, K; Niwa, T, 2015
)
0.42
" With increasing doses of intravenous garetosmab, mean peak concentration increased in a dose-proportional manner; mean steady-state estimates ranged from 41."( Pharmacokinetics and Pharmacodynamics of Garetosmab (Anti-Activin A): Results From a First-in-Human Phase 1 Study.
Davis, JD; DelGizzi, R; Drewery, T; Forleo-Neto, E; Herman, G; Liang, S; Rajadhyaksha, M; Ruddy, M; Vanhoutte, F; Wang, Y; Zhao, A, 2020
)
0.56

Compound-Compound Interactions

ExcerptReferenceRelevance
"To observe the clinical curative effect of Wenshen Yangxue Granule (WSYXG) combined with clomifene citrate (CC) in treating follicular maldevelopment (FM) infertility, and to explore its possible action channels."( [Regulation and control of wenshen yangxue granule combined with clomifene citrate on INH-ACT-FS system in patients with follicular maldevelopment infertility].
Jun-qin, H; Ming-wei, X; Xin-yun, L, 2011
)
0.37
"WSYXG combined with CC could improve Chinese medicine syndrome, regulate the expressions of FM patients' ovary local factors INHB, ACTA and FS, improve the condition of ovary functions, and control the follicle development."( [Regulation and control of wenshen yangxue granule combined with clomifene citrate on INH-ACT-FS system in patients with follicular maldevelopment infertility].
Jun-qin, H; Ming-wei, X; Xin-yun, L, 2011
)
0.37
" Activin A in combination with OP9 cells augmented development of Flk-1(+) PDGFRα(+) early mesodermal cells and Flk-1(+) PDGFRα(-) lateral mesodermal cells from ES cells."( Activin A in combination with OP9 cells facilitates development of Flk-1(+) PDGFRα(-) and Flk-1(+) PDGFRα(+) hematopoietic mesodermal cells from murine embryonic stem cells.
Hirota, S; Ogawa, M, 2015
)
0.42
" Here, we show that Activin A also has an ability to efficiently propagate ESCs without differentiation to EpiSCs when combined with a MEK inhibitor PD0325901."( Activin A in combination with ERK1/2 MAPK pathway inhibition sustains propagation of mouse embryonic stem cells.
Ashida, Y; Hirota, A; Nakajima-Koyama, M; Nishida, E; Yamamoto, T, 2017
)
0.46

Bioavailability

ExcerptReferenceRelevance
" These results suggest that follistatin can modulate activin action in a cell-type specific fashion, and that this protein may play an important role in regulating the bioavailability of activin."( Follistatin modulates activin activity in a cell- and tissue-specific manner.
Krummen, LA; Mather, JP; Roberts, PE, 1993
)
0.29
" The bioavailability of the sc dose was 38%."( Pharmacokinetic profile of recombinant human (rh) inhibin A and activin A in the immature rat. I. Serum profile of rh-inhibin A and rh-activin A in the immature female rat.
Allison, DE; Baly, DL; Chen, S; DeGuzman, G; Garg, S; Hebert, N; Krummen, LA; Lyon, R; Wong, WL; Woodruff, TK, 1993
)
0.29
" Although these results support a possible endocrine role for circulating activin A during the human menstrual cycle and pregnancy, the observation that all detectable activin A is associated with binding protein(s) raises questions about its relative bioavailability for action on peripheral target cells."( Changes in peripheral serum levels of total activin A during the human menstrual cycle and pregnancy.
Fowler, PA; George, L; Groome, NP; Knight, PG; Muttukrishna, S, 1996
)
0.29
" This molecule may function primarily as a regulator of activin bioavailability and bioactivity."( Follistatins and alpha 2-macroglobulin are soluble binding proteins for inhibin and activin.
Mather, JP, 1996
)
0.29
"Follistatin (FS) is a monomeric protein that binds and regulates the bioavailability of activin."( A two-site chemiluminescent assay for activin-free follistatin reveals that most follistatin circulating in men and normal cycling women is in an activin-bound state.
Bolf, N; Crowley, WF; Khoury, RH; McConnell, DS; Midgley, AR; Padmanabhan, V; Reame, NE; Schneyer, AL; Sluss, PM; Wang, Q, 1998
)
0.3
"Follistatin is a specific binding protein which controls bioavailability of activins and inhibins which have an important role in fetal development."( Follistatin and activin A in extra-embryonic coelomic and amniotic fluids and maternal serum in early pregnancy.
Balfour, C; Chard, T; Evans, LW; Groome, NP; Riley, SC; Wallace, EM; Wathen, NC, 1998
)
0.53
" We hypothesized that cell surface FS would differentially regulate the bioavailability of endogenous and exogenous activin in these cells."( Differential response to exogenous and endogenous activin in a human ovarian teratocarcinoma-derived cell line (PA-1): regulation by cell surface follistatin.
Delbaere, A; Schneyer, AL; Sidis, Y, 1999
)
0.3
" This is in line with the suggested role of follistatin as an activin-binding protein, which limits the bioavailability of activin to its membrane receptors."( Activin-A, but not inhibin, regulates 17beta-hydroxysteroid dehydrogenase type 1 activity and expression in cultured rat granulosa cells.
Akinola, L; Ghersevich, S; Isomaa, V; Kaminski, T; Poutanen, M; Vihko, P; Vihko, R,
)
0.13
" The purpose of this investigation was three fold: (i) to indirectly assess the bioavailability of GSPE in multiple target organs, (ii) quantify GSPE's capacity to avert cadmium chloride (CdCl2)-induced nephrotoxicity, dimethylnitrosamine (DMN)-induced splenotoxicity and O-ethyl-S,S-dipropyl phosphorodithioate (MOCAP)-induced neurotoxicity, and lastly (iii) to evaluate possible mechanisms of protection in mice."( Unique organoprotective properties of a novel IH636 grape seed proanthocyanidin extract on cadmium chloride-induced nephrotoxicity, dimethylnitrosamine (DMN)-induced splenotoxicity and mocap-induced neurotoxicity in mice.
Bagchi, D; Bagchi, M; Raje, RR; Ray, SD; Rinkovsky, A; Wong, V, 2000
)
0.31
" Activin bioavailability is locally regulated by its binding protein, follistatin, and also by the antagonist, inhibin."( Expression of activin receptors, follistatin and betaglycan by human endometrial stromal cells; consistent with a role for activins during decidualization.
Drummond, AE; Ethier, JF; Findlay, JK; Jones, RL; Salamonsen, LA; Zhao, YC, 2002
)
0.52
" We administered follistatin, the high-affinity binding protein for activin, to five ovariectomized sheep; we reasoned that the resultant binding of follistatin to activin should lower activin bioavailability and FSH secretion."( Neuroendocrine control of follicle-stimulating hormone (FSH) secretion: II. Is follistatin-induced suppression of FSH secretion mediated via changes in activin availability and does it involve changes in gonadotropin-releasing hormone secretion?
Battaglia, D; Brown, MB; Karsch, FJ; Lee, JS; Padmanabhan, V; Pan, W; Phillips, DJ; Van Cleeff, J, 2002
)
0.31
" It also represents a prototype for binding proteins that control bioavailability of other TGFbeta-related growth factors such as the bone morphogenetic proteins."( The role of follistatin domains in follistatin biological action.
Keutmann, HT; Schneyer, AL; Sidis, Y, 2004
)
0.32
" We demonstrate that high concentrations of activin A are produced by decidualising cells in excess of the antagonists, inhibin and follistatin, thus confirming its bioavailability within the decidual environment."( The role of activins during decidualisation of human endometrium.
Findlay, JK; Jones, RL; Salamonsen, LA, 2006
)
0.71
" Taken together, these results suggest that the bioavailability of the TGFbeta-specific receptor rather than TGFbeta dictates pituitary gonadotrope selectivity to activin, which is necessary to maintain normal reproductive function."( Cell-specificity of transforming growth factor-beta response is dictated by receptor bioavailability.
Suszko, MI; Woodruff, TK, 2006
)
0.33
" Using an orally bioavailable inhibitor of the Activin A pathway to attenuate oral cancer cell migration and invasion, we further demonstrate the targetability of this signaling axis."( ΔNp63 overexpression promotes oral cancer cell migration through hyperactivated Activin A signaling.
Basu, S; Dalal, S; Kumar, S; Mishra, R; Mundhe, D; Teni, T, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
" With the addition of FSP, an apparent increase in the ED50 of the activin dose-response curves was observed, but there were no changes in the maximum response."( Interaction between activin and follicle-stimulating hormone-suppressing protein/follistatin in the regulation of basal inhibin production by cultured rat granulosa cells.
Farnworth, PG; Findlay, JK; Xiao, S, 1992
)
0.28
" We found 1) that the two responses to activin A/EDF were distinctly affected by the initial cell density; 2) that the dose-response curves for activin A/EDF were similar (ED50 = approximately 100 pM), whereas the time course of induction of TXA2 synthetic activity was much faster; and 3) that other erythroid differentiation inducers of MEL cells, namely dimethyl sulfoxide and hexamethylene bisacetamide, had little or no effect on TXA2 synthesis."( Activin A/erythroid differentiation factor induces thromboxane A2 synthetic activity in murine erythroleukemia cells.
Ogata, E; Shimizu, T; Yamashita, T, 1991
)
0.28
" The dose-response curves of porcine follicular fluid and ovarian extract were parallel to the standard curve, and porcine follicular fluid contained high activin A/EDF immunoreactivity (1050 ng/ml)."( Radioimmunoassay for activin A/EDF. Method and measurement of immunoreactive activin A/EDF levels in various biological materials.
Saito, S; Shintani, Y; Takada, Y; Yamasaki, R, 1991
)
0.28
" The dose-response relationship and time course study indicated that PDGF-mediated release of activin correlated with initiation of DNA synthesis."( Production of activin A and follistatin in cultured rat vascular smooth muscle cells.
Kanzaki, M; Kawamura, N; Kojima, I; Mogami, H; Nobusawa, R; Yasuda, H, 1995
)
0.29
" We show that initial dose-response profiles are broad and smooth in contrast to the later threshold-bound patterns."( Slow emergence of a multithreshold response to activin requires cell-contact-dependent sharpening but not prepattern.
Gerhart, JC; Green, JB; Smith, JC, 1994
)
0.29
" Dose-response relationship for EGF-induced follistatin release correlated well with that for EGF-induced DNA synthesis."( Stimulation of follistatin production by epidermal growth factor in cultured rat hepatocytes.
Kanzaki, M; Kojima, I; Mine, T; Zhang, YQ, 1994
)
0.29
" The dose-response relationship for the activin A-mediated reduction of DAG mass correlated well with th at for the activin A-mediated reduction of DNA synthesis."( Activin A inhibits cell-cycle progression induced by insulin-like growth factor-I in Balb/c 3T3 cells.
Kawamura, N; Kojima, I; Mogami, H; Shibata, H, 1993
)
0.29
" The dose-response curves of porcine follicular and amniotic fluids were parallel to the standard curve, and porcine follicular fluid contained extremely high follistatin immunoreactivity (5."( Immunoradiometric assay for follistatin: serum immunoreactive follistatin levels in normal adults and pregnant women.
Abe, M; Liu, ZH; Saito, S; Shintani, Y; Shitsukawa, K; Wakatsuki, M, 1996
)
0.29
"4-fold) and with similar dose-response and time-course profiles as the mRNA levels."( Transcriptional activation of the gonadotropin-releasing hormone receptor gene by activin A.
Albarracin, CT; Chin, WW; Fernández-Vázquez, G; Kaiser, UB, 1996
)
0.29
" This characteristic bell-shaped dose-response curve was maintained in the presence of TGF-beta (10 ng/ml) or a maximally-effective dose of forskolin (6."( Activin-A stimulates, while transforming growth factor beta 1 inhibits, chorionic gonadotrophin production and aromatase activity in cultured human placental trophoblasts.
France, JT; Keelan, J; Song, Y, 1996
)
0.29
" As a result of this extraction procedure, the dose-response curve of serum extract was parallel to the standard curve and a single immunoreactive (ir-) peak was demonstrated on gel chromatographic analysis with constant recovery rates over 80%."( Serum immunoreactive activin A levels in normal subjects and patients with various diseases.
Harada, K; Saito, S; Sakamoto, Y; Shintani, Y; Shitsukawa, K; Wakatsuki, M, 1996
)
0.29
" Dose-response analysis revealed monophasic dose dependence (half maximal inhibitory doses of 16."( Activin-attenuated expression of transcripts encoding granulosa cell-derived insulin-like growth factor binding proteins 4 and 5 in the rat: a putative antiatretic effect.
Adashi, EY; Choi, D; Gargosky, SE; Matsumoto, T; Rohan, RM; Rosenfeld, RG, 1997
)
0.3
" Although the craniofacial phenotypes of the Inhba-null mutation were rescued by the InhbaBK allele, somatic, testicular, genital and hair growth were grossly affected and influenced by the dosage and bioactivity of the allele."( Insertion of Inhbb into the Inhba locus rescues the Inhba-null phenotype and reveals new activin functions.
Brown, CW; Houston-Hawkins, DE; Matzuk, MM; Woodruff, TK, 2000
)
0.31
"87-fold increase in colony numbers and a bell-shaped dose-response curve."( EDR is a stress-related survival factor from stroma and other tissues acting on early haematopoietic progenitors (E-Mix).
Dörmer, P; Möller, W; Spitzer, E,
)
0.13
" Significant differences in Smad and cell cycle regulator transcript levels correlating to Inhba gene dosage correspond to differences in Sertoli and germ cell numbers."( Activin A balances Sertoli and germ cell proliferation in the fetal mouse testis.
Loveland, KL; Meachem, SJ; Mendis, SH; Sarraj, MA, 2011
)
0.37
" The present article is aimed at investigating the role of dosage biochemical markers in non-invasive biological fluids such as S100B, a calcium binding protein, activin A, a protein expressed in Central nervous System (CNS)."( [Markers of brain injury in non-invasive biological fluids].
Bellissima, V; Colivicchi, M; Crivelli, S; Gazzolo, D; Guerriero, F; Moresco, L; Ricotti, A; Sabatini, M; Strozzi, MC; Temporini, F, 2010
)
0.36
" The importance of activin bioactivity levels or dosage in controlling balanced growth of spermatogonial cells and their niche at different stages of testis development is highlighted."( Activins and inhibins in mammalian testis development: new models, new insights.
Barakat, B; Itman, C; Loveland, KL; Mendis, SH, 2012
)
1.82
" Although palovarotene inhibited chondrogenic differentiation in vitro and reduced HO in juvenile FOP mice, daily dosing resulted in aggressive synovial joint overgrowth and long bone growth plate ablation."( Palovarotene reduces heterotopic ossification in juvenile FOP mice but exhibits pronounced skeletal toxicity.
Devarakonda, PM; Goldhamer, DJ; Lees-Shepard, JB; Nicholas, SE; Schneider, MJ; Stoessel, SJ; Yamamoto, M, 2018
)
0.48
" In the mdx model, engineered follistatin was dosed for 12 weeks in two studies comparing to an Fc fusion of the activin IIB receptor or an anti-myostatin antibody."( Myostatin and activin blockade by engineered follistatin results in hypertrophy and improves dystrophic pathology in mdx mouse more than myostatin blockade alone.
Comeau, R; Crooker, R; Deng, Q; Derakhchan, K; Dumas, J; Ehmann, DE; Huang, Y; Iskenderian, A; Kastrapeli, N; Liu, N; Lundberg, D; Norton, A; Palmieri, K; Pan, J; Pescatore, B; Romashko, A; Rong, H; Shen, C, 2018
)
0.48
" Excluding the lowest dosage (1 mg/kg) provided similar results (12 m [SE 5], P = 0."( Blocking the activin IIB receptor with bimagrumab (BYM338) increases walking performance: A meta-analysis.
Abe, T; Bell, ZW; Dankel, SJ; Kang, M; Loenneke, JP; Spitz, RW; Wong, V, 2021
)
0.62
" A particular emphasis is given to the relationship between sotatercept dosage and its efficacy or associated adverse reactions."( From bench to bedside: The promise of sotatercept in hematologic disorders.
Lan, Z; Lv, Z; Xiao, Y; Zuo, W, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,840)

TimeframeStudies, This Drug (%)All Drugs %
pre-199050 (1.30)18.7374
1990's1066 (27.76)18.2507
2000's1278 (33.28)29.6817
2010's1144 (29.79)24.3611
2020's302 (7.86)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 55.30

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index55.30 (24.57)
Research Supply Index8.29 (2.92)
Research Growth Index6.11 (4.65)
Search Engine Demand Index94.94 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (55.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials47 (1.20%)5.53%
Reviews500 (12.75%)6.00%
Case Studies11 (0.28%)4.05%
Observational5 (0.13%)0.25%
Other3,359 (85.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]