Page last updated: 2024-08-07 15:33:30
Renin
A renin that is encoded in the genome of human. [PRO:DNx, UniProtKB:P00797]
Synonyms
EC 3.4.23.15;
Angiotensinogenase
Research
Bioassay Publications (47)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 5 (10.64) | 18.7374 |
| 1990's | 10 (21.28) | 18.2507 |
| 2000's | 8 (17.02) | 29.6817 |
| 2010's | 22 (46.81) | 24.3611 |
| 2020's | 2 (4.26) | 2.80 |
Compounds (44)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 8-phenyltheophylline | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
| acetazolamide | Homo sapiens (human) | IC50 | 8.2000 | 1 | 1 |
| acetazolamide | Homo sapiens (human) | Ki | 3.3000 | 1 | 1 |
| theophylline | Homo sapiens (human) | Ki | 2.3250 | 1 | 2 |
| caffeine | Homo sapiens (human) | Ki | 15.0000 | 1 | 1 |
| furfurylamine | Homo sapiens (human) | IC50 | 300.0000 | 1 | 1 |
| 1-methyl-3-isobutylxanthine | Homo sapiens (human) | Ki | 2.7562 | 2 | 8 |
| nevirapine | Homo sapiens (human) | Ki | 7.0000 | 1 | 1 |
| rolipram | Homo sapiens (human) | IC50 | 3.5000 | 1 | 3 |
| pyrazolanthrone | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| 2-chloroadenosine | Homo sapiens (human) | Ki | 0.0100 | 1 | 1 |
| captopril | Homo sapiens (human) | Ki | 0.0017 | 1 | 1 |
| enalkiren | Homo sapiens (human) | IC50 | 0.0008 | 1 | 1 |
| toxoflavin | Homo sapiens (human) | IC50 | 0.9800 | 1 | 0 |
| 5-amino-1,3,4-thiadiazole-2-sulfonamide | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| 5-amino-1,3,4-thiadiazole-2-sulfonamide | Homo sapiens (human) | Ki | 7.4000 | 1 | 1 |
| phenylisopropyladenosine | Homo sapiens (human) | Ki | 0.0006 | 1 | 1 |
| h 142 | Homo sapiens (human) | IC50 | 0.0010 | 1 | 2 |
| cgp 38560a | Homo sapiens (human) | IC50 | 0.0013 | 3 | 4 |
| cgp 38560a | Homo sapiens (human) | Ki | 0.0007 | 1 | 1 |
| 1,6-dimethyl-3-(2-pyridinyl)pyrimido[5,4-e][1,2,4]triazine-5,7-dione | Homo sapiens (human) | IC50 | 1.2300 | 1 | 0 |
| 1-(3,4-dichlorophenyl)-3-(5-pyridin-4-yl-1,3,4-thiadiazol-2-yl)urea | Homo sapiens (human) | IC50 | 5.3000 | 1 | 0 |
| [1-(2-phenoxyethyl)-3-indolyl]-(1-pyrrolidinyl)methanethione | Homo sapiens (human) | IC50 | 3.9700 | 1 | 0 |
| 1,6-dimethyl-3-propylpyrimido[5,4-e][1,2,4]triazine-5,7-dione | Homo sapiens (human) | IC50 | 0.9800 | 1 | 0 |
| ellagic acid | Homo sapiens (human) | IC50 | 0.9800 | 1 | 0 |
| n-(1-methyl-2-phenylethyl)adenosine, (s)-isomer | Homo sapiens (human) | Ki | 0.0150 | 1 | 1 |
| ditekiren | Homo sapiens (human) | IC50 | 0.0003 | 1 | 1 |
| ditekiren | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| pepstatin | Homo sapiens (human) | IC50 | 44.4429 | 4 | 7 |
| pepstatin | Homo sapiens (human) | Ki | 6.5500 | 2 | 2 |
| norbinaltorphimine | Homo sapiens (human) | Ki | 0.0009 | 1 | 1 |
| aliskiren | Homo sapiens (human) | IC50 | 0.0010 | 23 | 23 |
| ro 42-5892 | Homo sapiens (human) | IC50 | 0.0000 | 1 | 2 |
| ro 42-5892 | Homo sapiens (human) | Ki | 0.0007 | 1 | 1 |
| tekturna | Homo sapiens (human) | IC50 | 0.0015 | 1 | 1 |
| (S)-2-amino-6-boronohexanoic acid | Homo sapiens (human) | IC50 | 1.4700 | 1 | 1 |
| n-cyclopropyl adenosine-5'-carboxamide | Homo sapiens (human) | Ki | 0.0055 | 1 | 1 |
| mk-8141 | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
| pf 877423 | Homo sapiens (human) | IC50 | 0.0041 | 1 | 1 |
| mk-1597 | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
| vtp-27999 | Homo sapiens (human) | IC50 | 0.0004 | 3 | 3 |
| gsk1482160 | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| 1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione | Homo sapiens (human) | Ki | 0.1590 | 1 | 1 |
| grassystatin a | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| lomofungin | Homo sapiens (human) | IC50 | 2.0600 | 1 | 0 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| angiotensin i, ile(5)- | Homo sapiens (human) | Km | 50.0000 | 1 | 1 |
| ly2811376 | Homo sapiens (human) | INH | 39.0000 | 1 | 1 |
Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.Chemistry & biology, , Volume: 7, Issue:7, 2000
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Non-peptide renin inhibitors containing 2-(((3-phenylpropyl)phosphoryl)oxy)alkanoic acid moieties as P2-P3 replacements.Journal of medicinal chemistry, , Feb-18, Volume: 37, Issue:4, 1994
Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
Novel inhibitors of human renin. Cyclic peptides based on the tetrapeptide sequence Glu-D-Phe-Lys-D-Trp.Journal of medicinal chemistry, , Volume: 33, Issue:9, 1990
Orally potent human renin inhibitors derived from angiotensinogen transition state: design, synthesis, and mode of interaction.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Novel renin inhibitors containing analogues of statine retro-inverted at the C-termini: specificity at the P2 histidine site.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine.Journal of medicinal chemistry, , Volume: 28, Issue:12, 1985
Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension.Journal of medicinal chemistry, , Volume: 24, Issue:4, 1981
Discovery of Novel 2-Carbamoyl Morpholine Derivatives as Highly Potent and Orally Active Direct Renin Inhibitors.ACS medicinal chemistry letters, , Aug-11, Volume: 13, Issue:8, 2022
Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Discovery of benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile.Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
Design, synthesis and biological evaluation of renin inhibitors guided by simulated annealing of chemical potential simulations.Bioorganic & medicinal chemistry, , 08-01, Volume: 25, Issue:15, 2017
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 25, Issue:7, 2015
Discovery of highly potent renin inhibitors potentially interacting with the S3' subsite of renin.European journal of medicinal chemistry, , Oct-20, Volume: 103, 2015
Dual inhibitors for aspartic proteases HIV-1 PR and renin: advancements in AIDS-hypertension-diabetes linkage via molecular dynamics, inhibition assays, and binding free energy calculations.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.ACS medicinal chemistry letters, , Oct-13, Volume: 2, Issue:10, 2011
Synthesis, biological evaluation and docking studies of octane-carboxamide based renin inhibitors with extended segments toward S3' site of renin.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Potential virtual lead identification in the discovery of renin inhibitors: application of ligand and structure-based pharmacophore modeling approaches.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Optimization of orally bioavailable alkyl amine renin inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 20, Issue:2, 2010
The P1N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Design and optimization of renin inhibitors: Orally bioavailable alkyl amines.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors.Journal of medicinal chemistry, , Jun-25, Volume: 52, Issue:12, 2009
Structural modification of the P2' position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.Chemistry & biology, , Volume: 7, Issue:7, 2000
Why Some Targets Benefit from beyond Rule of Five Drugs.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.Bioorganic & medicinal chemistry letters, , May-17, Volume: 9, Issue:10, 1999
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 25, Issue:7, 2015
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.ACS medicinal chemistry letters, , Oct-13, Volume: 2, Issue:10, 2011
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| aspartic-type endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a mechanism in which a water molecule bound by the side chains of aspartic residues at the active center acts as a nucleophile. [ISBN:0198506732] |
| signaling receptor binding | molecular function | Binding to one or more specific sites on a receptor molecule, a macromolecule that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:bf, GOC:ceb, ISBN:0198506732] |
| insulin-like growth factor receptor binding | molecular function | Binding to an insulin-like growth factor receptor. [GOC:jl] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| peptidase activity | molecular function | Catalysis of the hydrolysis of a peptide bond. A peptide bond is a covalent bond formed when the carbon atom from the carboxyl group of one amino acid shares electrons with the nitrogen atom from the amino group of a second amino acid. [GOC:jl, ISBN:0815332181] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| apical part of cell | cellular component | The region of a polarized cell that forms a tip or is distal to a base. For example, in a polarized epithelial cell, the apical region has an exposed surface and lies opposite to the basal lamina that separates the epithelium from other tissue. [GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
Involved In
This protein is involved in 18 target(s):
| Target | Category | Definition |
|---|
| kidney development | biological process | The process whose specific outcome is the progression of the kidney over time, from its formation to the mature structure. The kidney is an organ that filters the blood and/or excretes the end products of body metabolism in the form of urine. [GOC:dph, GOC:mtg_kidney_jan10, ISBN:0124020607, ISBN:0721662544] |
| mesonephros development | biological process | The process whose specific outcome is the progression of the mesonephros over time, from its formation to the mature structure. In mammals, the mesonephros is the second of the three embryonic kidneys to be established and exists only transiently. In lower vertebrates such as fish and amphibia, the mesonephros will form the mature kidney. [GOC:dph, ISBN:0124020607, ISBN:0721662544, PMID:10535314] |
| angiotensin maturation | biological process | The process leading to the attainment of the full functional capacity of angiotensin by conversion of angiotensinogen into mature angiotensin in the blood. [ISBN:0721643949] |
| renin-angiotensin regulation of aldosterone production | biological process | The process in which an increase in active angiotensin stimulates the adrenal cortices to secrete aldosterone. [ISBN:0721643949] |
| proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |
| regulation of blood pressure | biological process | Any process that modulates the force with which blood travels through the circulatory system. The process is controlled by a balance of processes that increase pressure and decrease pressure. [GOC:dph, GOC:mtg_cardio, ISBN:0721643949] |
| male gonad development | biological process | The process whose specific outcome is the progression of the male gonad over time, from its formation to the mature structure. [GOC:jid] |
| hormone-mediated signaling pathway | biological process | The series of molecular signals mediated by the detection of a hormone. [GOC:sm] |
| response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464] |
| response to immobilization stress | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of being rendered immobile. [GOC:bf, PMID:17683801, PMID:19893991] |
| drinking behavior | biological process | The specific behavior of an organism relating to the intake of liquids, especially water. [GOC:curators, GOC:pr] |
| regulation of MAPK cascade | biological process | Any process that modulates the frequency, rate or extent of signal transduction mediated by the MAP kinase (MAPK) cascade. [GOC:go_curators] |
| cell maturation | biological process | The cellular developmental process, independent of morphogenetic (shape) change, that is required for a specific cell to attain its fully functional state. [GOC:go_curators] |
| amyloid-beta metabolic process | biological process | The chemical reactions and pathways involving amyloid-beta, a glycoprotein associated with Alzheimer's disease, and its precursor, amyloid precursor protein (APP). [GOC:ai] |
| response to cAMP | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate) stimulus. [GOC:ai] |
| response to cGMP | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cGMP (cyclic GMP, guanosine 3',5'-cyclophosphate) stimulus. [GOC:sl] |
| cellular response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organism exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:krc, GOC:mah] |
| juxtaglomerular apparatus development | biological process | The process whose specific outcome is the progression of the juxtaglomerular apparatus over time, from its formation to the mature structure. The juxtaglomerular apparatus is an anatomical structure that lies adjacent to the glomerulus and regulates kidney function. [GOC:mtg_kidney_jan10] |