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GlossaryEnzyme Inhibition

reduction or cessation of enzyme activity by specific molecules

Enzyme inhibition refers to the process by which the activity of an enzyme is reduced or stopped. This can occur through various mechanisms, such as competitive inhibition, where an inhibitor molecule competes with the substrate for the active site, or non-competitive inhibition, where the inhibitor binds to a different part of the enzyme, altering its shape and function. Understanding enzyme inhibition is crucial in fields like pharmacology and biochemistry, as it can influence drug design and metabolic regulation.

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research Determination of the potency of a novel saw palmetto supercritical CO2 extract (SPSE) for 5α-reductase isoform II inhibition using a cell-free in vitro test system

2 citations , April 2016 in “DOAJ (DOAJ: Directory of Open Access Journals)”

The saw palmetto extract effectively inhibits an enzyme linked to prostate issues, showing promise for prostate health.

research Potency of a novel saw palmetto ethanol extract, SPET-085, for inhibition of 5α-reductase II

46 citations , July 2010 in “Advances in Therapy”

SPET-085 effectively inhibits an enzyme linked to prostate issues, similar to finasteride.

research Determination of the potency of a novel saw palmetto supercritical CO2 extract (SPSE) for 5α-reductase isoform II inhibition using a cell-free in vitro test system

3 citations , April 2016 in “Research and reports in urology”

The new saw palmetto extract effectively inhibits an enzyme linked to prostate enlargement and may be as good as standard treatments.

research Recent Advances in the Chemistry and Pharmacological Activity of New Steroidal Antiandrogens and 5α-Reductase Inhibitors

20 citations , March 2005 in “Current Medicinal Chemistry”

New compounds show promise for treating hair loss, enlarged prostate, and prostate cancer, with some being more effective and having different side effects than current treatments.

Inhibition of Rat Alpha-Reductases by Finasteride: Evidence for Isozyme Differences in the Mechanism of Inhibition

research Inhibition of rat α-reductases by finasteride: Evidence for isozyme differences in the mechanism of inhibition

98 citations , April 1997 in “The Journal of Steroid Biochemistry and Molecular Biology”

Finasteride effectively blocks rat enzymes, but with varying methods and strength.

research 2-Substituted 4-(Thio)chromenone 6-O-Sulfamates: Potent Inhibitors of Human Steroid Sulfatase

111 citations , August 2002 in “Journal of Medicinal Chemistry”

New compounds were made that block an enzyme linked to breast cancer better than existing treatments.

research Pharmacological Inhibition of Stearoyl CoA Desaturase in the Skin Induces Atrophy of the Sebaceous Glands

25 citations , February 2013 in “The journal of investigative dermatology/Journal of investigative dermatology”

Blocking SCD1 in the skin with XEN103 shrinks sebaceous glands in mice.

research Enzyme Inhibitory Activities of Marine Sponges Against Cholinesterase and 5α-Reductase

June 2019

Marine sponges from Tabuhan Island can inhibit enzymes linked to Alzheimer's and hair loss.

In Vivo Time-Dependent Inhibition of Human Steroid 5α-Reductase by Finasteride

research In Vivo Time-Dependent Inhibition of Human Steroid 5a-Reductase by Finasteride

29 citations , January 1996 in “Journal of Pharmaceutical Sciences”

Finasteride poorly inhibits type 1 5AR, affecting its effectiveness.

research Mimosine Dipeptide Enantiomsers: Improved Inhibitors against Melanogenesis and Cyclooxygenase

25 citations , August 2015 in “Molecules”

Mimosine dipeptides are promising for treating hyperpigmentation and inflammation.

research Clinical Pharmacokinetics and Pharmacodynamics of Finasteride

93 citations , January 1996 in “Clinical Pharmacokinectics”

Finasteride helps regrow hair and shrink prostate by reducing DHT, with some sexual side effects.

research Effect of C-ring modifications in benzo[c]quinolizin-3-ones, new selective inhibitors of human 5α-reductase 1

12 citations , June 2001 in “Bioorganic & Medicinal Chemistry”

Changing the C-ring structure in certain compounds can make them better at blocking a specific human enzyme.

research Exploring the Inhibitory Potential of Phytosterols β-Sitosterol, Stigmasterol, and Campesterol on 5-Alpha Reductase Activity in the Human Prostate: An In Vitro and In Silico Approach

12 citations , November 2024 in “Plants”

Phytosterols may help manage prostate issues but are less effective than synthetic drugs.

research Design, synthesis and structure-activity relationships studies on steroidal aromatase and 5α-reductase inhibitors as anti-tumors

December 2013 in “Estudo Geral (Universidade de Coimbra)”

Modified steroidal inhibitors showed promise in treating hormone-dependent cancers.

research Modulating testosterone pathway: a new strategy to tackle male skin aging?

6 citations , September 2012 in “Clinical Interventions in Aging”

Honokiol might help reduce male skin aging by maintaining testosterone levels.

research Inhibition of steroid 5 alpha-reductase with finasteride: sleep-related erections, potency, and libido in healthy men.

15 citations , June 1995 in “The Journal of Clinical Endocrinology and Metabolism”

Finasteride doesn't affect erections much, but may decrease libido in men.

In Vitro Selective Inhibition of Human UDP-Glucuronosyltransferase (UGT) 1A4 by Finasteride and Prediction of In Vivo Drug–Drug Interactions

research In vitro selective inhibition of human UDP-glucuronosyltransferase (UGT) 1A4 by finasteride, and prediction of in vivo drug–drug interactions

13 citations , November 2014 in “Toxicology Letters”

Finasteride affects UGT1A4 enzyme, but not enough to cause issues when combined with other drugs.

Cloning, Expression, and Characterization of Rhesus Macaque Types 1 and 2 5alpha-Reductase: Evidence for Mechanism-Based Inhibition by Finasteride

research Cloning, expression and characterization of rhesus macaque types 1 and 2 5alpha-Reductase: evidence for mechanism-Based inhibition by finasteride

25 citations , September 1998 in “The Journal of Steroid Biochemistry and Molecular Biology”

Finasteride inhibits enzyme activity in rhesus macaques, suggesting they're useful for evaluating similar drugs.

research Pharmacological BACE1 and BACE2 inhibition induces hair depigmentation by inhibiting PMEL17 processing in mice

58 citations , February 2016 in “Scientific reports”

Blocking BACE1 and BACE2 enzymes causes hair color loss in mice.

research Inhibition of skin 5α-reductase by oral contraceptive progestinsin vitro

78 citations , January 2000 in “Gynecological Endocrinology”

Norgestimate is the most effective birth control progestin for reducing an enzyme linked to acne and excessive hair growth in women.

research 258 11β-hydroxysteroid dehydrogenase type 1 inhibition attenuates the adverse effects of glucocorticoids on dermal papilla cells

1 citations , September 2017 in “Journal of Investigative Dermatology”

Blocking a specific enzyme can reduce the negative impact of stress hormones on hair growth cells.

research Determination of rat 5α-reductase type 1 isozyme activity and its inhibition by novel steroidal oxazolines

4 citations , August 2010 in “Acta Biologica Hungarica”

New steroidal compounds moderately block an enzyme related to testosterone conversion, less effectively than finasteride.

research Steroid Sulfatase: Molecular Biology, Regulation, and Inhibition

451 citations , March 2005 in “Endocrine Reviews”

The enzyme steroid sulfatase is linked to breast cancer and other conditions, and inhibitors are being developed for treatment.

research Phospholipase A₂ inhibition as potential therapy for inflammatory skin diseases

13 citations , April 2013 in “Immunotherapy”

Inhibiting PLA2 enzymes may help treat inflammatory skin diseases like psoriasis and dermatitis.

Physiopathological Role of the Enzymatic Complex 5α-Reductase and 3α/β-Hydroxysteroid Oxidoreductase in the Generation of Progesterone and Testosterone Neuroactive Metabolites

research Physiopathological role of the enzymatic complex 5α-reductase and 3α/β-hydroxysteroid oxidoreductase in the generation of progesterone and testosterone neuroactive metabolites

18 citations , March 2020 in “Frontiers in Neuroendocrinology”

The enzymes 5α-reductase and 3α/β-hydroxysteroid oxidoreductase help create brain-active substances from progesterone and testosterone, which could be used for treatment, but more research is needed to ensure their safety and effectiveness.

research Inhibition of 17α-hydroxylase/C17,20 lyase reduces gating deficits consequent to dopaminergic activation

19 citations , September 2013 in “Psychoneuroendocrinology”

Blocking CYP17A1 enzyme may help improve certain brain function issues related to dopamine.

research Allopregnanolone is required for prepulse inhibition deficits induced by D1 dopamine receptor activation

12 citations , June 2019 in “Psychoneuroendocrinology”

Allopregnanolone is needed for certain brain processing issues caused by D1 dopamine receptor activation.

Chemical Mechanism of the Covalent Modification of 5-Alpha-Reductases by Finasteride as Probed by Secondary Tritium Isotope Effects

research Chemical Mechanism of the Covalent Modification of 5.alpha.-Reductases by Finasteride as Probed by Secondary Tritium Isotope Effects

12 citations , March 1995 in “Journal of the American Chemical Society”

Finasteride modifies 5-alpha-reductases through a two-step process, affecting inhibitor potency and possibly causing side effects.

research Anabolic effects of testosterone are preserved during inhibition of 5α-reductase

42 citations , May 2007 in “Endocrinology and metabolism/American journal of physiology: endocrinology and metabolism”

Testosterone can build muscle and bone without enlarging the prostate when a specific enzyme is blocked.

research Molecular interactions of natural and synthetic steroids in female hamsters’ flank organs

1 citations , March 2012 in “Journal of Dermatological Science”

Testosterone, progesterone, and levonorgestrel change enzyme levels related to fat production in hamster skin, which could affect skin oil and acne.