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  • Endocrinology-Hormones

Endocrinology-Hormones

Small molecules play a pivotal role in Endocrinology Research. These are low molecular weight compounds that have a significant impact on the endocrine system, hormones, and their receptors. Here are some key aspects of how small molecules are involved in this field:

  • Hormone Mimetics and Inhibitors: Small molecules are used to develop synthetic compounds that mimic the actions of hormones or inhibit their effects. For example, drugs like metformin for diabetes management and selective estrogen receptor modulators (SERMs) for breast cancer treatment are used to either mimic or block hormonal activity.
  • Receptor Modulation: Small molecules can bind to hormone receptors and modulate their activity. This is crucial in developing drugs that target specific hormone receptors, like the use of small molecule agonists and antagonists to regulate thyroid hormone receptors.
  • Metabolism Regulation: Endocrinology research often focuses on metabolism and how hormones like insulin regulate it. Small molecules are employed to understand and develop drugs targeting enzymes involved in metabolism, such as glucagon-like peptide-1 (GLP-1) agonists for diabetes treatment.
  • Steroid Hormone Production: Small molecules may be utilized to influence the production of steroid hormones in the adrenal glands or gonads. This is essential for conditions like Cushing's syndrome or polycystic ovary syndrome (PCOS).
  • Hormone Assays: In laboratory research, small molecules are used as tracers or markers in hormone assays. For instance, small molecule fluorophores can be attached to antibodies to detect hormone levels in blood samples.

Drug Development: Endocrinology research relies on small molecules as potential drug candidates. Researchers design and test small molecules for their effectiveness in modulating hormonal pathways, with the goal of developing new therapies for endocrine disorders.
In summary, small molecules are indispensable tools in Endocrinology Research, enabling scientists to better understand the endocrine system's intricacies and develop novel treatments for a wide range of hormonal disorders and conditions. Their versatility and specificity make them valuable assets in advancing our knowledge of endocrinology and improving patient care.

Endocrinology Disease Products

Diabetes Research

Endocrinology Research Products

Kisspeptin Receptor

Leptin Receptors

Melanocortin (MC) Receptors

Mineralocorticoid Receptors

Galanin Receptors

TRH Receptors

Ghrelin Receptors

Natriuretic Peptide Receptors

NPY Receptors

Motilin Receptor

PTH Receptor

Items 1-50 of 1754

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Citations
  1. A14896
    Parathyroid Hormone (1-34), bovine
    Parathyroid hormone (PTH) is the most important endocrine regulator of calcium and phosphorus concentration in extracellular fluid, which is secreted by the chief cell of the parathyroid glands as a polypeptide containing 84 amino acids.
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  2. A11860
    Fluticasone propionate
    Fluticasone propionate is a high affinity, selective glucocorticoid receptor agonist (Kd = 0.5 nM).
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  3. A10961
    Ursolic acid (Malol)
    Ursolic acid(Malol) is a pentacyclic triterpene acid, used in cosmetics, that is also capable of inhibiting various types of cancer cells by inhibiting the STAT3 activation pathway and human fibrosarcoma cells by reducing the expression of matrix metalloproteinase-9 by acting through the glucocorticoid receptor.
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  4. A10457
    Hydrocortisone(Cortisol)
    Hydrocortisone is a steroid hormone or glucocorticoid produced by the adrenal gland.
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  5. A10495
    Kaempferol

    ERRα and ERRγ inverse agonist

    Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.
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  6. A13252
    GANT61

    GLI antagonist

    GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.
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  7. A10905
    Telmisartan

    AT1 Antagonist

    Telmisartan is an angiotensin II receptor antagonist that inhibits the angiotensin II AT1 receptor.
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  8. A13201
    PD 123319 ditrifluoroacetate

    angiotensin AT2 receptor antagonist

    PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. IC50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.
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  9. A12769
    Zofenopril calcium

    ACE inhibitor

    Zofenopril calcium is an angiotensin-converting enzyme ACE inhibitor.
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  10. A10591
    Mifepristone (Mifeprex)
    Mifepristone, an antioxidant and glucocorticoid receptor antagonist, demonstrates the ability to suppress activation of NFκB, a nuclear transcription factor that affects the expression of various adhesion molecules and several inflammatory genes.
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  11. A11923
    Apalutamide (ARN-509)

    Androgen Receptor inhibitor

    ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.
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  12. A16986
    (R)-Equol

    Estrogen receptor agonist

    (R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
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  13. A14130
    Lonaprisan

    progesterone receptor antagonist

    Lonaprisan is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity.
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  14. A10563
    Megestrol Acetate
    Megestrol Acetate is a progesterone derivative with antineoplastic properties
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  15. A15860
    17-Hydroxyprogesterone

    Steroid Hormone

    17-Hydroxyprogesterone is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
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  16. A10439
    GSK1292263

    GPR119 agonist

    GSK-1292263 is a novel GPR119 agonist.
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  17. A11616
    Aliskiren (CGP 60536)

    Renin inhibitor

    Aliskiren is an orally active, synthetic nonpeptide renin inhibitor.
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  18. A16117
    Etonogestrel

    Progesterone/ERR Agonist

    Etonogestrel is a steroidal progestin used in hormonal contraceptives, most notably the subdermal implant Nexplanon and the vaginal ring NuvaRing.
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  19. A10529
    Levonorgestrel
    Levonorgestrelis a synthetic progesterone analog; binds to the progesterone receptor (relative binding affinities are < 0.02, 7.5, 17, 58 and 323 % for estrogen receptors, glucocorticoid receptors, mineralocorticoid receptors, androgen receptors and progesterone receptors respectively).
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  20. A10338
    Dutasteride (Avodart)

    dual 5alpha-reductase inhibitor

    Dutasteride is a dual 5-a reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT).
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  21. A12639
    Endoxifen (Z-isomer)

    Estrogen receptor antagonist

    Endoxifen is a secondary metabolite of tamoxifen. It is a primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.
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  22. A10791
    Rifampin

    RNA polymerase inhibitor

    Antibiotic; inhibits bacterial RNA polymerase. Prototypical activator of the pregnane X receptor (PXR).
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  23. A14873
    Angiotensin 1/2 (1-9)
    Angiotensin 1/2 (1-9) is a peptide (ASP-ARG-VAL-TYR-ILE-HIS-PRO-PHE-HIS) containing the amino acids 1-9 that are converted from Angiotensin I/II peptide.
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  24. A14887
    Angiotensin 1/2 (1-6)
    Angiotensin 1/2 (1-6) is a peptide that contains the amino acids 1-6 and is converted from Angiotensin I/II peptide.
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  25. A12376
    SR 144528

    CB2 inverse agonist

    SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.
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  26. A10142
    Bicalutamide (Casodex)

    Androgen Receptor antagonist

    Bicalutamide is an oral non-steroidal anti-androgen used in the treatment of prostate cancer and hirsutism.
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  27. A13740
    Zearalenone
    Zearalenone is a phytoestrogenic mycotoxin usually produced by Fusarium species, is shown to be a cytotoxic compound, but alos binds to the estrogen receptor (ER) (IC50 values are 166 and 240 nM for ERβ and ERα respectively) and was found to stimulate the transcriptional activity of both subtypes at concentrations between 1 - 10 nM.
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  28. A10175
    Candesartan (Atacand)

    RAAS antagonist

    Candesartan is an angiotensin receptor blocker (also called an angiotensin-II receptor antagonist or an AIIRA).
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  29. A12396
    AZD3514

    AR inhibitor downregulator

    AZD-3514 is a potent androgen receptor downregulator with potential anticancer cancer activity.
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  30. A10387
    Finasteride
    Finasteride is a synthetic type II 5α-reductase inhibitor. This enzyme converts testosterone to dihydrotestosterone (DHT).
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  31. A11665
    Bazedoxifene acetate
    Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene acetate significantly prevents bone mass loss at 20 mg/day in healthy postmenopausal women with normal or low bone mineral density.
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  32. A10375
    Evista (Raloxifene HCl)
    Raloxifene is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women.
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  33. A10885
    Tamoxifen Citrate

    Estrogen receptor antagonist

    Tamoxifen Citrateis a selective and potent inhibitor of mammalian sterol isomerase.
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  34. A11300
    Dimethylcurcumin (ASC-J9)
    ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
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  35. A16956
    GSK4716

    ERRβ & ERRγ Agonist

    GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ
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  36. A19383
    GSK5182

    ERRγ agonist

    GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.
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  37. A11088
    Fadrozole

    Aromatase inhibitor

    Fadrozole is a nonsteroidal aromatase inhibitor exhibiting a very potent and selective inhibitory effect of the aromatase enzyme system in vivo and estrogen biosynthesis in vivo.
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  38. A10299
    Dexamethasone

    glucocorticoid receptor agonist

    Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.
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  39. A13292
    Arzoxifene HCl
    Arzoxifene HCl is the hydrochloride salt of arzoxifene, a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist.
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  40. A12771
    Acolbifene (EM 652, SCH57068)

    estrogen receptor modulator

    acolbifene is a substance being studied in the prevention of breast cancer in women at high risk of breast cancer. Acolbifene hydrochloride binds to estrogen receptors in the body and blocks the effects of estrogen in the breast. It is a type of selective estrogen receptor modulator (SERM).
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  41. A15797
    Darolutamide (ODM-201)

    Androgen receptor antagonist

    ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.
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  42. A10562
    Enzalutamide (MDV3100)

    Androgen receptor antagonist

    MDV3100 is androgen-receptor inhibitor. Highly recommended inhibitor in AR research.
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  43. A11615
    Olmesartan medoxomil
    Olmesartan medoxomil is an angiotensin II receptor antagonist used to treat high blood pressure. Olmesartan works by blocking the binding of angiotensin II to the AT1 receptors in vascular muscle. By blocking the binding rather than the synthesis of angiotensin II, olmesartan inhibits the negative regulatory feedback on renin secretion.
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  44. A15451
    EXP-3174 (Losartan Carboxylic Acid)

    AT1 receptor antagonist

    EXP-3174 (Losartan Carboxylic Acid) is a potent and selective noncompetitive AT1 receptor antagonist with IC50 value of 37 nM.

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  45. A10670
    Olmesartan (RNH6270, CS-088)
    Olmesartan is an angiotensin II receptor antagonist indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.
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  46. A18250
    Taltirelin

    TRH-R agonist

    Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release).
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  47. A21041
    Ulipristal acetate

    progesterone receptor modulator

    Ulipristal (acetate) is a novel selective progesterone receptor modulator (SPRM) for the treatment of benign gynecological conditions such as uterine myoma.
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  48. A16364
    TC-G-1008

    GPR39 agonist

    TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).
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  49. A14862
    Talfirastide [Angiotensin (1-7)]
    Angiotensin (1-7) is an endogenous peptide fragment that can be produced from Ang I or Ang II via endo- or carboxy-peptidases respectively.
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  50. A10523
    Letrozole

    Aromatase inhibitor

    Letrozole is an Aromatase inhibitor. CGS 20267 is a new non-steroidal compound which potently inhibits aromatase in vitro (IC50 of 11.5 nM) and in vivo (ED50 of 1?€?3 μg/kg p.o.)
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