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.
NVP-BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and acute skin inflammation.
R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.
JI-101 is an orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRβ), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities.
TAK-593 is an oral formulation containing a small-molecule receptor tyrosine kinase inhibitor of both vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with potential antineoplastic activity.
AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
Altiratinib is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with a HGF antagonist in vitro.
Fruquintinib is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities.
E-3810 is a potent and selective dual inhibitor of VEGF and FGF receptors with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM and 82.5 nM for VEGFR-1, VEGFR-2, VEGFR-3, FGFR-1 and FGFR-2, respectively.
N-desethyl sunitinib is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively).
Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.
TG 100801 is the prodrug of TG 100572 (HY-10184), TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM or VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.
Toceranib phosphate is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ.
SU10944 is a small molecule kinase inhibitor of VEGFR that inhibits neovascularization and permeability, and is distributed to the eye upon systemic delivery.
EG00229 is the first small molecule inhibitors of the neuropilin-1 and VEGF-A interaction with an IC50 of inhibition of 8 uM(125I-VEGF binding to PAE/NRP1 cells).
Ningetinib Tosylate,also known as CT-053Tosylate and DE-120, is a VEGF and PDGF inhibitor potentially for the treatment of wet age-related macular degeneration. CAS: 1394820-69-9 (free base) 1394820-77-9 (tosylate)
Anlotinib, also known as AL3818, is a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. CAS: 1058156-90-3 (free base) 1360460-82-7 (HCl)
Sorafenib (Bay 43-9006) is a potent, orally active multikinase inhibitor with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
PTC299 is a potent, orally bioavailable VEGFA inhibitor, targets dihydroorotate dehydrogenase (DHODH), resulting in cell growth inhibition and differentiation in leukemias, including acute myeloid leukemia, linking DHODH regulation and stress-induced VEGFA and angiogenesis.
ODM-203 is a potent FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively.
R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.
Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively.