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estradiol (E2III)

✓ Approved

Johnson & Johnson Services, Inc. · ESR1 · Small Molecule

What is estradiol?

estradiol is a small molecule developed by Johnson & Johnson Services, Inc.. It is approved for therapeutic indications via transdermal.

Drug Profile

Brand NamesE2III
CompanyJohnson & Johnson Services, Inc.
Drug ClassSmall Molecule
Molecular TargetESR1
RouteTransdermal
StatusApproved

Mechanism of Action

Molecular Targets

estradiol acts on 1 molecular target:

ESR1estrogen receptor 1 (ER, ESR)
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Therapeutic Indications

estradiol is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Surgical and medical proceduresHormone replacement therapy✓ Approved

Related Research Articles

PubMedRSC advances2026-11-11

Upcycling recycled PET into a conductive electrode for a molecularly imprinted polymer based electrochemical sensor for 17β-estradiol detection.

Tahir Muhammad Faran MF, Yimyai Tiwa T, D'Haen Jan J, Thoelen Ronald R et al.

The upcycling of plastic waste into advanced materials has emerged as a promising strategy across various technologies, including the development of next-generation sensors. This sustainable approach promotes green technological development. In this work, we transformed recycled polyethylene terephthalate (rPET) into a functional conductive electrode substrate for a molecularly imprinted polymer (MIP) based electrochemical sensor for the detection of 17β-estradiol (E2). The latter also serves as a relevant model compound as a pollutant to study the sensor's applicability in complex matrices. The MIP-based sensor was fabricated by the electropolymerization of an o-phenylenediamine (o-PD) monomer in the presence of E2 template molecules and gold(iii) chloride trihydrate onto gold-coated rPET substrates. The physical properties of MIP films were characterized by scanning electron microscopy (SEM), atomic force microscopy, contact angle measurement, cyclic voltammetry, and electrochemical impedance spectroscopy. The binding of E2 molecules to the MIP surface hindered electron transfer of the redox probes, resulting in a concentration-dependent suppression of the electrochemical current measured by square wave voltammetry. The sensor showed high affinity for E2 molecules with a dissociation constant (K d) of 11.2 nM over a linear detection range of E2 concentrations (0.5-500 nM), and a limit of detection (LOD) of 0.18 and 0.41 nM in PBS and in wastewater samples without any complex pretreatment steps, respectively. This developed MIP-based sensor demonstrated the potential of alternative sensors for real-world environmental monitoring of trace endocrine disruptors, while successfully converting rPET into valuable technological products offers a practical roadmap to accelerate the development of sustainable and circular electronics.

PubMedAnalytical chemistry2026-11-11

A Versatile Aza-BODIPY-Based Activatable Probe for High-Contrast NIR-II Biosensing.

Yao Chenzhi C, Huang Liwen L, He Qian Q, Guo Jiahao J et al.

Activatable molecular probes in the second near-infrared (NIR-II, 900-1700 nm) window are sought-after for in vivo optical imaging and biosensing. However, current molecular skeletons are confined to a limited range of dye systems, including cyanine, hemicyanine, and xanthene derivatives. Herein, we report a series of ortho-halogenated phenol-conjugated aza boron dipyrromethene platforms (OBDP-xOH, where X = H, F, Cl, Br, or 2Cl) that achieve bright NIR-II emission through a pH-regulated intramolecular charge transfer mechanism. The optimized scaffold, OBDP-2ClOH (pKa = 6.1), concurrently demonstrates the NIR-II emission maximum at approximately 905 nm, a large Stokes shift of 117 nm, high NIR-II brightness (εmaxΦf>1000 nm ≈ 38.46 M-1 cm-1), and excellent photochemical stability. To validate the broad applicability of this platform, we further designed three target-activatable NIR-II nanoprobes responsive to UV light, H2S, and Cu2+, respectively. Each nanoprobe exhibited a high fluorescence turn-on ratio exceeding 29-fold and limits of detection below 10.3 nM. Leveraging these probes, we achieved rapid (<30 min) dynamic imaging of labile Cu2+ in the brains of Parkinson's disease models, as well as high-fidelity in vivo early detection of acute liver injury within 5 min, which is substantially faster than conventional clinical serum analysis that requires approximately 90 min. Collectively, these findings underscore the translational potential of the OBDP-2ClOH scaffold as a versatile and generalizable platform for the development of advanced activatable NIR-II probes.

PubMedChemical science2026-11-11

Azobenzene-mediated reversible conformational switching in 9,9'-bifluorenylidene-based molecular machines.

Mahajan Sohail S, Rich Reese R, Jiao Lin L, Zhang Duhan D et al.

Intrinsically dynamic molecules offer attractive building blocks for molecular machines, yet controlling their conformational motion with external stimuli remains a fundamental challenge. Here, we report Azo-BF-Azo, a visible-light-driven molecular machine in which an intrinsically dynamic 9,9'-bifluorenylidene (BF) core is coupled to two photoswitchable tetra-ortho-fluorinated azobenzene (Azo) units that act as molecular actuators. By using variable-temperature NMR spectroscopy and UV-vis spectroscopy, together with computational studies, we demonstrate that irradiation at 525 nm induces Azo trans-cis photoisomerization and shifts the BF conformational equilibrium from the closed toward the open state, whereas 456 nm irradiation reverses Azo isomerization and promotes recovery of the BF-closed state. DFT calculations reveal that the extended trans-Azo units favor intramolecular π-π interactions that stabilize the closed BF conformation, while their conversion to the folded cis state disrupts these interactions and alters the steric environment surrounding the BF core. Variable-temperature NMR spectroscopy provides experimental support for the role of these intramolecular interactions in regulating the BF conformational equilibrium. The photoinduced metastable state further undergoes spontaneous thermal relaxation in the dark, recovering approximately 65% of the initial state. Together, these results demonstrate that local photoisomerization can reshape the conformational energy landscape of a second, intrinsically dynamic molecular degree of freedom through switchable noncovalent interactions. This work provides a strategy for converting intrinsic molecular dynamics into externally programmable motion and establishes a design principle for constructing integrated molecular machines in which one type of molecular motion regulates another.

PubMedAnalytical chemistry2026-11-11

Soft Wearable Aptamer Wristband Enables Real-Time Sweat Dual-Hormone Monitoring for Menstrual Cycle Tracking.

Liu Jiaqi J, Yang Yuyang Y, Dong Renfeng R, Xu Tailin T

Noninvasive and longitudinal monitoring of female reproductive hormones could provide valuable information on individualized endocrine dynamics across the menstrual cycle. Here, we developed an integrated wearable electrochemical platform for simultaneous monitoring of estradiol (E2) and progesterone (P4), together with sweat pH and ionic strength. Competitive-displacement aptamer sensing interfaces were constructed for dual-hormone detection, while a Tesla-valve microfluidic network supported passive sweat transport and sequential sample replacement. A flexible wireless electronic system provided multiplexed signal acquisition and wireless data transmission. To improve quantitative reliability under variable sweat conditions, pH-dependent calibration was incorporated into hormone analysis. The platform was evaluated in two volunteers over approximately one complete menstrual cycle, and the longitudinal E2 and P4 profiles obtained by the wearable sensors showed similar temporal trends to those obtained by paired sweat enzyme-linked immunosorbent assay (ELISA) measurements. pH compensation further improved the correlation between sensor and ELISA measurements of hormone concentrations. These results demonstrate the feasibility of integrating dual-hormone sensing, pH-dependent calibration, microfluidic sweat management, and wireless electronics into a wearable platform for longitudinal monitoring of reproductive hormone dynamics.

PubMedTranslational psychiatry2026-11-11

Disruption of the Non-classical ERα-PCYT1A-Phospholipid-NR5A2 Axis impairs kisspeptin signaling in hypothalamic KNDy neurons and drives postpartum depression.

Yang Juanjuan J, Shen Yifen Y, Zhang Jiayi J, Chen Xuan X et al.

Postpartum depression (PPD) is a common neuroendocrine disorder associated with the rapid decline in estrogen levels following childbirth. However, the precise molecular mechanisms through which estrogen withdrawal disrupts hypothalamic signaling, particularly in key reproductive neurons, remain poorly understood. To investigate this, we developed an in vitro PPD-like model using primary embryonic hypothalamic Kisspeptin/Neurokinin B/Dynorphin (KNDy) neurons subjected to estradiol (E2) exposure and subsequent withdrawal. Multi-omics analyses, including proteomics, lipidomics, and transcriptomics, were integrated with functional studies. We discovered that the transcription factor NR5A2 is critical for initiating Kisspeptin rebound after short-term E2 withdrawal by directly binding to the Kiss1 promoter. However, under prolonged withdrawal conditions, this recovery fails. This failure is driven by a disruption in neuronal phospholipid metabolism, characterized by the downregulation of the rate-limiting enzyme PCYT1A and a consequent reduction in specific phosphatidylcholines, PC(32:1) and LPC(24:0), which we identified as crucial stabilizers of NR5A2 activity. Further mechanistic analysis revealed that prolonged E2 withdrawal impairs non-classical Estrogen Receptor α (ncERα) signaling, which upstream regulates PCYT1A expression. Reactivating this ncERα pathway restored phospholipid synthesis and NR5A2-mediated Kisspeptin expression. The entire ncERα-PCYT1A-phospholipid-NR5A2-Kiss1 axis was validated in an in vivo rat model of PPD, where direct intracerebroventricular administration of phospholipids successfully alleviated depressive-like behaviors. Our study defines a novel signaling cascade that links estrogen dynamics with neuronal lipid metabolism to control postpartum neuroendocrine recovery, offering fresh mechanistic and therapeutic insights into PPD.

PubMedAMB Express2026-11-11

HSD17B8 axis modulates Pseudomonas aeruginosa-associated lung inflammatory injury in bronchiectasis.

Zheng Shaochu S, Bao Chongxi C, Tang Jinling J, Hong Kangkang K et al.

Non-cystic fibrosis bronchiectasis (NCFB) is characterized by persistent Pseudomonas aeruginosa (P. aeruginosa) colonization and uncontrolled pulmonary inflammation, while the underlying metabolic regulatory mechanism remains poorly understood. This study aimed to explore the potential analyze correlations of the HSD17B8 metabolic axis in lung inflammatory injury related to P. aeruginosa in NCFB. Transcriptome sequencing was performed on peripheral blood and tissue samples from NCFB patients and healthy controls to screen differentially expressed genes. Two-sample Mendelian randomization integrated with protein quantitative trait locus data was applied to evaluate the potential association between candidate genes and NCFB susceptibility. The expression of HSD17B8 in clinical samples was further validated by RT-qPCR. Meanwhile, a rat model of P. aeruginosa-infected pulmonary inflammation was established to investigate the influences of estrone intervention on lung pathology, pro-inflammatory cytokines (IL1β, IL6), and steroid metabolite homeostasis. A total of 249 overlapping differentially expressed genes were identified. Mendelian randomization analysis indicated that downregulated HSD17B8 expression was nominally correlated with elevated NCFB risk (OR 0.76, 95% CI 0.60-0.95, P = 0.0159). Clinically, HSD17B8 was significantly decreased in NCFB patients and correlated with higher E-FACED severity scores. In the P. aeruginosa-related rat model, reduced HSD17B8 expression disturbed estradiol/estrone balance, increased IL1β and IL6 levels, and aggravated lung pathological lesions. Exogenous estrone was correlated with dose-dependent alleviation of inflammatory lesions via inhibiting inflammatory response and restoring metabolic homeostasis. Collectively, HSD17B8 is potentially involved in the progression of P. aeruginosa-associated NCFB. Altered HSD17B8 expression is associated with disturbed steroid balance and aggravated inflammatory responses related to microbial infection. Targeting HSD17B8 and its downstream steroid metabolites may offer a promising metabolic intervention strategy for P. aeruginosa-associated infectious bronchiectasis.

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