Delving into the Latest Updates on Celastrol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Tripterin, celastrol

Target

CDC37 x COMMD3 x COMMD8 x HSP90 x LEPR x SHP2 x TEAD x YAP1

Mechanism

CDC37 antagonists(cell division cycle 37, HSP90 cochaperone antagonists), COMMD3 inhibitors(COMM domain containing 3 inhibitors), COMMD8 inhibitors(COMM domain containing 8 inhibitors)

+ [5]

Therapeutic Areas

NeoplasmsImmune System DiseasesInfectious Diseases+ [5]

Active Indication

Fractures, BonePrader-Willi SyndromeAutoimmune Diseases+ [2]

Inactive Indication

Diabetes MellitusNonalcoholic SteatohepatitisPancreatic Cancer

Originator Organization

The Ohio State University

Active Organization

Osaka UniversityERX Pharmaceuticals Inc

H. Lee Moffitt Cancer Center & Research Institute, Inc.

+ [3]

Inactive Organization

Harvard Medical School

The Ohio State University

Drug Highest PhasePhase 2/3

First Approval Date-

RegulationOrphan Drug (US)

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Structure

Molecular FormulaC29H38O4

InChIKeyKQJSQWZMSAGSHN-JJWQIEBTSA-N

CAS Registry34157-83-0

This is an open label safety study that will not be blinded or placebo controlled.
Purpose is to evaluate the safety of Celastrol in healthy men and women volunteers, between 18 and 40 years of age, over a 90-day period.
Celastrol is different than Cholesterol. Cholesterol is a risk for heart disease. Celastrol is a natural occurring compound extracted from the root of Tripterygium wilfordii, a herb used in Chinese medicine.

Start Date25 May 2022

Sponsor / Collaborator

LEGEND LABZ, INC.

NCT05413226 / RecruitingNot Applicable

Effect of Different Ingestion Doses of Celastrol on Human Sperm Motility

Five healthy participants with normal sperm counts and motility will ingest increasing doses of celastrol over a period of several days. After each dose ingestion the participants will provide an ejaculate the next day for sperm analysis. The objective is to see if increasing ingestion levels of celastrol will affect the sperm counts and motility of the participants.

Start Date28 Sep 2021

Sponsor / Collaborator

LEGEND LABZ, INC.

100 Clinical Results associated with Celastrol

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100 Translational Medicine associated with Celastrol

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100 Patents (Medical) associated with Celastrol

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1,180

Literatures (Medical) associated with Celastrol

01 Jan 2025·Biomaterials

Orchestrated metal-coordinated carrier-free celastrol hydrogel intensifies T cell activation and regulates response to immune checkpoint blockade for synergistic chemo-immunotherapy

Article

Author: Tan, Xinru ; Yao, Shuchang ; Wu, Linying ; Wang, Zhixia ; Zhang, Xiang ; Huang, Xuemei ; Pi, Wenmin ; Lu, Jihui ; Lin, Xiaoyu ; Yang, Luping ; Wang, Penglong

The challenges generated by insufficient T cell activation and infiltration have constrained the application of immunotherapy. Making matters worse, the complex tumor microenvironment (TME), resistance to apoptosis collectively poses obstacles for cancer treatment. The carrier-free small molecular self-assembly strategy is a current research hotspot to overcome these challenges. This strategy can transform multiple functional agents into sustain-released hydrogel without the addition of any excipients. Herein, a coordination and hydrogen bond mediated tricomponent hydrogel (Cel hydrogel) composed of glycyrrhizic acid (GA), copper ions (Cu²⁺) and celastrol (Cel) was initially constructed. The hydrogel can regulate TME by chemo-dynamic therapy (CDT), which increases reactive oxygen species (ROS) in conjunction with GA and Cel, synergistically expediting cellular apoptosis. What's more, copper induced cuproptosis also contributes to the anti-tumor effect. In terms of regulating immunity, ROS generated by Cel hydrogel can polarize tumor-associated macrophages (TAMs) into M1-TAMs, Cel can induce T cell proliferation as well as activate DC mediated antigen presentation, which subsequently induce T cell proliferation, elevate T cell infiltration and enhance the specific killing of tumor cells, along with the upregulation of PD-L1 expression. Upon co-administration with aPD-L1, this synergy mitigated both primary and metastasis tumors, showing promising clinical translational value.

31 Dec 2024·Drug Delivery

Advances in cell membrane-based biomimetic nanodelivery systems for natural products

Review

Author: Li, Chunhong ; Zhou, Ziyun ; Zhang, Qian ; Lei, Hui ; Liu, Minghua ; Zhang, Dan ; Zhang, Yifeng

Active components of natural products, which include paclitaxel, curcumin, gambogic acid, resveratrol, triptolide and celastrol, have promising anti-inflammatory, antitumor, anti-oxidant, and other pharmacological activities. However, their clinical application is limited due to low solubility, instability, low bioavailability, rapid metabolism, short half-life, and strong off-target toxicity. To overcome these drawbacks, cell membrane-based biomimetic nanosystems have emerged that avoid clearance by the immune system, enhance targeting, and prolong drug circulation, while also improving drug solubility and bioavailability, enhancing drug efficacy, and reducing side effects. This review summarizes recent advances in the preparation and coating of cell membrane-coated biomimetic nanosystems and in their applications to disease for targeted natural products delivery. Current challenges, limitations, and prospects in this field are also discussed, providing a research basis for the development of multifunctional biomimetic nanosystems for natural products.

16 Dec 2024·Animal Biotechnology

PI3K/AKT/mTORC1 signalling pathway regulates MMP9 gene activation via transcription factor NF-κB in mammary epithelial cells of dairy cows

Article

Author: Mao, Yongjin ; Ma, Xiaocong ; Zhao, Bing ; Zhao, Feng ; Yang, Yang ; Qu, Bo ; Cui, Yingjun ; Hou, Xiaoming ; Su, Chen ; Yang, Huilin

Matrix metalloproteinase 9 (MMP9) plays a pivotal role in mammary ductal morphogenesis, angiogenesis and glandular tissue architecture remodeling. However, the molecular mechanism of MMP9 expression in mammary epithelial cells of dairy cows remains unclear. This study aimed to explore the underlying mechanism of MMP9 expression. In this study, to determine whether the PI3K/AKT/mTORC1/NF-κB signalling pathway participates in the regulation of MMP9 expression, we treated mammary epithelial cells with specific pharmacological inhibitors of PI3K (LY294002), mTORC1 (Rapamycin) or NF-κB (Celastrol), respectively. Western blotting results indicated that LY294002, Rapamycin and Celastrol markedly decreased MMP9 expression and P65 nuclear translocation. Furthermore, we found that NF-κB (P65) overexpression resulted in elevated expression of MMP9 protein and activation of MMP9 promoter. In addition, we observed that Celastrol markedly decreases P65-overexpression-induced MMP9 promoter activity. Moreover, the results of the promoter assay indicated that the core regulation sequence for MMP9 promoter activation may be located at -420 ∼ -80 bp downstream from the transcription start site. These observations indicated that the PI3K/AKT/mTORC1 signalling pathway is involved in MMP9 expression by regulating MMP9 promoter activity via NF-κB in the mammary epithelial cells of dairy cows.

100 Deals associated with Celastrol

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Fractures, Bone	Phase 3	IR	Shahid Beheshti University of Medical Sciences	22 Dec 2023
Diabetes Mellitus	Phase 2	US	Harvard Medical School	04 Mar 2019
Nonalcoholic Steatohepatitis	Phase 2	US	Harvard Medical School	04 Mar 2019
Obesity	Phase 2	US	Harvard Medical School	21 May 2015
Pancreatic Cancer	Phase 2	US	The Ohio State University	01 Jan 2008
Prader-Willi Syndrome	Preclinical	US	ERX Pharmaceuticals Inc	10 Apr 2024
Autoimmune Diseases	Preclinical	CN	Osaka University	31 May 2023
Hepatitis C	Preclinical	CN	University of Macau	18 Apr 2023
Neoplasms	Preclinical	US	H. Lee Moffitt Cancer Center & Research Institute, Inc.	15 Apr 2011

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ARVO2013	Not Applicable	Glaucoma \| Optic Nerve Injuries	-	Celastrol	enmtpjivxs(nkzvutkzdv) = crsvicakvd bensiumcgf (yivbpiyzmt ) View more	Positive	01 Jun 2013
				Vehicle	enmtpjivxs(nkzvutkzdv) = cvymngtybd bensiumcgf (yivbpiyzmt ) View more