TLR7 antagonists(Toll like receptor 7 antagonists), TLR8 antagonists(Toll like receptor 8 antagonists), TLR9 antagonists(Toll like receptor 9 antagonists)

Therapeutic Areas

Immune System DiseasesNervous System DiseasesEye Diseases+ [3]

Active Indication

Multiple SclerosisSjogren's SyndromeSystemic Lupus Erythematosus

Inactive Indication-

Originator Organization

Jiangsu Hengrui Pharmaceutical Group Co. Ltd.

Active Organization

Jiangsu Hengrui Pharmaceutical Group Co. Ltd.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

100 Clinical Results associated with TLR7/8/9 inhibitor(Hengrui pharmaceuticals)

100 Translational Medicine associated with TLR7/8/9 inhibitor(Hengrui pharmaceuticals)

100 Patents (Medical) associated with TLR7/8/9 inhibitor(Hengrui pharmaceuticals)

Literatures (Medical) associated with TLR7/8/9 inhibitor(Hengrui pharmaceuticals)

01 Apr 2024·European Journal of Medicinal Chemistry

Active site-directed probes targeting dipeptidyl peptidases 8 and 9

Article

Author: Benramdane, Siham ; De Meester, Ingrid ; Van Rymenant, Yentl ; Corthaut, Sam ; Verhulst, Emile ; Pintelon, Isabel ; Espadinha, Margarida ; Augustyns, Koen ; Van Wielendaele, Pieter ; Van der Veken, Pieter ; De Loose, Joni ; Filippi, Nicolò ; Thys, Sofie

Dipeptidyl peptidases (DPP) 8 and 9 are intracellular serine proteases that play key roles in various biological processes and recent findings highlight DPP8 and DPP9 as potential therapeutic targets for hematological and inflammasome-related diseases. Despite the substantial progress, the precise biological functions of these proteases remain elusive, and the lack of selective chemical tools hampers ongoing research. In this paper, we describe the synthesis and biochemical evaluation of the first active site-directed DPP8/9 probes which are derived from DPP8/9 inhibitors developed in-house. Specifically, we synthesized fluorescent inhibitors containing nitrobenzoxadiazole (NBD), dansyl (DNS) and cyanine-3 (Cy3) reporters to visualize intracellular DPP8/9. We demonstrate that the fluorescent inhibitors have high affinity and selectivity towards DPP8/9 over related S9 family members. The NBD-labeled DPP8/9 inhibitors were nominated as the best in class compounds to visualize DPP8/9 in human cells. Furthermore, a method has been developed for selective labeling and visualization of active DPP8/9 in vitro by fluorescence microscopy. A collection of potent and selective biotinylated DPP8/9-targeting probes was also prepared by replacing the fluorescent reporter with a biotin group. The present work provides the first DPP8/9-targeting fluorescent compounds as useful chemical tools for the study of DPP8 and DPP9's biological functions.

28 Apr 2016·Journal of Medicinal ChemistryQ1 · MEDICINE

Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription

Q1 · MEDICINE

Article

Author: Handa, Noriko ; Umehara, Takashi ; Fujiwara, Takashi ; Niwa, Hideaki ; Hirano, Tomoya ; Ito, Akihiro ; Dan, Shingo ; Nishino, Norikazu ; Sonoda, Takeshi ; Yoshida, Minoru ; Yokoyama, Shigeyuki ; Ogawa, Kenji ; Takemoto, Yasushi ; Tariq, Mohammad ; Kagechika, Hiroyuki ; Okamura, Mutsumi ; Yamori, Takao

SET domain containing lysine methyltransferase 7/9 (Set7/9), a histone lysine methyltransferase (HMT), also methylates non-histone proteins including estrogen receptor (ER) α. ERα methylation by Set7/9 stabilizes ERα and activates its transcriptional activities, which are involved in the carcinogenesis of breast cancer. We identified cyproheptadine, a clinically approved antiallergy drug, as a Set7/9 inhibitor in a high-throughput screen using a fluorogenic substrate-based HMT assay. Kinetic and X-ray crystallographic analyses revealed that cyproheptadine binds in the substrate-binding pocket of Set7/9 and inhibits its enzymatic activity by competing with the methyl group acceptor. Treatment of human breast cancer cells (MCF7 cells) with cyproheptadine decreased the expression and transcriptional activity of ERα, thereby inhibiting estrogen-dependent cell growth. Our findings suggest that cyproheptadine can be repurposed for breast cancer treatment or used as a starting point for the discovery of an anti-hormone breast cancer drug through lead optimization.

01 Feb 1999·Journal of NeurophysiologyQ3 · MEDICINE

C-PR Neuron ofAplysiaHas Differential Effects on “Feeding” Cerebral Interneurons, Including Myomodulin-Positive CBI-12

Q3 · MEDICINE

Article

Author: Kupfermann, Irving ; Hurwitz, Itay ; Perrins, Ray ; Weiss, Klaudiusz R. ; Xin, Yuanpei

C-PR neuron of Aplysia has differential effects on “feeding” cerebral interneurons, including myomodulin-positive CBI-12. Head lifting and other aspects of the appetitive central motive state that precedes consummatory feeding movements in Aplysia is promoted by excitation of the C-PR neuron. Food stimuli activate C-PR as well as a small population of cerebral-buccal interneurons (CBIs). We wished to determine if firing of C-PR produced differential effects on the various CBIs or perhaps affected all the CBIs uniformly as might be expected for a neuron involved in producing a broad undifferentiated arousal state. We found that when C-PR was fired, it produced a wide variety of effects on various CBIs. Firing of C-PR evoked excitatory input to a newly identified CBI (CBI-12) the soma of which is located in the M cluster near the previously identified CBI-2. CBI-12 shares certain properties with CBI-2, including a similar morphology and a capacity to drive rhythmic activity of the buccal-ganglion. Unlike CBI-2, CBI-12 exhibits myomodulin immunoreactivity. Furthermore when C-PR is fired, CBI-12 receives a polysynaptic voltage-dependent slow excitation, whereas, CBI-2 receives relatively little input. C-PR also polysynaptically excites other CBIs including CBI-1 and CBI-8/9 but produces inhibition in CBI-3. In addition, firing of C-PR inhibits plateau potentials in CBI-5/6. The data suggest that activity of C-PR may promote the activity of one subset of cerebral-buccal interneurons, perhaps those involved in ingestive behaviors that occur during the head-up posture. C-PR also inhibits some cerebral-buccal interneurons that may be involved in behaviors in which C-PR activity is not required or may even interfere with other feeding behaviors such as rejection or grazing, that occur with the head down.

100 Deals associated with TLR7/8/9 inhibitor(Hengrui pharmaceuticals)

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Multiple Sclerosis	Preclinical	CN	Jiangsu Hengrui Pharmaceutical Group Co. Ltd.	26 Nov 2021
Sjogren's Syndrome	Preclinical	CN	Jiangsu Hengrui Pharmaceutical Group Co. Ltd.	26 Nov 2021
Systemic Lupus Erythematosus	Preclinical	CN	Jiangsu Hengrui Pharmaceutical Group Co. Ltd.	26 Nov 2021

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