AMPK modulators(AMP activated protein kinase modulators), Forkhead box protein O1 expression modulators, HNF4A modulators(hepatocyte nuclear factor 4 alpha modulators)

+ [2]

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication-

Inactive Indication

Dyslipidemias

Originator Organization

Syndromex

Active Organization-

Inactive Organization

Syndromex

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

100 Clinical Results associated with M-1001

100 Translational Medicine associated with M-1001

100 Patents (Medical) associated with M-1001

Literatures (Medical) associated with M-1001

01 Jan 2023·Zoological Research

EPAS1 prevents telomeric damage-induced senescence by enhancing transcription of TRF1, TRF2, and RAD50

Article

Author: Zhang, Jiao ; Chang, Qing ; Liu, Gao-Jing ; Liu, Xiu-Yun ; Chen, Qiong-Fang ; Hua, Rong ; Xu, Dong-Ming ; Li, Kai-Qin ; Liu, Zhen ; Xie, Yun-Hua ; Zhao, Bo ; Huang, Xiao-Yan ; Tu, Qiu

Telomeres are nucleoprotein structures located at the end of each chromosome, which function in terminal protection and genomic stability. Telomeric damage is closely related to replicative senescence in vitro and physical aging in vivo. As relatively long-lived mammals based on body size, bats display unique telomeric patterns, including the up-regulation of genes involved in alternative lengthening of telomeres (ALT), DNA repair, and DNA replication. At present, however, the relevant molecular mechanisms remain unclear. In this study, we performed cross-species comparison and identified EPAS1, a well-defined oxygen response gene, as a key telomeric protector in bat fibroblasts. Bat fibroblasts showed high expression of EPAS1, which enhanced the transcription of shelterin components TRF1 and TRF2, as well as DNA repair factor RAD50, conferring bat fibroblasts with resistance to senescence during long-term consecutive expansion. Based on a human single-cell transcriptome atlas, we found that EPAS1 was predominantly expressed in the human pulmonary endothelial cell subpopulation. Using in vitro-cultured human pulmonary endothelial cells, we confirmed the functional and mechanistic conservation of EPAS1 in telomeric protection between bats and humans. In addition, the EPAS1 agonist M1001 was shown to be a protective compound against bleomycin-induced pulmonary telomeric damage and senescence. In conclusion, we identified a potential mechanism for regulating telomere stability in human pulmonary diseases associated with aging, drawing insights from the longevity of bats.

01 Feb 2021·European Journal of Medicinal ChemistryQ1 · MEDICINE

Insight into the binding mode of HIF-2 agonists through molecular dynamic simulations and biological validation

Q1 · MEDICINE

Article

Author: Yu, Quanwei ; Zhang, Xiaojin ; Yu, Yancheng ; Wu, Chenyang ; Liu, Simeng

Hypoxia-inducible factor-2 (HIF-2), a heterodimeric transcriptional protein consisting of HIF-2α and aryl hydrocarbon receptor nuclear translocator (ARNT) subunits, has a broad transcriptional profile that plays a vital role in human oxygen metabolism. M1001, a HIF-2 agonist identified by high-throughput screening (HTS), is capable of altering the conformation of Tyr281 of the HIF-2α PAS-B domain and enhancing the affinity of HIF-2α and ARNT for transcriptional activation. M1002, an analog of M1001, shows improved efficacy than M1001. However, the cocrystal structure of M1001 and HIF-2 has some defects in revealing the agonist binding mode due to the relatively low resolution, while the binding mode of M1002 remained unexplored. To in-depth understand agonist binding profiles, herein, the molecular dynamic (MD) simulations was applied to construct a stable agonist-protein model, and a possible binding mode was proposed through the analysis of the binding free energy and hydrogen bonding of the simulation results. Nine compounds were then synthesized and evaluated to verify the proposed binding mode. Among them, compound 10 manifested improved agonistic activity and reduced toxicity compared to M1002. This study provides deep insight into the binding mode of such HIF-2 agonists, which would be useful for designing novel agonists for HIF-2.

01 Jul 1995·Proceedings of the National Science Council, Republic of China. Part B, Life sciences

Production, purification and characterization of two proteinaceous hen-egg-white lysozyme inhibitors from Pseudomonas aeruginosa M-1001.

Article

Author: Pai, C S ; Shieh, S T ; Wang, S L

Two proteinaceous lysozyme inhibitors, hen-egg-white lysozyme inhibitors F-I and F-II, were isolated from the culture broth of a bacterial strain identified as Pseudomonas aeruginosa M-1001. Maximum lysozyme inhibitory activity was obtained when the bacterium was grown aerobically in a medium consisting of 0.25% glucose, 0.25% beef extract, 0.25% polypepton, 1.0% sodium L-glutamate, and 1.0% soluble starch (pH 7.0) at 37 degrees C after 20-24 hrs. F-I and F-II were purified 20 and 7.5-fold, respectively, from the culture supernatant of P. aeruginosa M-1001 by ammonium sulfate fractionation, DEAE-Sepharose CL-6B column chromatography, and Sephacryl S-200 gel chromatography. The molecular weights of F-I and F-II were estimated to be about 57,000 and 33,000, by SDS-PAGE, respectively. F-I was stable in a pH range between 6 and 10 and below 50 degrees C. F-II was stable in a pH range between 6 and 11 and below 40 degrees C. Many Gram-positive bacteria were found to be inhibited by the crude lysozyme inhibitors.

100 Deals associated with M-1001

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Dyslipidemias	Phase 2	IL	Syndromex	24 Dec 2020

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