Delving into the Latest Updates on Naicons Srl with Synapse

概览

疾病领域	数量

感染	2
神经系统疾病	1

排名前五的药物类型	数量

重组多肽	1
未知	1
小分子化药	1

排名前五的靶点	数量

TRPVs(瞬时受体电位阳离子通道亚家族V)	1

关联

5

项与 Naicons Srl 相关的药物

NAI-107

靶点

TRPVs

作用机制

TRPVs调节剂 [+1]

在研机构

Naicons Srl

原研机构

Sentinella Pharmaceuticals, Inc.

在研适应症

革兰氏阳性细菌感染

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

NAI-603

靶点-

作用机制

细胞壁抑制剂

在研机构

Naicons Srl

原研机构

Vicuron Pharmaceuticals LLC

在研适应症

革兰氏阳性细菌感染

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

NAI-112

靶点-

作用机制-

在研机构

Naicons Srl

原研机构

Naicons Srl

在研适应症

神经痛

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

1

项与 Naicons Srl 相关的临床试验

EUCTR2014-001491-62-SK / Not yet recruiting临床2期

Clinical efficacy and safety of NAI-Acne gel 3% applied twice-a-day to patients with facial acne vulgaris - NAI-003 3% gel efficacy pilot

开始日期2014-08-11

申办/合作机构

Naicons Srl

100 项与 Naicons Srl 相关的临床结果

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0 项与 Naicons Srl 相关的专利（医药）

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5

项与 Naicons Srl 相关的文献（医药）

bioRxiv, Molecular Biology

Antibacterial nucleoside-analog inhibitor of bacterial RNA polymerase: pseudouridimycin

作者: Deho, Gianni ; Maffioli, Sonia I. ; Degen, David ; Serina, Stefania ; Kaltofen, Petra ; Chiriac, Alina Iulia ; Ebright, Richard H. ; Facchetti, Giuseppe ; Del Gatto, Giancarlo ; Candiani, Gianpaolo ; Mazzetti, Carlo ; Carzaniga, Thomas ; Sahl, Hans-Georg ; Donadio, Stefano ; Monciardini, Paolo ; Zhang, Yu ; Guglierame, Paola

There is an urgent need for new antibacterial drugs effective against bacterial pathogens resistant to current drugs.Nucleoside-analog inhibitors (NAIs) of viral nucleotide polymerases have had transformative impact in treatment of HIVand HCV.NAIs of bacterial RNA polymerase (RNAP) potentially could have major impact on treatment of bacterial infection, particularly because functional constraints on substitution of RNAP nucleoside triphosphate (NTP) binding sitescould limit resistance emergence.Here we report the discovery, from microbial extract screening, of an NAI that inhibits bacterial RNAP and exhibits antibacterial activity against a broad spectrum of drug-sensitive and drug-resistant bacterial pathogens: pseudouridimycin (PUM).PUM is a novel microbial natural product consisting of a formamidinylated, N-hydroxylated Gly-Gln dipeptide conjugated to 6'-amino-pseudouridine.PUM potently and selectively inhibits bacterial RNAP in vitro, potently and selectively inhibits bacterial growth in culture, and potently clears infection in a mouse model of Streptococcus pyogenes peritonitis.PUM inhibits RNAP through a binding site on RNAP (the "i+1" NTP binding site) and mechanism (competition with UTP for occupancy of the "i+1" NTP binding site) that differ from those of the RNAP inhibitor and current antibacterial drug rifampin (Rif).PUM exhibits additive antibacterial activity when co-administered with Rif, exhibits no cross-resistance with Rif, and exhibits a spontaneous resistance rate an order-of-magnitude lower than that of Rif.The results provide the first example of a selective NAI of bacterial RNAP, provide an advanced lead compound for antibacterial drug development, and provide structural information and synthetic routes that enable lead optimization for antibacterial drug development.

Lantibiotics and other antibacterial peptides

作者: Sosio, Margherita ; Donadio, Stefano

A review.Lantibiotics and other ribosomally synthesized peptides have attracted increasing attention in the search for new chem. classes of antibacterial agents effective against multidrug-resistant pathogens.Several factors have probably contributed to this resurgent interest.Among them, the realization that many different classes of ribosomally synthesized peptides were produced by almost all taxa of bacteria; that lantibiotics, being ribosomally synthesized, are amenable to the generation of analogs by codon substitutions in the structural gene; and that, by binding to biosynthetic intermediates and not directly to enzymes, resistance in bacterial pathogens cannot be simply acquired by mutations in the target enzymes.In this chapter, the authors will review the chem., biosynthesis, occurrence and mechanism of action of lanthipeptides, with particular focus on lantibiotics.The authors will also present three lantibiotics that are currently under advanced preclin. or early clin. development, as well as some recently discovered compounds which represent improved variants of known lantibiotics.

RSC Advances

Allopeptimicins: unique antibacterial metabolites generated by hybrid PKS-NRPS, with original self-defense mechanism in Actinoallomurus

作者: Landini, Paolo ; Sosio, Margherita ; Iorio, Marianna ; Brunati, Cristina ; Maffioli, Sonia Ilaria ; Donadio, Stefano ; Tocchetti, Arianna ; Gentile, Andrea

In the search for structurally novel metabolites with antibacterial activity, innovative approaches must be implemented to increase the probability of discovering novel chem. from microbial sources.Here we report on the application of metabolomic tools to the genus Actinoallomurus, a poorly explored member of the Actinobacteria.From examining extracts derived from 88 isolates belonging to this genus, we identified a family of cyclodepsipeptides acylated with a C20 polyketide chain, which we named allopeptimicins.These mols. possess unusual structural features, including several double bonds in the amino-polyketide chain and four non-proteinogenic amino acids in the octapeptide.Remarkably, allopeptimicins are produced as a complex of active and inactive congeners, the latter carrying a sulfate group on the polyketide amine.This modification is also a mechanism of self-protection in the producer strain.The structural uniqueness of allopeptimicins is reflected in a biosynthetic gene cluster showing a mosaic structure, with dedicated gene cassettes devoted to formation of specialized precursors and modular assembly lines related to those from different pathways.

100 项与 Naicons Srl 相关的药物交易

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100 项与 Naicons Srl 相关的转化医学

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管线布局

2024年09月16日管线快照

管线布局中药物为当前组织机构及其子机构作为药物机构进行统计，早期临床1期并入临床1期，临床1/2期并入临床2期，临床2/3期并入临床3期

临床前

3

2

其他

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当前项目

药物(靶点)	适应症	全球最高研发状态

NAI-112	神经痛更多	临床前
NAI-107 ( TRPVs )	革兰氏阳性细菌感染更多	临床前
NAI-603	革兰氏阳性细菌感染更多	临床前
NAI-Acne ( EEF1A1 )	寻常痤疮更多	无进展
NAI-802	革兰氏阳性细菌感染更多	无进展