Delving into the Latest Updates on Beryllium Discovery Corp. with Synapse

概览

疾病领域	数量

肿瘤	1

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

L-lactate dehydrogenase(L-乳酸脱氢酶)	1

关联

1

项与 Beryllium Discovery Corp. 相关的药物

NCATS-SM1440

靶点

L-lactate dehydrogenase

作用机制

L-lactate dehydrogenase抑制剂

在研机构

Beryllium Discovery Corp.

原研机构

Beryllium Discovery Corp.

在研适应症

肿瘤

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-

100 项与 Beryllium Discovery Corp. 相关的临床结果

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0 项与 Beryllium Discovery Corp. 相关的专利（医药）

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17

项与 Beryllium Discovery Corp. 相关的文献（医药）

2024-04-01·Acta Crystallographica Section F Structural Biology Communications

Structural and functional characterization of FabG4 from Mycolicibacterium smegmatis

Article

作者: Lorimer, Donald D ; Staker, Bart L ; McLaughlin, Krystle J ; Arakaki, Tracy L ; Myler, Peter ; Ran, Xinping ; Mayclin, Stephen ; Clifton, Matthew C ; Parikh, Prashit ; Edwards, Thomas E ; Abendroth, Jan

The rise in antimicrobial resistance is a global health crisis and necessitates the development of novel strategies to treat infections. For example, in 2022 tuberculosis (TB) was the second leading infectious killer after COVID-19, with multi-drug-resistant strains of TB having an ∼40% fatality rate. Targeting essential biosynthetic pathways in pathogens has proven to be successful for the development of novel antimicrobial treatments. Fatty-acid synthesis (FAS) in bacteria proceeds via the type II pathway, which is substantially different from the type I pathway utilized in animals. This makes bacterial fatty-acid biosynthesis (Fab) enzymes appealing as drug targets. FabG is an essential FASII enzyme, and some bacteria, such as Mycobacterium tuberculosis, the causative agent of TB, harbor multiple homologs. FabG4 is a conserved, high-molecular-weight FabG (HMwFabG) that was first identified in M. tuberculosis and is distinct from the canonical low-molecular-weight FabG. Here, structural and functional analyses of Mycolicibacterium smegmatis FabG4, the third HMwFabG studied to date, are reported. Crystal structures of NAD+ and apo MsFabG4, along with kinetic analyses, show that MsFabG4 preferentially binds and uses NADH when reducing CoA substrates. As M. smegmatis is often used as a model organism for M. tuberculosis, these studies may aid the development of drugs to treat TB and add to the growing body of research that distinguish HMwFabGs from the archetypal low-molecular-weight FabG.

2022-08-30·mBio

Genetic Interaction Analysis Reveals that Cryptococcus neoformans Utilizes Multiple Acetyl-CoA-Generating Pathways during Infection

Article

作者: Alden, Katy M. ; Beattie, Sarah R. ; Krysan, Damian J. ; Jezewski, Andrew J. ; Fox, David

The adaptation of environmental fungal pathogens to the mammalian host is critical to pathogenesis. Of these adaptations, the remodeling of carbon metabolism is particularly important.

2021-06-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Optimization of ether and aniline based inhibitors of lactate dehydrogenase

4区 · 医学

Article

作者: Christov, Plamen P ; Lee, Tobie D ; Hu, Xin ; Brimacombe, Kyle R ; Romaine, Ian M ; Urban, Daniel J ; Maloney, David J ; Flint, Andrew J ; Green, Neal ; Waterson, Alex G ; Hall, Matthew D ; Sulikowski, Gary A ; Lamers, Alexander ; Davies, Douglas R ; Mott, Bryan T ; Jadhav, Ajit ; Jana, Somnath ; Moore, William J ; Stott, Gordon M ; Rai, Ganesha ; Lukacs, Christine M ; Kim, Kwangho ; Allweil, Alexander A

Lactate dehydrogenase (LDH) is a critical enzyme in the glycolytic metabolism pathway that is used by many tumor cells. Inhibitors of LDH may be expected to inhibit the metabolic processes in cancer cells and thus selectively delay or inhibit growth in transformed versus normal cells. We have previously disclosed a pyrazole-based series of potent LDH inhibitors with long residence times on the enzyme. Here, we report the elaboration of a new subseries of LDH inhibitors based on those leads. These new compounds potently inhibit both LDHA and LDHB enzymes, and inhibit lactate production in cancer cell lines.

100 项与 Beryllium Discovery Corp. 相关的药物交易

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100 项与 Beryllium Discovery Corp. 相关的转化医学

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