Feb 1, 2025 · KGA is synthesized via cross-aldol condensation of pyruvic and glyoxylic acids to 2-hydroxy-4-oxopentanedioic acid, followed by its sequential dehydration and hydrogenation on Pd/TiO 2, affording...

使用来自80周龄小鼠脂肪、皮肤和肺的间充质细胞群进行荧光激活细胞分类，发现1-10%的细胞CD26阳性（图3E）。与CD26阴性相比，CD26高表达组SA–β-gal阳性细胞比例更高，KGA和p16表达更高（图3E-F），表明SnCs在体内主要通过溶酶体膜损伤介导的酸中毒表达KGA。

作为催化谷氨酰胺分解的第一种酶，人肾型谷氨酰胺酶异构体 (KGA) 正成为 BPTES [bis-2- (5 phenylacetamido-1, 2, 4-thiadiazol-2-yl)ethyl硫化物]，尽管 KGA 的调控机制尚不清楚。 基于晶体结构，我们揭示了 BPTES 与 KGA 二聚体界面处的变构口袋结合，触发了催化位点附近关键环（Glu312-Pro329）的显着构象变化并使其失活。 BPTES 在疏水口袋上的结合模式解释了它对 KGA 的特异性。 有趣的是，细胞中的 KGA 活性受 EGF 刺激，和 KGA 与 Raf-1/Mek2/Erk 信 …

Jul 1, 2022 · GLS1 enzymes (Glutaminase C (GAC) and kidney-type Glutaminase (KGA)) are gaining prominence as a target for tumor treatment including lung, breast, kidney, prostate, and colorectal. To date, several medicinal chemistry studies are being conducted to develop new and effective inhibitors against GLS1 enzymes.

2-keto-D-gluconic acid (14) (2-KGA) is an organic acid used in cosmetics, pharmaceutical and environmental industries. Moreover, it is a key intermediate in the synthesis of several products, including erythorbic acid (isoascorbic acid), which is an important food additive, preservative and mild antioxidant approved by the FDA (Chia et al. 2008 ...

Apr 5, 2023 · In 2020, Bridget et al. reported compound 14 with a mercaptoethyl(-SCH 2 CH 2-) linker as a novel GLS1 inhibitor (Fig. 6 A). It exerted potent inhibitory activity against GLS1 with an IC 50 value of 0.05 μM. Additionally, its derivatives, containing a n-propyl linked chain, possessed inferior efficacy (IC 50 = 2.3 μM).

Oct 16, 2023 · GLS1可翻译产生两种不同的活性形式：肾谷氨酰胺酶A（KGA）和高度活化的谷氨酰胺酶亚型C（GAC），其中GAC亚型在多种癌症中因其对谷氨酰胺的高度利用而高度表达。 已有研究表明谷氨酰胺酶的抑制显示出抑制癌症细胞生长和诱导细胞凋亡的潜力，因此成为癌症治疗中备受瞩目的治疗靶点。 目前，一种特定的谷氨酰胺酶抑制剂正在进行多项临床试验。...

In the present study, a kguK gene encoding 2-ketogluconate kinase from P. plecoglossicida JUIM01 was cloned and heterologously expressed in Pichia pastoris. The recombinant KguK showed the highest...

Mar 4, 2024 · Our findings highlight how ankyrin repeats on GLS2 regulate enzymatic activity, while allosteric activators stabilize, and clinically relevant inhibitors block, filament formation that enables...

Spindle Thread : 14 m; Electricity Connection : Single Phase; Voltage : 240 V; Frequency : 50 Hz