glutamine metabolism

Sirpiglenastat (DRP-104) 是一种谷氨酰胺 (glutamine) 拮抗剂，是DON的前药，具有抗肿瘤活性，通过抑制谷氨酰胺代谢和刺激先天性和适应性免疫系统来发挥作用。

L-Pyroglutamic acid (pidolic acid) 是 Pyroglutamic acid 的左旋异构体，是人体中具有生物特性的对映异构体。Pyroglutamic acid 是谷胱甘肽代谢中的中间体。

Trivalent hydroxyarsinothricn (R-AST-OH) 是一种共价且不可逆的肾型谷氨酰胺酶 (KGA) 抑制剂。它通过与谷氨酰胺结合位点结合并与活性位点半胱氨酸残基形成共价键来起作用。Trivalent hydroxyarsinothricn 能选择性地杀死三阴性乳腺癌 (TNBC) 细胞，而对照细胞系则没有细胞毒性。KGA 作为控制谷氨酰胺代谢的酶，与肿瘤的恶性程度相关。

Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) reduces tumor growth in an SW1990 mouse xenograft model. |1. Zhang, P., Li, X.-M., Wang, J.-N., et al. New butenolide derivatives from the marine-derived fungus Paecilomyces variotii with DPPH radical scavenging activity. Phytochem. Lett. 11, 85-88 (2015).|2. Sun, W., Luan, S., Qi, C., et al. Aspulvinone O, a natural inhibitor of GOT1 suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism. Cell Commun. Signal. 17(1), 111 (2019).

Aspulvinone H is a natural inhibitor of glutamic oxaloacetate transaminase 1 (GOT1), suppressing glutamine metabolism, making PDAC cells sensitive to oxidative stress and inhibiting cell proliferation, exhibiting potent in vivo antitumor activity in an SW1990-cell-induced xenograft model.

GLS1 Inhibitor-4 (compound 41e)作为一种高效的GLS1抑制剂，具有11.86 nM的IC50值。该化合物展现了抗增殖效果、优秀的代谢稳定性以及强大的GLS1结合亲和力。它通过阻断谷氨酰胺代谢和诱导ROS生成，能够引发细胞凋亡并表现出对抗肿瘤的活性。

LWG-301是一种针对Glutaminase1(GLS1)的变构抑制剂，具有(IC50=7 nM)。通过显著阻断谷氨酰胺代谢并增加细胞内ROS，LWG-301能够诱导细胞凋亡(apoptosis)。在HCT116异种移植模型中，LWG-301展示出中等抗肿瘤活性。

GlutaminaseC-IN-2（compound 11）为GAC变构抑制剂，IC50值为10.64 nM。该化合物通过干扰谷氨酰胺代谢，调控细胞代谢产物，进而提高ROS水平，并展现出抗癌活性。

L-Pyroglutamic acid (Standard) 是 L-Pyroglutamic acid 的标准品，适用于定量分析、质量控制及生化实验等相关研究。L-Pyroglutamic acid (pidolic acid) 是 Pyroglutamic acid 的左旋异构体，是人体中具有生物特性的对映异构体。Pyroglutamic acid 是谷胱甘肽代谢中的中间体。