tr-1

LY3022859 (IMC-TR1) 是靶向 TBFbR2 的人源化抗体，可用于研究晚期实体瘤。

BTR-1 (5-Benzylidene-3-ethyl rhodanine) 是一种活性抗癌剂， 可激活细胞凋亡并诱导细胞死亡。它能够诱导细胞周期 S 期停滞，影响 DNA 复制。

TR-100 是一种小分子抑制剂，靶向肿瘤相关肌钙蛋白 (Tpm)。通过与 Tpm3.1 的 C-末端结合，TR-100 改变了 Tpm3.1 和肌动蛋白丝之间的相互作用，从而影响肌动蛋白丝束的稳定性和功能。此机制使 TR-100 在不影响心肌功能的前提下，特异性地作用于癌细胞的肌动蛋白丝束。TR-100 可用于研究 Tpm3.1 在癌细胞增殖和存活中的作用，以及 Tpm3.1 在胰岛素刺激下对葡萄糖摄取和胰岛素分泌的影响。

Naloxegol (NKTR-118; AZ-13337019) is an opioid-receptor antagonist[1]. [1]. Yoon SC, et al. Naloxegol in opioid-induced constipation: a new paradigm in the treatment of a common problem. Patient Prefer Adherence. 2017 Jul 24;11:1265-1271.

TR-14035 (MDK-1191) 是一种具有口服活性的 α4β7/α4β1整合素双重抑制剂，对 α4β7和 α4β1作用的 IC50值分别为 7 和 87 nM，可用于炎症和自体免疫疾病的研究。

FTR1335 is a CaNMT inhibitor (IC50 = 0.49 nM) with good fungal selectivity. CaNMT inhibitors are fungicidal and show antifungal activity against Candida (especially fluconazole-resistant strains). They function by inhibiting N-myristoyltransferase (NMT), which catalyzes the transfer of a C14 fatty acif from myristoyl-CoA to the N-terminal of glycine in many fungal proteins. Without this process, fungi can die. This process also occurs in humans, and as such selectivity is an important characteristic of these drugs.

MTR-105 is a nitric oxide synthase inhibitor.

TR-107 (Anticancer agent 230) 是一种具有选择性和高效性的线粒体蛋白酶 ClpP 激活剂，抑制 MDA-MB-231 异种移植模型中的肿瘤生长。

Meclinertant (SR 48692) 是神经降压素受体-1（NT1）拮抗剂，可阻断神经降压素诱导的兴奋，可用于研究神经系统疾病。

Trifluoromethyl-tubercidin (TFMT)可抑制宿主Mtr1并抑制病毒复制。TFMT 通过其S-adenosyl-l-methionine 结合袋相互作用抑制Mtr1，限制流感病毒复制。TFMT 能有效抑制病毒在小鼠体内的复制，毒性很小。

Montelukast sodium (MK0476) 是可口服的半胱氨酸白三烯受体1 选择性拮抗剂，可用于研究预防哮喘和肝损伤。它还可减少心脏损伤，在肠缺血-再灌注损伤中也具有抗氧化作用。

TbPTR1 inhibitor 2 被确定为改进的蝶啶还原酶-1 (PTR1) 抑制剂和抗锥虫药物的新发展。

7-Amino-4-(trifluoromethyl)coumarin (Coumarin 151) 是一种荧光标记物，其激发和发射波长分别为400和500 nm，可用来灵敏的检测蛋白酶。

Aristolochic acid A 是植物提取物 Aristolochic acids 的主要成分，主要存在于 Aristolochia和 Asarum 草本植物中，能够显著降低激活蛋白1（AP-1）和NF-κB的活性，并下调人细胞中与膀胱癌相关的BLCAP基因的表达，常用于诱导肾毒性模型。

Nevanimibe is an orally active and selective inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) (EC50 of 9 nM).

Nevanimibe hydrochloride (PD-132301 hydrochloride) 是一种口服有效的，选择性酰基辅酶 A：胆固醇 O-酰基转移酶 1 抑制剂，EC50为 9 nM。它抑制 ACAT2，EC50为 368 nM。它诱导细胞凋亡，具有抗肾上腺皮质癌的潜力。

Montelukast (Singular) 是可口服的半胱氨酸白三烯受体1 选择性拮抗剂，可用于研究预防哮喘和肝损伤。它还可减少心脏损伤，在肠缺血-再灌注损伤中也具有抗氧化作用。

SBI-553 是能透过血脑屏障的NTR1的别构抑制剂，EC50值为 0.34 μM。

LZTR1-KRAS modulator 1 作为一种KRAS-LZTR1相互作用的调节剂，能够促进LZTR1-KRAS复合物的聚集。

Fimasartan (BR-A-657) 是血管紧张素受体 AT1 非肽类拮抗剂，用于研究高血压和心力衰竭。

MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂，在豚鼠和人肺膜的 Ki 分别为0.22 和 2.1 nM。

Naloxegol oxalate (NKTR-118) 是一种外周选择性 opioid 样物质拮抗剂，用于治疗 opioid 样物质引起的便秘。

Resolvin conjugate in tissue regeneration 1 (RCTR1) is a specialized pro-resolving mediator (SPM) biosynthesized from docosahexaenoic acid by isolated human macrophages and apoptotic polymorphonuclear (PMN) neutrophils.1It has been found in human spleen and bone marrow.2RCTR1 is produced via lipoxygenase-mediated oxidation of DHA to 7(S)-8-epoxy-17(S)-HDHA, which is conjugated to glutathione.1,2,3RCTR1 (10 nM) increases phagocytosis ofE. colior apoptotic neutrophils in isolated human monocyte-derived macrophages.2It decreases chemotaxis induced by leukotriene B4in isolated human neutrophils when used at a concentration of 10 nM. RCTR1 (1 and 10 nM) accelerates tissue regeneration in planaria. Intraperitoneal administration of RCTR1 (100 ng/animal) shortens the inflammatory resolution period and decreases inflammatory exudate neutrophil infiltration in a mouse model ofE. coli-induced peritonitis. 1.Dalli, J., Ramon, S., Norris, P.C., et al.Novel proresolving and tissue-regenerative resolvin and protectin sulfido-conjugated pathwaysFASEB J.29(5)2120-2136(2015) 2.de la Rosa, X., Norris, P.C., Chiang, N., et al.Identification and complete stereochemical assignments of the new resolvin conjugates in tissue regeneration in human tissues that stimulate proresolving phagocyte functions and tissue regenerationAm. J. Pathol.188(4)950-966(2018) 3.Rodriguez, A.R., and Spur, B.W.First total synthesis of pro-resolving and tissue-regenerative resolvin sulfido-conjugatesTetrahedron Lett.58(16)1662-1668(2017)

Protectin conjugates in tissue regeneration 1 (PCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid . DHA is oxidized to 16S,17S-epoxy-protectin, which is then converted to PCTR1 by glutathione S-transferase. PCTR1 levels increase during resolution of acute microbial-induced peritonitis in mice. PCTR1 (30 ng, i.p.) administration 12 hours post-infection increases macrophage numbers and activity and shortens the resolution phase of inflammation by 57%. It also reduces the levels of PGE2 , PGD2 , and TXB2 in peritoneal exudates.