cysteine-activated

H2S Donor 5a 是一种稳定的、半胱氨酸活化的的 H2S 供体。它是研究 H2S 的有用工具。

NAAA-IN-3 (Compound 17a) 是一种有效的、选择性的 NAAA 抑制剂，IC50为 50 nM。NAAA 是一种半胱氨酸酰胺酶，它优先水解内源性生物脂棕榈酰乙醇酰胺 (PEA) 和油酰乙醇酰胺 (OEA)。PEA 是核过氧化物酶体增殖物激活受体-α (PPAR-α) 的内源性激动剂，PPAR-α 是炎症和疼痛的关键调节因子。 NAAA-IN-3 的潜在作用是作为炎症和疼痛的治疗剂。

Cefminox (Sodium) is a new cephamycin antibiotic possessing a D-amino acid moiety derived from D-cysteine at the C-7B side chain. Cefminox is active against a wide range of bacteria, especially Gram-negative and anaerobic bacteria. Cefminox shows excellent in vivo efficacy (ED50) which is higher than would be expected from its in vitro activity (MIC). Moreover, cefminox possesses more potent activity in suppression of bacterial regrowth than other cephems[1]. Cefminox (Sodium) was the most active beta-lactam, with an MIC at which 50% of isolates are inhibited (MIC50) of 1.0 microg/ml and an MIC90 of 16.0 microg/ml. Cefminox was especially active against Bacteroides fragilis (MIC90, 2.0 microg/ml), Bacteroides thetaiotaomicron (MIC90, 4.0 microg/ml), fusobacteria (MIC90, 1.0 microg/ml), peptostreptococci (MIC90, 2.0 microg/ml), and clostridia, including Clostridium difficile (MIC90, 2.0 microg/ml)[2]. The use of a single preoperative dose of cefminox was similar in efficacy to 3 doses of cefoxitin administered every 4 hours, and that the serum and tissue concentrations attained provide adequate antibiotic coverage[3]. Moreover, cefminox as a dual agonist of IP (Prostacyclin receptor) and PPARγ (peroxisome proliferator-activated receptor-gamma) that significantly inhibits PASMC proliferation by up-regulation of PTEN (phosphatase and tensin homolog) and cAMP ( cyclic adenosine monophosphate), suggesting that it has potential for treatment of PAH(pulmonary arterial hypertension)[4].

Olmutinib is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor, used in the treatment of T790M mutation positive non-small cell lung cancer. Olmutinib covalently binds a cysteine residue near the kinase domain of mutant EGFRs to prevent phosphorylation of the receptor. EGFRs are frequently over-expressed in lung cancer and contribute to activation of the phosphoinositide 3-kinase and mitogen-activated protein kinase pathways which both promote cell survival and proliferation. By inhibiting EGFR activation, Olmutinib attenuates the activation of these tumor-promoting pathways. In the first phase I/II clinical study of Osimertinib, 800 mg/ day was chosen as the dose for subsequent studies, and the dose-limiting toxicity and maximum tolerated dose was not reached. Olmutinib received breakthrough therapy designation in the United States in December 2015 and was approved for use in Korea in May 2016.

Cys(Npys)-TAT(47-57)为TAT多肽中的一个段，可通过静电相互作用与质粒DNA结合。该段对应TAT的转导域，并含有活化的C端半胱氨酸残基。TAT为HIV-1编码的一种核转录激活蛋白。

BBO-8520 是首创的直接双重抑制剂，能够同时抑制 KRASG12C 的活化态（ON）与失活态（OFF）。BBO-8520 结合于 KRASG12C 的 Switch-II/Helix3 口袋，并通过共价修饰靶点半胱氨酸残基，进而阻断活化态下的效应子结合。BBO-8520 在生长因子激活条件下可强效抑制 KRAS 信号传导，而现有仅作用于 OFF 态的抑制剂活性有限。在体内实验中，BBO-8520 能快速结合靶点并抑制信号，从而在多种模型中实现持久的肿瘤回缩，包括对 OFF 态抑制剂耐药的模型。