Patchett A, Harris E, Tristram E, Wyvratt M, Wu M, Taub D, Peterson E, Ikeler T, ten Broeke J, Payne L, Ondeyka D, Thorsett E, Greenlee W, Lohr N, Hoffsommer R, Joshua H, Ruyle W, Rothrock J, Aster S, Maycock A, Robinson F, Hirschmann R, Sweet C, Ulm E, Gross D, Vassil T, Stone C (1980). "A new class of angiotensin-converting enzyme inhibitors". Nature 288 (5788): 280-3. PMID 6253826. doi:10.1038/288280a0. ...

آنزیم ۲ مبدل آنژیوتانسین (به انگلیسی: Angiotensin-converting enzyme 2) یا به اختصار ACE2، یک اگزوپپتیداز است که موجب تبدیل آنژیوتانسین ۱ به «آنژیوتانسین ۹-۱» (نُه پپتیدی)،[۳] یا تبدیل آنژیوتانسین ۲ به «آنژیوتانسین ۷-۱» می‌گردد.[۴][۵] این آنزیم اثرات مستقیمی بر عملکرد قلب دارد،a و بیشتر در لایهٔ داخلی رگ‌های خونی، قلب و کلیه‌ها بیان می‌شود.[۶] داروهای بازدارندهٔ آنزیم مبدل آنژیوتانسین که در درمان فشار خون بالا استفاده می‌شوند، اثری بر آنزیم ACE2 ندارند.[۷] مشخص شده که گیرنده‌های ACE2، نقطهٔ ورود برخی از انواع کروناویروس‌ها به سلول‌های بدن انسان هستند.[۸] دو گروه مجزا از ...

Sheer Heart Attack》은 1974년 11월 8일 영국의 EMI 레코드와 미국의 엘렉트라 레코드에 의해 발매된 영국의 록 밴드 퀸의 세 번째 스튜디오 음반이다. 그들의 첫 두 음반에 수록된 프로그레시브 주제에서 발췌한 이 음반은 더 전통적인 록 트랙을 특징으로 하고 "클래식" 퀸 사운드를 향한 발걸음을 내디뎠다.[1] 그 음반은 밴드와 로이 토머스 베이커에 의해 제작되었고 영국과 전 세계에서 퀸을 주류로 만들었다. 이 음반의 첫 번째 싱글 음반인 〈Killer Queen〉은 영국 차트에서 2위에 올랐고 빌보드 싱글 차트에서 12위를 차지하며 미국에서 그들의 첫 번째 톱 20 히트곡을 제공했다. 《Sheer Heart Attack》은 1975년에 12위를 차지하며 미국 탑 20을 기록한 첫 번째 퀸 음반이었다. 이 음반은 "뛰어난 하드 록 기타 트랙"을 많이 포함하고 있는 것으로 인정받았다.[2] 돌이켜 보면, 이 ...

... s (ARBs), also known as angiotensin II receptor antagonists , AT1 receptor antagonists or sartans, are a group of pharmaceuticals that modulate the renin-angiotensin system. Their main uses are in the treatment of hypertension (high blood pressure), diabetic nephropathy (kidney damage due to diabetes) and congestive heart failure. They block the activation of AT1 receptors, preventing the binding of angiotensin II. Angiotensin II receptor blockers are used primarily for the treatment of hypertension where the patient is intolerant of ACE inhibitor therapy. They do not inhibit the breakdown of bradykinin or other kinins, and are thus only rarely associated with the persistent dry cough and/or angioedema that limit ACE inhibitor therapy.[citation needed] More recently, they have ...

... (rINN) /ˌkændɪˈsɑːrtən/ is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. The prodrug candesartan cilexetil is marketed by AstraZeneca and Takeda Pharmaceuticals, commonly under the trade names Diceran,Blopress, Atacand, Amias, and Ratacand. It is available in generic form. As with other angiotensin II receptor antagonists, candesartan is indicated for the treatment of hypertension. Results from the CHARM study (early 2000s) demonstrated the morbidity and mortality reduction benefits of candesartan therapy in congestive heart failure. Thus, while ACE inhibitors are still considered first-line therapy in heart failure, candesartan can be used in combination with an ACE to achieve improved mortality and morbidity vs. an ACE alone and additionally is an alternative in patients intolerant of ACE ...

... is an ACE inhibitor used to treat high blood pressure, it may also be used to treat other conditions. It is marketed by Abbott Laboratories under the brand name Mavik. Trandolapril is a prodrug that is de-esterified to trandolaprilat. It is believed to exert its antihypertensive effect through the renin-angiotensin-aldosterone system. Trandolapril has a half-life of about 6 hours, and trandolaprilat has a half life of about 10 h. Trandolaprilat has about eight times the activity of its parent drug. About one-third of trandolapril and its metabolites are excreted in the urine, and about two-thirds of trandolapril and its metabolites are excreted in the feces. Serum protein binding of trandolapril is about 80%. Trandolapril acts by competitive inhibition of angiotensin converting enzyme (ACE), a key enzyme in the renin-angiotensin system which plays an ...

... (marketed under the brand name Accupril by Pfizer) is an angiotensin-converting enzyme inhibitor (ACE inhibitor) used in the treatment of hypertension and congestive heart failure. A prodrug, it is converted to its active metabolite, quinaprilat, in the liver. Quinapril inhibits angiotensin converting enzyme, an enzyme which catalyses the formation of angiotensin II from its precursor, angiotensin I. Angiotensin II is a powerful vasoconstrictor and increases blood pressure through a variety of mechanisms. Due to reduced angiotensin production, plasma concentrations of aldosterone are also reduced, resulting in increased excretion of sodium in the urine and increased concentrations of potassium in the blood. Quinapril is indicated for the treatment of high blood pressure ...

... , brand name Lotensin (Novartis), is an ACE inhibitor used primarily in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing the renal and retinal complications of diabetes. ACE inhibitors relax blood vessels, and decrease blood volume, which lowers blood pressure and decreases oxygen demand from the heart. They inhibit angiotensin-converting enzyme, which is part of the renin-angiotensin-aldosterone system. Benazepril is a prodrug which is metabolized by the liver into its active form benazeprilat via cleavage of the drug's ester group. Patients with advanced renal insufficiency taking benazepril show "substantial" kidney benefits. A long-term study of patients' ...

... hydrochloride is a potent orally active nonsulfhydryl angiotensin converting enzyme inhibitor (ACE inhibitor) which is used for the treatment of hypertension and congestive heart failure. Moexipril can be administered alone or with other antihypertensives or diuretics. It works by inhibiting the conversion of angiotensin I to angiotensin II. Moexipril is available from Schwarz Pharma under the trade name Univasc. Moexipril is available as a prodrug moexipril hydrochloride, and is metabolized in the liver to form the pharmacologically active compound moexiprilat. Formation of moexiprilat is caused by hydrolysis of an ethyl ester group. Moexipril is incompletely absorbed after oral administration, and its bioavailability is low. The long pharmacokinetic half-life and persistent ACE inhibition of moexipril allows once-daily administration. Moexipril is ...

Common adverse drug reactions include: hypotension, cough, hyperkalemia, headache, dizziness, fatigue, nausea, and kidney impairment.[21][22] ACE inhibitors might increase inflammation-related pain, perhaps mediated by the buildup of bradykinin that accompanies ACE inhibition.[23][24][25]. The main adverse effects of ACE inhibition can be understood from their pharmacological action. The other reported adverse effects are hepatotoxicity and effect on the fetus.[22] Renal impairment is a significant potential adverse effect of all ACE inhibitors that directly follows from their mechanism of action. Patients starting on an ACE inhibitor usually have a modest reduction in glomerular filtration rate (GFR) that stabilizes after several days. However, the decrease may be significant in conditions of decreased renal perfusion, such as renal artery stenosis, heart ...

First-line therapy for people with heart failure due to reduced systolic function should include angiotensin-converting enzyme (ACE) inhibitors (ACE-I) or angiotensin receptor blockers (ARBs) if the person develops a long term cough as a side effect of the ACE-I.[60] Use of medicines from this class is associated with improved survival and quality of life in people with heart failure.[61]. Beta-adrenergic blocking agents (beta blockers) also form part of the first line of treatment, adding to the improvement in symptoms and mortality provided by ACE-I/ARB.[61][62] The mortality benefits of beta blockers in people with systolic dysfunction who also have atrial fibrillation (AF) is more limited than in those who do not have AF.[63] If the ejection fraction is not diminished (HFpEF), the benefits of beta blockers is more modest; a decrease in mortality has ...

As enzymes have evolved to bind their substrates tightly, and most reversible inhibitors bind in the active site of enzymes, it is unsurprising that some of these inhibitors are strikingly similar in structure to the substrates of their targets. Inhibitors of DHFR are prominent examples[2][3][1]. Other example of these substrate mimics are the protease inhibitors, a very successful class of antiretroviral drugs used to treat HIV.[24] The structure of ritonavir, a protease inhibitor based on a peptide and containing three peptide bonds, is shown on the right. As this drug resembles the protein that is the substrate of the HIV protease, it competes with this substrate in the enzyme's active site. Enzyme inhibitors are often designed to mimic the transition state or intermediate of an enzyme-catalyzed reaction. This ensures that the inhibitor exploits the transition state ...

آنزیم ۲ مبدل آنژیوتانسین (به انگلیسی: Angiotensin-converting enzyme 2) یا به اختصار ACE2، یک اگزوپپتیداز است که موجب تبدیل آنژیوتانسین ۱ به «آنژیوتانسین ۹-۱» (نُه پپتیدی)،[۳] یا تبدیل آنژیوتانسین ۲ به «آنژیوتانسین ۷-۱» می‌گردد.[۴][۵] این آنزیم اثرات مستقیمی بر عملکرد قلب دارد،a و بیشتر در لایهٔ داخلی رگ‌های خونی، قلب و کلیه‌ها بیان می‌شود.[۶] داروهای بازدارندهٔ آنزیم مبدل آنژیوتانسین که در درمان فشار خون بالا استفاده می‌شوند، اثری بر آنزیم ACE2 ندارند.[۷] مشخص شده که گیرنده‌های ACE2، نقطهٔ ورود برخی از انواع کروناویروس‌ها به سلول‌های بدن انسان هستند.[۸] دو گروه مجزا از ...