Pharmaceutical biotechnology最新文献_第8页

LHRH agonists. 激动剂。

Pharmaceutical biotechnology Pub Date : 1998-01-01 DOI: 10.1007/0-306-47384-4_8

K W Funk, J Greer, A L Adjei

引用次数: 0

LHRH agonists.

Pharmaceutical biotechnology Pub Date : 1998-01-01 DOI: 10.1093/humrep/3.suppl_1.2

K. Funk, J. Greer, A. Adjei

引用次数: 5

Discovery and development of somatostatin agonists. 生长抑素激动剂的发现与发展。

Pharmaceutical biotechnology Pub Date : 1998-01-01 DOI: 10.1007/0-306-47384-4_9

P Marbach, W Bauer, D Bodmer, U Briner, C Bruns, A Kay, I Lancranjan, J Pless, F Raulf, R Robison, J Sharkey, T Soranno, B Stolz, P Vit, G Weckbecker

引用次数: 10

Discovery and development of novel melanogenic drugs. Melanotan-I and -II. 新型黑色素药物的发现与开发。黑色素- i和-II。

Pharmaceutical biotechnology Pub Date : 1998-01-01 DOI: 10.1007/0-306-47384-4_25

M E Hadley, V J Hruby, J Blanchard, R T Dorr, N Levine, B V Dawson, F al-Obeidi, T K Sawyer

引用次数: 26

LHRH antagonists. LHRH拮抗剂。

Pharmaceutical biotechnology Pub Date : 1998-01-01 DOI: 10.1007/0-306-47384-4_7

F Haviv, E N Bush, J Knittle, J Greer

{"title":"LHRH antagonists.","authors":"F Haviv, E N Bush, J Knittle, J Greer","doi":"10.1007/0-306-47384-4_7","DOIUrl":"https://doi.org/10.1007/0-306-47384-4_7","url":null,"abstract":"<p><p>After almost two decades, the research on LHRH antagonists has produced a number of decapeptides that are currently in clinical studies. The structures of these antagonists, unlike the agonists, differ substantially from that of LHRH. Five of the ten amino acids are unnatural and of D configuration. The structural combination of a hydrophobic N-terminus (residues 1, 2, and 3) and a basic/hydrophilic C-terminus (residues 6 and 8) was thought to be responsible for some HR reactions encountered with the second generation of LHRH antagonists. This side effect was greatly reduced by substituting the appropriate combination of amino acids at positions 5, 6, and 8. The next hurdle in the drug development of LHRH antagonists was solubility and aggregation. In the case of A-75998, water solubility was improved by 12- to 25-fold via substitution of NMeTyr at position 5. However, based on DLS analysis, the aqueous solutions still contained some large aggregates that were not visible to the naked eye. This formation of aggregates was eliminated on formulating A-75998 in Encapsin. In men, a single s.c. dose of 2 mg of A-75998 suppressed T to the castrate levels for over 30 hr. Other LHRH antagonists including ganirelix and cetrorelix are also in phase I/II clinical studies. Clinical studies with cetrorelix in prostate cancer; in vitro fertilization, and benign prostate hypotrophy have been reported.</p>","PeriodicalId":19777,"journal":{"name":"Pharmaceutical biotechnology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1998-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/0-306-47384-4_7","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20673631","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Factors impacting the delivery of therapeutic levels of pyrone-based HIV protease inhibitors. 影响以吡咯酮为基础的HIV蛋白酶抑制剂治疗水平递送的因素。

Pharmaceutical biotechnology Pub Date : 1998-01-01 DOI: 10.1007/0-306-47384-4_10

G E Padbury, G L Zipp, F J Schwende, Z Zhao, K A Koeplinger, K T Chong, T J Raub, S Thaisrivongs

引用次数: 4

The integration of medicinal chemistry, drug metabolism, and pharmaceutical research and development in drug discovery and development. The story of Crixivan, an HIV protease inhibitor. 药物化学，药物代谢和药物研究与开发在药物发现和开发中的整合。HIV蛋白酶抑制剂Crixivan的故事。

Pharmaceutical biotechnology Pub Date : 1998-01-01 DOI: 10.1007/0-306-47384-4_11

J H Lin, D Ostovic, J P Vacca

引用次数: 21

Orally active growth hormone secretagogues. 口服活性生长激素促分泌剂。

Pharmaceutical biotechnology Pub Date : 1998-01-01 DOI: 10.1007/0-306-47384-4_23

A A Patchett, R G Smith, M J Wyvratt

引用次数: 3

Renin inhibitors. 肾素抑制剂。

Pharmaceutical biotechnology Pub Date : 1998-01-01 DOI: 10.1007/0-306-47384-4_2

S H Rosenberg, H D Kleinert

引用次数: 1

Discovery and development of GG745, a potent inhibitor of both isozymes of 5 alpha-reductase. 5 α -还原酶同工酶的有效抑制剂GG745的发现和开发。

Pharmaceutical biotechnology Pub Date : 1998-01-01 DOI: 10.1007/0-306-47384-4_17

S V Frye, H N Bramson, D J Hermann, F W Lee, A K Sinhababu, G Tian

引用次数: 27