Science Academy of India (Regd.), Palavantangal, Chennai - 600114, India.
School of Chemical Sciences, Mahatma Gandhi University, Priyadarshini Hills, Kottayam, Kerala - 686560, India.
Curr Med Chem. 2019;26(13):2330-2355. doi: 10.2174/0929867324666171012103559.
Peptide therapeutics has made tremendous progress in the past decade. Many of the inherent weaknesses of peptides which hampered their development as therapeutics are now more or less effectively tackled with recent scientific and technological advancements in integrated drug discovery settings. These include recent developments in synthetic organic chemistry, high-throughput recombinant production strategies, highresolution analytical methods, high-throughput screening options, ingenious drug delivery strategies and novel formulation preparations. Here, we will briefly describe the key methodologies and strategies used in the therapeutic peptide development processes with selected examples of the most recent developments in the field. The aim of this review is to highlight the viable options a medicinal chemist may consider in order to improve a specific pharmacological property of interest in a peptide lead entity and thereby rationally assess the therapeutic potential this class of molecules possesses while they are traditionally (and incorrectly) considered 'undruggable'.
在过去的十年中，肽治疗学取得了巨大的进展。许多阻碍肽作为治疗药物发展的固有弱点，现在或多或少地通过综合药物发现环境中的最新科学和技术进步得到了有效解决。这些进步包括合成有机化学、高通量重组生产策略、高分辨率分析方法、高通量筛选选择、巧妙的药物输送策略和新颖的制剂制备方面的进展。在这里，我们将简要描述治疗性肽开发过程中使用的关键方法和策略，并选择该领域的最新进展作为示例。本文的目的是强调药物化学家在改善肽先导化合物的特定药理性质时可能考虑的可行选择，从而合理评估此类分子的治疗潜力，尽管它们传统上（且不正确）被认为是“不可成药”的。
