Donald E. Bierer

Enhancing cyclic peptide functionality with hydrophilic diamino acids for improved APC-Asef interaction inhibition

Shipeng He, Jie Ping Zhong, Zhifeng Yu, Haohao Bai et autres

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Enhancing Cyclic Peptide Functionality with Hydrophilic Diamino Acids for Improved Apc-Asef Interaction Inhibition

Shipeng He, Jie Ping Zhong, Ziqiang Yu, Haohao Bai et autres

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Author response for "Cyclobutane-bearing restricted anchoring residues enabled geometry-specific hydrocarbon peptide stapling"

Honggang Hu, Baobao Chen, Chao Liu, Wei Cong et autres

Rational design of highly stabilized and selective adrenomedullin analogs

Eva‐Maria Jülke, Jan‐Patrick Fischer, Sylvia Els‐Heindl, Donald E. Bierer et autres

The peptide hormone adrenomedullin (ADM) consists of 52 amino acids with a disulfide bond and an amidated C‐terminus. Due to the vasodilatory and cardioprotective effects, the agonistic activity of the peptide on the adrenomedullin 1 receptor (AM1R) is of high pharmacological interest. …

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New Generation of sGC Stimulators: Discovery of Imidazo[1,2-a]pyridine Carboxamide BAY 1165747 (BAY-747), a Long-Acting Soluble Guanylate Cyclase Stimulator for the Treatment of Resistant Hypertension

Alexandros Vakalopoulos, Frank Wunder, Ingo Volker Hartung, Gorden Redlich et autres

Herein, we describe the identification, chemical optimization, and preclinical characterization of novel soluble guanylate cyclase (sGC) stimulators. Given the very broad therapeutic opportunities for sGC stimulators, new tailored molecules for distinct indications with specific pharmacokinetics, tissue distribution, and physicochemical properties will be …

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Synthesis of disulfide surrogate peptides incorporating an ethylene glycol bridge

Xiao‐Xiong Wei, Jibin Cui, Rui Zhao, Jie Luo et autres

We report a new diaminodiacid containing an ethylene glycol bridge for the synthesis of disulfide surrogate peptides.

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Cyclobutane-bearing restricted anchoring residues enabled geometry-specific hydrocarbon peptide stapling

Baobao Chen, Chao Liu, Wei Cong, Fei Gao et autres

geometry-specific stapled peptides indeed exhibit higher α-helicity and thus stronger biological activity than canonical hydrocarbon stapled peptides. We believe that this methodology possesses great potential to expand the scope of the existing peptide stapling strategy. These cyclobutane-bearing restricted anchoring residues served as …

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Single‐Shot Solid‐Phase Synthesis of Full‐Length H2 Relaxin Disulfide Surrogates

Rui Jie Zhao, Pan Shi, Jibin Cui, Chaowei Shi et autres

Chemical synthesis of insulin superfamily proteins (ISPs) has recently been widely studied to develop next-generation drugs. Separate synthesis of multiple peptide fragments and tedious chain-to-chain folding are usually encountered in these studies, limiting accessibility to ISP derivatives. Here we report the finding …

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Single‐Shot Solid‐Phase Synthesis of Full‐Length H2 Relaxin Disulfide Surrogates

Rui Jie Zhao, Pan Shi, Jibin Cui, Chaowei Shi et autres

Abstract Chemical synthesis of insulin superfamily proteins (ISPs) has recently been widely studied to develop next‐generation drugs. Separate synthesis of multiple peptide fragments and tedious chain‐to‐chain folding are usually encountered in these studies, limiting accessibility to ISP derivatives. Here we report the …

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Pinpointing the interaction site between semaphorin‐3A and its inhibitory peptide

Kevin Kretschmer, Jan Stichel, Kathrin Bellmann‐Sickert, Lars Baumann et autres

Semaphorin-3A (Sema-3A) is a chemorepellant protein with various biological functions, including kidney development. It interacts with a protein complex consisting of the receptors neuropilin-1 (NRP-1) and plexin-A1. After acute kidney injury, Sema-3A is overexpressed and secreted, leading to a loss of kidney …

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CCDC 2102965: Experimental Crystal Structure Determination

Qiupeng Peng, Bingjia Yan, Fangyi Li, Ming Lang et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Biomimetic enantioselective synthesis of β,β-difluoro-α-amino acid derivatives

Qiupeng Peng, Bingjia Yan, Fangyi Li, Ming Lang et autres

Although utilization of fluorine compounds has a long history, synthesis of chiral fluorinated amino acid derivatives with structural diversity and high stereoselectivity is still very appealing and challenging. Here, we report a biomimetic study of enantioselective [1,3]-proton shift of β,β-difluoro-α-imine amides catalyzed …

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