Cangming Yang

Publications (2)5.3 Total impact

• Article: Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.

  Zhicai Wu, Cangming Yang, Yusheng Xiong, Zhe Feng, Matthew Lombardo, Andreas Verras, Renee M Chabin, Suoyu Xu, Xinchun Tong, Dan Xie, [......], Margarita M Garcia-Calvo, Wayne Geissler, Zhu Shen, Qing Chen, Ranabir Sinharoy, Jeffrey J Hale, James R Tata, Shirly Pinto, Dong-Ming Shen, Steven L Colletti
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  ABSTRACT: Efforts to modify the central proline portion of lead compound 4 lead to the discovery of novel prolylcarboxypeptidase (PrCP) inhibitors. Especially, replacement with alanine afforded compound 19 displaying more potent human and mouse PrCP inhibitory activity than 4 and an overall comparable profile.
  Bioorganic & medicinal chemistry letters 02/2012; 22(4):1774-8. · 2.65 Impact Factor
• Article: Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.

  Zhicai Wu, Cangming Yang, Thomas H Graham, Andreas Verras, Renee M Chabin, Suoyu Xu, Xinchun Tong, Dan Xie, Mike E Lassman, Urmi R Bhatt, Margarita M Garcia-Calvo, Zhu Shen, Qing Chen, Kelly Bleasby, Ranabir Sinharoy, Jeffrey J Hale, James R Tata, Shirly Pinto, Steven L Colletti, Dong-Ming Shen
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  ABSTRACT: Efforts were dedicated to develop potent and brain penetrant prolylcarboxypeptidase (PrCP) inhibitors by replacing the amide group of original leads 1 and 2 with heterocycles. Aminopyrimidines including compound 32a were identified to display good PrCP inhibitory activity (32a, IC(50)=43 nM) and impressive ability to penetrate brain in mice (brain/plasma ratio: 1.4).
  Bioorganic & medicinal chemistry letters 02/2012; 22(4):1727-30. · 2.65 Impact Factor