Identification and optimization of small molecule antagonists of vasoactive intestinal peptide receptor-1 (VIPR1)

…, A Roy, A Gupta, S Karmakar, T Karatt, A Mathur…

Index: Harikrishnan, Lalgudi S.; Srivastava, Neelam; Kayser, Lauren E.; Nirschl, David S.; K, Kumaragurubaran; Roy, Amrita; Gupta, Anuradha; Karmakar, Sukhen; Karatt, Tajudheen; Mathur, Arvind; Burford, Neil T.; Chen, Jing; Kong, Yan; Cvijic, Maryellen; Cooper, Christopher B.; Poss, Michael A.; Trainor, George L.; Wong, Tai W. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2287 - 2290

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Citation Number: 7

Abstract

In addition to inhibition of cancer cell proliferation, the VIPR1 antagonist SNH has been reported to potentiate the effect of various chemotherapeutic agents on the NSCLC NCI-H727 cell line. 6b Further, the VIP hybrid antagonist (neurotensin 6–11 VIP 7–28 ) has been shown to reduce tumor volume in vivo in mice. 6a Encouraged by the literature data as well as in-house siRNA experiments, 10 we decided to investigate VIPR1 as an oncology target. All the reported ...