Literature DB >> 23585920

Inhibition of Ras-Effector Interaction by Cyclic Peptides.

Xianghong Wu1, Punit Upadhyaya, Miguel A Villalona-Calero, Roger Briesewitz, Dehua Pei.   

Abstract

A combinatorial library of 6 × 106 cyclic peptides was synthesized in the one bead-two compound format, with each bead displaying a unique cyclic peptide on its surface and a linear peptide encoding tag in its interior. Screening of the library against K-Ras identified compounds that bound K-Ras with submicromolar affinity and disrupted its interaction with effector proteins.

Entities:  

Year:  2013        PMID： 23585920      PMCID： PMC3621770          DOI： 10.1039/C2MD20329D

Source DB:  PubMed          Journal:  Medchemcomm        ISSN： 2040-2503            Impact factor:   3.597


  23 in total

1.  Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity.

Authors:  Till Maurer; Lindsay S Garrenton; Angela Oh; Keith Pitts; Daniel J Anderson; Nicholas J Skelton; Benjamin P Fauber; Borlan Pan; Shiva Malek; David Stokoe; Mary J C Ludlam; Krista K Bowman; Jiansheng Wu; Anthony M Giannetti; Melissa A Starovasnik; Ira Mellman; Peter K Jackson; Joachim Rudolph; Weiru Wang; Guowei Fang
Journal:  Proc Natl Acad Sci U S A       Date:  2012-03-19       Impact factor: 11.205

2.  Homogeneous time-resolved fluorescence-based assay to screen for ligands targeting the growth hormone secretagogue receptor type 1a.

Authors:  Jean-Philippe Leyris; Thomas Roux; Eric Trinquet; Pascal Verdié; Jean-Alain Fehrentz; Nadia Oueslati; Stéphanie Douzon; Emmanuel Bourrier; Laurent Lamarque; Didier Gagne; Jean-Claude Galleyrand; Céline M'kadmi; Jean Martinez; Sophie Mary; Jean-Louis Banères; Jacky Marie
Journal:  Anal Biochem       Date:  2010-09-24       Impact factor: 3.365

Review 3.  Targeting Ras and Rho GTPases as opportunities for cancer therapeutics.

Authors:  Katharine Walker; Michael F Olson
Journal:  Curr Opin Genet Dev       Date:  2005-02       Impact factor: 5.578

Review 4.  The Ras superfamily at a glance.

Authors:  Krister Wennerberg; Kent L Rossman; Channing J Der
Journal:  J Cell Sci       Date:  2005-03-01       Impact factor: 5.285

5.  A gene expression signature associated with "K-Ras addiction" reveals regulators of EMT and tumor cell survival.

Authors:  Anurag Singh; Patricia Greninger; Daniel Rhodes; Louise Koopman; Sheila Violette; Nabeel Bardeesy; Jeff Settleman
Journal:  Cancer Cell       Date:  2009-06-02       Impact factor: 31.743

6.  Traceless capping agent for peptide sequencing by partial edman degradation and mass spectrometry.

Authors:  Amit Thakkar; Anne-Sophie Wavreille; Dehua Pei
Journal:  Anal Chem       Date:  2006-08-15       Impact factor: 6.986

7.  Activated Kras and Ink4a/Arf deficiency cooperate to produce metastatic pancreatic ductal adenocarcinoma.

Authors:  Andrew J Aguirre; Nabeel Bardeesy; Manisha Sinha; Lyle Lopez; David A Tuveson; James Horner; Mark S Redston; Ronald A DePinho
Journal:  Genes Dev       Date:  2003-12-17       Impact factor: 11.361

8.  On-bead screening of combinatorial libraries: reduction of nonspecific binding by decreasing surface ligand density.

Authors:  Xianwen Chen; Pauline H Tan; Yanyan Zhang; Dehua Pei
Journal:  J Comb Chem       Date:  2009 Jul-Aug

9.  An orthosteric inhibitor of the Ras-Sos interaction.

Authors:  Anupam Patgiri; Kamlesh K Yadav; Paramjit S Arora; Dafna Bar-Sagi
Journal:  Nat Chem Biol       Date:  2011-07-17       Impact factor: 15.040

10.  Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation.

Authors:  Qi Sun; Jason P Burke; Jason Phan; Michael C Burns; Edward T Olejniczak; Alex G Waterson; Taekyu Lee; Olivia W Rossanese; Stephen W Fesik
Journal:  Angew Chem Int Ed Engl       Date:  2012-05-08       Impact factor: 15.336
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  17 in total

Review 1.  Targeting Ras with Macromolecules.

Authors:  Dehua Pei; Kuangyu Chen; Hui Liao
Journal:  Cold Spring Harb Perspect Med       Date:  2018-03-01       Impact factor: 6.915

2.  Targeting the α4-α5 interface of RAS results in multiple levels of inhibition.

Authors:  Russell Spencer-Smith; Lie Li; Sheela Prasad; Akiko Koide; Shohei Koide; John P O'Bryan
Journal:  Small GTPases       Date:  2017-12-31

3.  Xenoprotein engineering via synthetic libraries.

Authors:  Zachary P Gates; Alexander A Vinogradov; Anthony J Quartararo; Anupam Bandyopadhyay; Zi-Ning Choo; Ethan D Evans; Kathryn H Halloran; Alexander J Mijalis; Surin K Mong; Mark D Simon; Eric A Standley; Evan D Styduhar; Sarah Z Tasker; Faycal Touti; Jessica M Weber; Jessica L Wilson; Timothy F Jamison; Bradley L Pentelute
Journal:  Proc Natl Acad Sci U S A       Date:  2018-05-21       Impact factor: 11.205

4.  Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices.

Authors:  Elizaveta S Leshchiner; Andrey Parkhitko; Gregory H Bird; James Luccarelli; Joseph A Bellairs; Silvia Escudero; Kwadwo Opoku-Nsiah; Marina Godes; Norbert Perrimon; Loren D Walensky
Journal:  Proc Natl Acad Sci U S A       Date:  2015-01-26       Impact factor: 11.205

Review 5.  Macrocycles as protein-protein interaction inhibitors.

Authors:  Patrick G Dougherty; Ziqing Qian; Dehua Pei
Journal:  Biochem J       Date:  2017-03-15       Impact factor: 3.857

Review 6.  Personal Mutanomes Meet Modern Oncology Drug Discovery and Precision Health.

Authors:  Feixiong Cheng; Han Liang; Atul J Butte; Charis Eng; Ruth Nussinov
Journal:  Pharmacol Rev       Date:  2018-12-13       Impact factor: 25.468

7.  Discovery of a Bicyclic Peptidyl Pan-Ras Inhibitor.

Authors:  Marina Buyanova; Shurui Cai; Jahan Cooper; Curran Rhodes; Heba Salim; Ashweta Sahni; Punit Upadhyaya; Rui Yang; Amar Sarkar; Na Li; Qi-En Wang; Dehua Pei
Journal:  J Med Chem       Date:  2021-08-20       Impact factor: 8.039

8.  Inhibition of RAS function through targeting an allosteric regulatory site.

Authors:  Russell Spencer-Smith; Akiko Koide; Yong Zhou; Raphael R Eguchi; Fern Sha; Priyanka Gajwani; Dianicha Santana; Ankit Gupta; Miranda Jacobs; Erika Herrero-Garcia; Jacqueline Cobbert; Hugo Lavoie; Matthew Smith; Thanashan Rajakulendran; Evan Dowdell; Mustafa Nazir Okur; Irina Dementieva; Frank Sicheri; Marc Therrien; John F Hancock; Mitsuhiko Ikura; Shohei Koide; John P O'Bryan
Journal:  Nat Chem Biol       Date:  2016-11-07       Impact factor: 15.040

Review 9.  Direct inhibition of RAS: Quest for the Holy Grail?

Authors:  Russell Spencer-Smith; John P O'Bryan
Journal:  Semin Cancer Biol       Date:  2017-12-14       Impact factor: 15.707

Review 10.  Efforts to Develop KRAS Inhibitors.

Authors:  Matthew Holderfield
Journal:  Cold Spring Harb Perspect Med       Date:  2018-07-02       Impact factor: 6.915
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