Publications by Sangram Shivdas Kale

Picomole-Scale Synthesis and Screening of Macrocyclic Compound Libraries by Acoustic Liquid Transfer

Gerardo Turcatti, Jonathan Patrice Vesin, Christian Heinis, Alessandro Zorzi, Gontran Sangouard, Julien Bortoli Chapalay, Sangram Shivdas Kale, Mischa Schüttel, Yu Teng Wu, Cristina Diaz Perlas

Macrocyclic compounds are an attractive class of therapeutic ligands against challenging targets, such as protein-protein interactions. However, the development of macrocycles as drugs is hindered by the lack of large combinatorial macrocyclic libraries, w ...

Wiley-VCH Verlag GmbH2021

Macrocycle synthesis strategy based on step-wise “adding and reacting” three components enables screening of large combinatorial libraries

Gerardo Turcatti, Jonathan Patrice Vesin, Christian Heinis, Alessandro Angelini, Alessandro Zorzi, Julien Bortoli Chapalay, Sangram Shivdas Kale, Kaycie Marie Butler, Ganesh Kumar Mothukuri, Carl Leonard Stenbratt

Macrocycles provide an attractive modality for drug development, but generating ligands for new targets is hampered by the limited availability of large macrocycle libraries. We have established a solution-phase macrocycle synthesis strategy in which three ...

2020

Thiol-to-amine cyclization reaction enables screening of large libraries of macrocyclic compounds and the generation of sub-kilodalton ligands

Gerardo Turcatti, Jonathan Patrice Vesin, Christian Heinis, Van Manh Pham, Julien Bortoli Chapalay, Sangram Shivdas Kale, Xudong Kong, Milan Bergeron-Brlek, Patrick Andreas Gonschorek, João Miguel Franco Machado

Macrocyclic compounds are an attractive modality for drug development, but the limited availability of large, structurally diverse macrocyclic libraries hampers the discovery of leads. Here, we describe the discovery of efficient macrocyclization reactions ...

2019

Cyclization of peptides with two chemical bridges affords large scaffold diversities

Christian Heinis, Alessandro Zorzi, Camille Villequey, Sangram Shivdas Kale, Xudong Kong

2018

Polar Hinges as Functionalized Conformational Constraints in (Bi) cyclic Peptides

Christian Heinis, Sangram Shivdas Kale

Two polar hinges for cyclization of peptides have been developed, leading to bicyclic peptides and cyclized peptides with improved solubility and biological activity. Increasingly, we note that a good aqueous solubility of peptides is an absolute prerequis ...

Wiley-Blackwell2017