Publications by Sangram Shivdas Kale

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

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

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

Christian Heinis, Gerardo Turcatti, Julien Bortoli Chapalay, Xudong Kong, Van Manh Pham, Patrick Andreas Gonschorek, Jonathan Patrice Vesin, Sangram Shivdas Kale, Milan Bergeron-Brlek, 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, Xudong Kong, Alessandro Zorzi, Sangram Shivdas Kale, Camille Villequey

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