Pavel A. Savitsky

Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations

Rafael M. Couñago, F. Gama, Alessandra Mascarello, O. Gileadi et autres

The human genome encodes two active Vaccinia-related protein kinases (VRK), VRK1 and VRK2. These proteins have been implicated in a number of cellular processes and linked to a variety of tumors. However, understanding the cellular role of VRKs and establishing their potential …

us (code pays fourni par la source)

Multivalent Histone and DNA Engagement by a PHD/BRD/PWWP Triple Reader Cassette Recruits ZMYND8 to K14ac-Rich Chromatin

Colin R. Goding, Brian D. Strahl, Pavel A. Savitsky, Hans Friedrichsen et autres

Elucidation of interactions involving DNA and histone post-translational-modifications (PTMs) is essential for providing insight into complex biological functions. Reader assemblies connected via flexible linkages facilitate avidity and increase affinity, however little is known of the contribution to the recognition process of multiple …

us (code pays fourni par la source)

Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains

Jean‐Philippe Lambert, S. Picaud, Takao Fujisawa, Huayun Hou et autres

Targeting bromodomains (BRDs) of the bromo-and-extra-terminal (BET) family offers opportunities for therapeutic intervention in cancer and other diseases. Here, we profile the interactomes of BRD2, BRD3, BRD4, and BRDT following treatment with the pan-BET BRD inhibitor JQ1, revealing broad rewiring of the …

ca, gb, ee, ch, us (code pays fourni par la source)

Direct interaction between the PRDM3 and PRDM16 tumor suppressors and the NuRD chromatin remodeling complex

Danton Ivanochko, Levon Halabelian, Elizabeth Henderson, Pavel A. Savitsky et autres

Aberrant isoform expression of chromatin-associated proteins can induce epigenetic programs related to disease. The MDS1 and EVI1 complex locus (MECOM) encodes PRDM3, a protein with an N-terminal PR-SET domain, as well as a shorter isoform, EVI1, lacking the N-terminus containing the PR-SET …

ca, gb (code pays fourni par la source)

Human SLK bound to a maleimide inhibitor

F.J. Sorrell, Benedict‐Tilman Berger, E. Salah, Ricardo A. M. Serafim et autres

Human Poly (Adp-Ribose) Polymerase Family Member 14 (Parp14); A Target Enabling Package

Marion Schuller, Christian Sieg, Kristein Uth, Kerstin Riedel et autres

This work provides reagents to develop specific inhibitors of the macrodomains of PARP14, for potential use for cancer and/or inflammation. Targeting the macrodomains of PARP14 is an alternative targeting strategy to PARP catalytic domain inhibitors that may allow greater inhibitor selectivity, and …

de, gb (code pays fourni par la source)

Human Poly (Adp-Ribose) Polymerase Family Member 14 (Parp14); A Target Enabling Package

Marion Schuller, Christian Sieg, Kristein Uth, Kerstin Riedel et autres

This work provides reagents to develop specific inhibitors of the macrodomains of PARP14, for potential use for cancer and/or inflammation. Targeting the macrodomains of PARP14 is an alternative targeting strategy to PARP catalytic domain inhibitors that may allow greater inhibitor selectivity, and …

de, gb (code pays fourni par la source)

Human Poly (Adp-Ribose) Polymerase Family Member 14 (Parp14); A Target Enabling Package

Marion Schuller, Christian Sieg, Kristein Uth, Kerstin Riedel et autres

This work provides reagents to develop specific inhibitors of the macrodomains of PARP14, for potential use for cancer and/or inflammation. Targeting the macrodomains of PARP14 is an alternative targeting strategy to PARP catalytic domain inhibitors that may allow greater inhibitor selectivity, and …

de, gb (code pays fourni par la source)

Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation

Julia C. Meier, C. Tallant, Oleg Fedorov, Hanna Witwicka et autres

Histone acetyltransferases of the MYST family are recruited to chromatin by BRPF scaffolding proteins. We explored functional consequences and the therapeutic potential of inhibitors targeting acetyl-lysine dependent protein interaction domains (bromodomains) present in BRPF1-3 in bone maintenance. We report three potent and …

gb, us, ca, de (code pays fourni par la source)

Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations

Rafael M. Couñago, C.K. Allerston, Pavel A. Savitsky, Hatylas F. Z de Azevedo et autres

The human genome encodes two active Vaccinia-related protein kinases (VRK), VRK1 and VRK2. These proteins have been implicated in a number of cellular processes and linked to a variety of tumors. However, understanding the cellular role of VRKs and establishing their potential …

br, gb, us (code pays fourni par la source)

Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins

Niall Igoe, Elliott D. Bayle, C. Tallant, Oleg Fedorov et autres

The bromodomain and plant homeodomain finger-containing (BRPF) family are scaffolding proteins important for the recruitment of histone acetyltransferases of the MYST family to chromatin. Here, we describe NI-57 (16) as new pan-BRPF chemical probe of the bromodomain (BRD) of the BRPFs. Inhibitor …

gb, se, de, us (code pays fourni par la source)

Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations

Rafael M. Couñago, C.K. Allerston, Pavel A. Savitsky, Hatylas F. Z de Azevedo et autres

ABSTRACT The human genome encodes two active Vaccinia-related protein kinases (VRK), VRK1 and VRK2. These proteins have been implicated in a number of cellular processes and linked to a variety of tumors. However, understanding the cellular role of VRKs and establishing their …

br, gb, us (code pays fourni par la source)