Discovery, development, and cellular delivery of potent and selective bicyclic peptide inhibitors of Grb7 cancer target

GM Watson, K Kulkarni, J Sang, X Ma… - Journal of Medicinal …, 2017 - ACS Publications
… block Grb7 mediated interactions in a breast cancer cell line, … A nonphosphorylated
thioether-linked cyclic peptide 1, … even more potent Grb7SH2 domain bicyclic inhibitors. In this …

Evaluation of cyclic peptide inhibitors of the Grb7 breast Cancer target: small change in cargo results in large change in cellular activity

J Sang, K Kulkarni, GM Watson, X Ma, DJ Craik… - Molecules, 2019 - mdpi.com
… able to bind to the Grb7-SH2 domain with micromolar affinity [… the Grb7-SH2 domain over
other closely related SH2 domains … the peptides to SKBR-3 (HER2+ve breast cancer cell line) …

Insight into the selectivity of the G7-18NATE inhibitor peptide for the Grb7-SH2 domain target

GM Watson, WAH Lucas, MJ Gunzburg… - Frontiers in Molecular …, 2017 - frontiersin.org
… the binding of the cyclic peptide G7-18NATE to the Grb7-SH2 wild-… cyclic peptide inhibitors
that are able to inhibit proliferation and migration in breast cancer cell lines and reduce tumor

Enhancing the bioactivity of bicyclic peptides targeted to Grb7-SH2 by restoring cell permeability

NP Sturre, RN Colson, N Shah, GM Watson, X Yang… - Biomedicines, 2022 - mdpi.com
… that inhibiting the Grb7-SH2 domain would inhibit breast cancer cell migration as well as other
… This cyclic peptide is 11 amino acids in length (sequence: WFEGYDNTFPC) and is highly …

Unexpected involvement of staple leads to redesign of selective bicyclic peptide inhibitor of Grb7

MJ Gunzburg, K Kulkarni, GM Watson, ND Ambaye… - Scientific Reports, 2016 - nature.com
… in a number of breast cancer cell lines, primary breast tumors 12 … the crystal structure of
G7-B1 in complex with Grb7-SH2 domain, … We have previously shown that the cyclic peptide G7-…

Grb7, a critical mediator of EGFR/ErbB signaling, in cancer development and as a potential therapeutic target

PY Chu, YL Tai, TL Shen - Cells, 2019 - mdpi.com
SH2 domain of Grb7 in Grb7-mediated oncogenesis. Together, these studies emphasize the
critical role of the SH2 domain of Grb7 … -apoptotic effects on cancer cells [50]. Furthermore, …

Grb7-derived calmodulin-binding peptides inhibit proliferation, migration and invasiveness of tumor cells while they enhance attachment to the substrate

J Alcalde, M González-Muñoz, A Villalobo - Heliyon, 2020 - cell.com
… bound protein 7 (Grb7) is a modular Src homology domain 2 (SH2)-containing adaptor …
whether a peptide based on the CaM-BD of Grb7 could disrupt relevant tumor cell functions in …

[图书][B] Investigation of the Binding Interface between the Grb7SH2 and Grb7RAPH Domains

AK Biswas - 2021 - search.proquest.com
cancer cell lines overexpress Hax-1, a cytoskeletalassociated protein component. Grb7
interacts with Hax-1 by its RAPH domain … potential effect of Grb7 SH2 domain posttranslational …

Shortened penetratin cell-penetrating peptide is insufficient for cytosolic delivery of a Grb7 targeting peptide

GM Watson, K Kulkarni, R Brandt, MP Del Borgo… - ACS …, 2017 - ACS Publications
… an 11-residue cyclic peptide inhibitor, G7-18NATE, that … In HER2+ breast cancer cells, both
G7-18NATE-P16 and G7-… constructs could still bind to the Grb7-SH2 domain in vitro. For this, …

Synthesis of Grb2 SH2 domain proteins for mirror-image screening systems

T Noguchi, T Noguchi - … of Chemistry-Based Screening Platform for …, 2018 - Springer
… also employed to identify potent phosphorylated peptides [11] or cyclic peptides G1TE [12]. …
potent peptide ligands in the binding pockets of Grb2 SH2 domain [13], a number of inhibitors