Macrocyclic peptides as drug candidates: recent progress and remaining challenges

AA Vinogradov, Y Yin, H Suga - Journal of the American Chemical …, 2019 - ACS Publications
Peptides as a therapeutic modality attract much attention due to their synthetic accessibility,
high degree of specific binding, and the ability to target protein surfaces traditionally …

Targeting transcription factors for cancer treatment

M Lambert, S Jambon, S Depauw… - Molecules, 2018 - mdpi.com
Transcription factors are involved in a large number of human diseases such as cancers for
which they account for about 20% of all oncogenes identified so far. For long time, with the …

Methods for generating and screening libraries of genetically encoded cyclic peptides in drug discovery

C Sohrabi, A Foster, A Tavassoli - Nature Reviews Chemistry, 2020 - nature.com
Drug discovery has traditionally focused on using libraries of small molecules to identify
therapeutic drugs, but new modalities, especially libraries of genetically encoded cyclic …

Cyclic peptides: Promising scaffolds for biopharmaceuticals

D Gang, DW Kim, HS Park - Genes, 2018 - mdpi.com
To date, small molecules and macromolecules, including antibodies, have been the most
pursued substances in drug screening and development efforts. Despite numerous …

B-cell lymphoma 6 inhibitors: current advances and prospects of drug development for diffuse Large b-cell lymphomas

H Gu, J He, Y Li, D Mi, T Guan, W Guo… - Journal of medicinal …, 2022 - ACS Publications
B-cell lymphoma 6 (BCL6) is a transcriptional repressor that regulates the differentiation of B
lymphocytes and mediates the formation of germinal centers (GCs) by recruiting …

Methodologies for backbone macrocyclic peptide synthesis compatible with screening technologies

K Shinbara, W Liu, RHP Van Neer, T Katoh… - Frontiers in …, 2020 - frontiersin.org
Backbone macrocyclic structures are often found in diverse bioactive peptides and
contribute to greater conformational rigidity, peptidase resistance, and potential membrane …

Progress toward B-cell lymphoma 6 BTB domain inhibitors for the treatment of diffuse large B-cell lymphoma and beyond

Y Ai, L Hwang, AD MacKerell Jr… - Journal of medicinal …, 2021 - ACS Publications
B-cell lymphoma 6 (BCL6) is a master regulator of germinal center formation that produce
antibody-secreting plasma cells and memory B-cells for sustained immune responses. The …

GSK137, a potent small-molecule BCL6 inhibitor with in vivo activity, suppresses antibody responses in mice

AC Pearce, MJ Bamford, R Barber, A Bridges… - Journal of Biological …, 2021 - ASBMB
B-cell lymphoma 6 (BCL6) is a zinc finger transcriptional repressor possessing a BTB–POZ
(BR-C, ttk, and bab for BTB; pox virus and zinc finger for POZ) domain, which is required for …

Structural diversity in de novo cyclic peptide ligands from genetically encoded library technologies

TE McAllister, OD Coleman, G Roper… - Peptide …, 2021 - Wiley Online Library
Cyclic peptides discovered by genetically encoded library technologies have emerged as a
class of promising molecules in chemical biology and drug discovery. Here we review the …

Genetically encoded cyclic peptide libraries: From hit to lead and beyond

J Valentine, A Tavassoli - Methods in enzymology, 2018 - Elsevier
With the increasing utilization of high-throughput screening for lead identification in drug
discovery, the need for easily constructed and diverse libraries which cover significant …