Fragment-to-lead medicinal chemistry publications in 2021

L Walsh, DA Erlanson, IJP de Esch… - Journal of medicinal …, 2023 - ACS Publications
This Perspective is the seventh in an annual series that summarizes successful Fragment-to-
Lead (F2L) case studies published in a given year. A tabulated summary of relevant articles …

Soluble TIM-3 as a biomarker of progression and therapeutic response in cancers and other of human diseases

C Bailly, X Thuru, L Goossens, JF Goossens - Biochemical pharmacology, 2023 - Elsevier
Immune checkpoints inhibition is a privileged approach to combat cancers and other human
diseases. The TIM-3 (T cell immunoglobulin and mucin-domain containing-3) inhibitory …

Identification of a small-molecule Tim-3 inhibitor to potentiate T cell–mediated antitumor immunotherapy in preclinical mouse models

S Ma, Y Tian, J Peng, C Chen, X Peng, F Zhao… - Science Translational …, 2023 - science.org
T cell immunoglobulin and mucin-containing molecule 3 (Tim-3), expressed in dysfunctional
and exhausted T cells, has been widely acknowledged as a promising immune checkpoint …

Brief report: Gender identity differences in autistic adults: Associations with perceptual and socio-cognitive profiles

RJ Walsh, L Krabbendam, J Dewinter… - Journal of autism and …, 2018 - Springer
Prior research has shown an elevation in autism traits and diagnoses in individuals seen for
gender related consultation and in participants self-identifying as transgender. To …

Glycoproteomic landscape and structural dynamics of TIM family immune checkpoints enabled by mucinase SmE

J Chongsaritsinsuk, AD Steigmeyer… - Nature …, 2023 - nature.com
Mucin-domain glycoproteins are densely O-glycosylated and play critical roles in a host of
biological functions. In particular, the T cell immunoglobulin and mucin-domain containing …

Discovery of small-molecule TIM-3 inhibitors for acute myeloid leukemia using pharmacophore-based virtual screening

SA Abdel-Rahman, V Talagayev, S Pach… - Journal of Medicinal …, 2023 - ACS Publications
T-cell immunoglobulin and mucin domain 3 (TIM-3) is a negative immune checkpoint that
represents a promising target for cancer immunotherapy. Although encouraging results have …

[HTML][HTML] Therapeutic potential of induced iron depletion using iron chelators in Covid-19

PP Naseef, M Elayadeth-Meethal, KTM Salim… - Saudi Journal of …, 2022 - Elsevier
Ferritin, which includes twenty-four light and heavy chains in varying proportions in different
tissues, is primarily responsible for maintaining the body's iron metabolism. Its normal value …

Sifting through the Noise: A Survey of Diffusion Probabilistic Models and Their Applications to Biomolecules

T Norton, D Bhattacharya - Journal of Molecular Biology, 2024 - Elsevier
Diffusion probabilistic models have made their way into a number of high-profile
applications since their inception. In particular, there has been a wave of research into using …

Modulation of the Gal-9/TIM-3 immune checkpoint with α-lactose. Does anomery of lactose matter?

C Bailly, X Thuru, B Quesnel - Cancers, 2021 - mdpi.com
Simple Summary The disaccharide lactose is a common excipient in pharmaceutical
products. In addition, the two anomers α-and β-lactose can exert immuno-modulatory effects …

Contribution of the TIM-3/Gal-9 immune checkpoint to tropical parasitic diseases

C Bailly - Acta Tropica, 2023 - Elsevier
Neglected tropical parasitic diseases (NTD) are prevalent in many countries and cost-
effective treatments remain urgently needed. Novel approaches have been proposed to …