[HTML][HTML] The use of spirocyclic scaffolds in drug discovery

Y Zheng, CM Tice, SB Singh - Bioorganic & Medicinal Chemistry Letters, 2014 - Elsevier
Owing to their inherent three-dimensionality and structural novelty, spiro scaffolds have
been increasingly utilized in drug discovery. In this brief review, we highlight selected …

Pharmacophore models and pharmacophore-based virtual screening: concepts and applications exemplified on hydroxysteroid dehydrogenases

T Kaserer, KR Beck, M Akram, A Odermatt, D Schuster - Molecules, 2015 - mdpi.com
Computational methods are well-established tools in the drug discovery process and can be
employed for a variety of tasks. Common applications include lead identification and scaffold …

Tumors produce glucocorticoids by metabolite recycling, not synthesis, and activate Tregs to promote growth

MD Taves, S Otsuka, MA Taylor… - The Journal of …, 2023 - Am Soc Clin Investig
Glucocorticoids are steroid hormones with potent immunosuppressive properties. Their
primary source is the adrenals, where they are generated via de novo synthesis from …

Identification of 11β-HSD1 inhibitors through enhanced sampling methods

R Singh, VK Bhardwaj, P Das, R Purohit - Chemical Communications, 2022 - pubs.rsc.org
Aminoarylbenzosuberene (AAB) molecules were chosen for in silico analysis to develop
effective and more competent 11β-hydroxysteroid dehydrogenase (11β-HSD1) protein …

Navigating the Pauson–Khand reaction in total syntheses of complex natural products

Z Yang - Accounts of Chemical Research, 2021 - ACS Publications
Conspectus “Total synthesis endeavors provide wonderful opportunities to discover and
invent new synthetic reactions as a means to advance organic synthesis in general. Such …

11β‐Hydroxysteroid dehydrogenase and the brain: Not (yet) lost in translation

J Seckl - Journal of Internal Medicine, 2024 - Wiley Online Library
beta‐hydroxysteroid dehydrogenases (11β‐HSDs) catalyse the conversion of active 11‐
hydroxy glucocorticoids (cortisol, corticosterone) and their inert 11‐keto forms (cortisone, 11 …

[HTML][HTML] Glucocorticoid activation by HSD11B1 limits T cell-driven interferon signaling and response to PD-1 blockade in melanoma

LMN Melo, D Herrera-Rios, D Hinze… - … for Immunotherapy of …, 2023 - ncbi.nlm.nih.gov
Background Immune responses against tumors are subject to negative feedback regulation.
Immune checkpoint inhibitors (ICIs) blocking Programmed cell death protein 1 (PD-1), a …

Steroid and xenobiotic receptor signalling in apoptosis and autophagy of the nervous system

A Wnuk, M Kajta - International journal of molecular sciences, 2017 - mdpi.com
Apoptosis and autophagy are involved in neural development and in the response of the
nervous system to a variety of insults. Apoptosis is responsible for cell elimination, whereas …

Rhodium (III)-catalyzed site-selective C–H alkylation and arylation of pyridones using organoboron reagents

P Peng, J Wang, H Jiang, H Liu - Organic letters, 2016 - ACS Publications
In this study we developed a method for the pyridine-directed, rhodium-catalyzed, site-
selective C–H alkylation and arylation of pyridones using commercially available …

Cortisol as a target for treating mental disorders: a promising avenue for therapy

VK Patel, A Vaishnaw, E Shirbhate… - Mini Reviews in …, 2024 - ingentaconnect.com
Cortisol, commonly known as the" stress hormone," plays a critical role in the body's
response to stress. Elevated cortisol levels have been associated with various mental …