Gretchen M Schroeder
Overview
Explore the profile of Gretchen M Schroeder including associated specialties, affiliations and a list of published articles.
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24
Citations
427
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Recent Articles
1.
Jecs E, Tahirovic Y, Wilson R, Miller E, Kim M, Truax V, et al.
J Med Chem
. 2022 Feb;
65(5):4058-4084.
PMID: 35179893
Our first-generation CXCR4 antagonist TIQ15 was rationally modified to improve drug-like properties. Introducing a nitrogen atom into the aromatic portion of the tetrahydroisoquinoline ring led to several heterocyclic variants including...
2.
Cherney E, Zhang L, Lo J, Huynh T, Wei D, Ahuja V, et al.
J Med Chem
. 2022 Feb;
65(4):3518-3538.
PMID: 35108011
The identification of agonists of the stimulator of interferon genes (STING) pathway has been an area of intense research due to their potential to enhance innate immune response and tumor...
3.
Nguyen H, Tahirovic Y, Truax V, Wilson R, Jecs E, Miller E, et al.
ACS Med Chem Lett
. 2021 Oct;
12(10):1605-1612.
PMID: 34676043
This work surveys a variety of diamino-heterocycles as an isosteric replacement for the piperazine substructure of our previously disclosed piperarinyl-tetrahydroisoquinoline containing CXCR4 antagonists. A late-stage Buchwald coupling route was developed...
4.
Katzman B, Cox B, Prosser A, Alcaraz A, Murat B, Heroux M, et al.
ACS Med Chem Lett
. 2019 Jan;
10(1):67-73.
PMID: 30655949
The rationale for the structural and mechanistic basis of a tetrahydroisoquinoline (THIQ) based series of CXCR4 antagonists is presented. Using the previously reported crystal structures which reveal two distinct binding...
5.
Nguyen H, Kim M, Wilson R, Butch C, Kuo K, Miller E, et al.
J Med Chem
. 2018 Jul;
61(16):7168-7188.
PMID: 30052039
CXCR4 is a G-protein-coupled receptor that interacts with its cognate ligand, CXCL12, to synchronize many physiological responses and pathological processes. Disruption of the CXCL12-CXCR4 circuitry by small-molecule antagonists has emerged...
6.
Discovery of -Alkyl Piperazine Side Chain Based CXCR4 Antagonists with Improved Drug-like Properties
Tahirovic Y, Truax V, Wilson R, Jecs E, Nguyen H, Miller E, et al.
ACS Med Chem Lett
. 2018 May;
9(5):446-451.
PMID: 29795757
A novel series of CXCR4 antagonists with piperidinyl and piperazinyl alkylamine side chains designed as butyl amine replacements are described. Several of these compounds showed similar activity to the parent...
7.
Jecs E, Miller E, Wilson R, Nguyen H, Tahirovic Y, Katzman B, et al.
ACS Med Chem Lett
. 2018 Feb;
9(2):89-93.
PMID: 29456793
A structure-activity relationship study of potent TIQ15-derived CXCR4 antagonists is reported. In this investigation, the TIQ15 side-chain was constrained to improve its drug properties. The cyclohexylamino congener was found to...
8.
Miller E, Jecs E, Truax V, Katzman B, Tahirovic Y, Wilson R, et al.
J Med Chem
. 2018 Jan;
61(3):946-979.
PMID: 29350534
CXCR4 is a seven-transmembrane receptor expressed by hematopoietic stem cells and progeny, as well as by ≥48 different cancers types. CXCL12, the only chemokine ligand of CXCR4, is secreted within...
9.
Wilson R, Jecs E, Miller E, Nguyen H, Tahirovic Y, Truax V, et al.
ACS Med Chem Lett
. 2018 Jan;
9(1):17-22.
PMID: 29348805
CXCR4 is the most common chemokine receptor expressed on the surface of many cancer cell types. In comparison to normal cells, cancer cells overexpress CXCR4, which correlates with cancer cell...
10.
Donnell A, Zhang Y, Stang E, Wei D, Tebben A, Perez H, et al.
Bioorg Med Chem Lett
. 2017 Nov;
27(23):5267-5271.
PMID: 29102228
Macrocyclic pyrrolobenzodiazepine dimers were designed and evaluated for use as antibody-drug conjugate payloads. Initial structure-activity exploration established that macrocyclization could increase the potency of PBD dimers compared with non-macrocyclic analogs....