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Krista Menard

Explore the profile of Krista Menard including associated specialties, affiliations and a list of published articles. Areas
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Articles 12
Citations 336
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Recent Articles
1.
Obermajer N, Zwolak A, van de Ven K, Versmissen S, Menard K, Rogers K, et al.
iScience . 2025 Mar; 28(3):111876. PMID: 40060890
T cell-redirecting bispecific antibodies (bsAbs) to treat advanced stage solid tumors are gaining interest after recent clinical successes. The immune checkpoint human leukocyte antigen G (HLA-G) is expressed in several...
2.
Mattson Cypert B, Menard K, Chu G, McDevitt T, Verona R, Rupnow B, et al.
Mol Cancer Ther . 2025 Feb; PMID: 40008870
Prostate cancer is considered immunologically "cold", with low mutational burden, tumor-infiltrating immune cells, and PD-L1 levels, culminating in poor response to immune checkpoint therapies. Bispecific CD3 redirection antibodies can elicit...
3.
Hill M, Fang H, Norris D, Delucca G, Huang H, DeBenedetto M, et al.
ACS Med Chem Lett . 2022 Jul; 13(7):1165-1171. PMID: 35859878
We describe the synthesis of triazole-containing carboline derivatives and their utility as bromodomain and extra-terminal (BET) inhibitors. A convergent synthetic route permitted the detailed investigation of deuteration and fluorination strategies...
4.
Gavai A, Norris D, Delucca G, Tortolani D, Tokarski J, Dodd D, et al.
J Med Chem . 2021 Sep; 64(19):14247-14265. PMID: 34543572
Inhibition of the bromodomain and extra-terminal (BET) family of adaptor proteins is an attractive strategy for targeting transcriptional regulation of key oncogenes, such as c-MYC. Starting with the screening hit...
5.
Hill M, Fang H, Tokarski J, Fanslau C, Haarhoff Z, Huang C, et al.
Bioorg Med Chem Lett . 2021 May; 44:128108. PMID: 33991625
We describe our efforts to identify structurally diverse leads in the triazole-containing N1-carboline series of bromodomain and extra-terminal inhibitors. Replacement of the N5 "cap" phenyl moiety with various heteroaryls, coupled...
6.
Tu M, Lee F, Jones R, Kimball A, Saravia E, Graziano R, et al.
Sci Adv . 2019 Feb; 5(2):eaav2437. PMID: 30801016
While a fraction of cancer patients treated with anti-PD-1 show durable therapeutic responses, most remain unresponsive, highlighting the need to better understand and improve these therapies. Using an in vivo...
7.
Shen H, Wang L, Chen W, Menard K, Hong Y, Tian Y, et al.
Acta Pharm Sin B . 2016 Oct; 6(5):460-467. PMID: 27709015
To assess targeting of an epothilone folate conjugate (BMS-753493) to the folate receptor (FR)-overexpressed tumor in mice bearing both FR+ and FR- tumors, a series of experiments were conducted by...
8.
Gavai A, Quesnelle C, Norris D, Han W, Gill P, Shan W, et al.
ACS Med Chem Lett . 2015 May; 6(5):523-7. PMID: 26005526
Structure-activity relationships in a series of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides identified highly potent inhibitors of γ-secretase mediated signaling of Notch1/2/3/4 receptors. On the basis of its robust in vivo efficacy at tolerated doses...
9.
Shan W, Balog A, Quesnelle C, Gill P, Han W, Norris D, et al.
Bioorg Med Chem Lett . 2015 Apr; 25(9):1905-9. PMID: 25857941
This Letter describes synthesis, SAR, and biological activity of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides as inhibitors of γ-secretase mediated signaling of Notch receptors. Optimization of this series led to the identification of BMS-871 (compound...
10.
Ross-Macdonald P, de Silva H, Patel V, Truong A, He A, Neuhaus I, et al.
Bioorg Med Chem . 2011 Dec; 20(6):1961-72. PMID: 22137930
Therapeutic development of a targeted agent involves a series of decisions over additional activities that may be ignored, eliminated or pursued. This paper details the concurrent application of two methods...